PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 23583259-4 2013 In transiently transfected HepG2 cells, rilpivirine, etravirine, and efavirenz, but not nevirapine or delavirdine, activated human, mouse, and rat PXR. efavirenz 69-78 nuclear receptor subfamily 1, group I, member 2 Rattus norvegicus 147-150 23583259-6 2013 Rilpivirine, etravirine, and efavirenz, but not nevirapine or delavirdine, increased hPXR target gene (CYP3A4) expression in primary cultures of human hepatocytes. efavirenz 29-38 nuclear receptor subfamily 1 group I member 2 Homo sapiens 85-89 23583259-6 2013 Rilpivirine, etravirine, and efavirenz, but not nevirapine or delavirdine, increased hPXR target gene (CYP3A4) expression in primary cultures of human hepatocytes. efavirenz 29-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-109 23583259-8 2013 Rilpivirine, etravirine, and efavirenz, but not nevirapine or delavirdine, were identified as agonists of hPXR, as assessed in mechanistic experiments, and inducers of CYP3A4, as determined in primary cultures of human hepatocytes. efavirenz 29-38 nuclear receptor subfamily 1 group I member 2 Homo sapiens 106-110 23583259-8 2013 Rilpivirine, etravirine, and efavirenz, but not nevirapine or delavirdine, were identified as agonists of hPXR, as assessed in mechanistic experiments, and inducers of CYP3A4, as determined in primary cultures of human hepatocytes. efavirenz 29-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 168-174 23563240-4 2013 EFV treatment led to cell proliferation arrest and cell death of the NHKs by inducing autophagy mediated by proteasome-dependent degradation of p53. efavirenz 0-3 tumor protein p53 Homo sapiens 144-147 23563240-5 2013 EFV also reduced the levels of mTOR and active ERK signaling in NHKs. efavirenz 0-3 mechanistic target of rapamycin kinase Homo sapiens 31-35 23467454-3 2013 Drugs metabolized mainly by CYP2B6 include artemisinin, bupropion, cyclophosphamide, efavirenz, ketamine, and methadone. efavirenz 85-94 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 28-34 23372109-8 2013 For patients receiving previously efavirenz, there was a significant reduction in TC (-23 mg/dL; -13%) and LDL-C (-25 mg/dL; -21%) levels and a trend to a better TG level (-38 mg/dL; -21%;P = .06). efavirenz 34-43 component of oligomeric golgi complex 2 Homo sapiens 107-112 23385314-2 2013 The present study showed that efavirenz was a potent competitive inhibitor of CYP2B6 (average K(i) = 1.68 microM in HLMs and K(i) = 1.38 microM in expressed CYP2B6) and CYP2C8 (K(i) = 4.78 microM in pooled HLMs and K(i) = 4.80 microM in HLMs with CYP2C8*3/*3 genotype). efavirenz 30-39 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 78-84 23385314-2 2013 The present study showed that efavirenz was a potent competitive inhibitor of CYP2B6 (average K(i) = 1.68 microM in HLMs and K(i) = 1.38 microM in expressed CYP2B6) and CYP2C8 (K(i) = 4.78 microM in pooled HLMs and K(i) = 4.80 microM in HLMs with CYP2C8*3/*3 genotype). efavirenz 30-39 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 157-163 23385314-2 2013 The present study showed that efavirenz was a potent competitive inhibitor of CYP2B6 (average K(i) = 1.68 microM in HLMs and K(i) = 1.38 microM in expressed CYP2B6) and CYP2C8 (K(i) = 4.78 microM in pooled HLMs and K(i) = 4.80 microM in HLMs with CYP2C8*3/*3 genotype). efavirenz 30-39 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 169-175 23385314-2 2013 The present study showed that efavirenz was a potent competitive inhibitor of CYP2B6 (average K(i) = 1.68 microM in HLMs and K(i) = 1.38 microM in expressed CYP2B6) and CYP2C8 (K(i) = 4.78 microM in pooled HLMs and K(i) = 4.80 microM in HLMs with CYP2C8*3/*3 genotype). efavirenz 30-39 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 247-253 23385314-3 2013 Efavirenz was a moderate inhibitor of CYP2C9 (K(i) = 19.46 microM) and CYP2C19 (K(i) = 21.31 microM); and a weak inhibitor of CYP3A (K(i) = 40.33 microM). efavirenz 0-9 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 38-44 23385314-3 2013 Efavirenz was a moderate inhibitor of CYP2C9 (K(i) = 19.46 microM) and CYP2C19 (K(i) = 21.31 microM); and a weak inhibitor of CYP3A (K(i) = 40.33 microM). efavirenz 0-9 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 71-78 23385314-3 2013 Efavirenz was a moderate inhibitor of CYP2C9 (K(i) = 19.46 microM) and CYP2C19 (K(i) = 21.31 microM); and a weak inhibitor of CYP3A (K(i) = 40.33 microM). efavirenz 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 126-131 25505649-2 2013 Artemether is a substrate of CYP3A4 and CYP2B6, antiretrovirals such as efavirenz induce these enzymes and have the potential to reduce artemether pharmacokinetic exposure. efavirenz 72-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-35 25505649-2 2013 Artemether is a substrate of CYP3A4 and CYP2B6, antiretrovirals such as efavirenz induce these enzymes and have the potential to reduce artemether pharmacokinetic exposure. efavirenz 72-81 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 40-46 23302874-1 2013 Efavirenz (EFV), a nonnucleoside reverse transcriptase (RT) inhibitor, also inhibits HIV-1 particle release through enhanced Gag/Gag-Pol processing by protease (PR). efavirenz 0-9 Pr55(Gag) Human immunodeficiency virus 1 125-128 23302874-1 2013 Efavirenz (EFV), a nonnucleoside reverse transcriptase (RT) inhibitor, also inhibits HIV-1 particle release through enhanced Gag/Gag-Pol processing by protease (PR). efavirenz 0-9 Gag-Pol Human immunodeficiency virus 1 129-136 23302874-1 2013 Efavirenz (EFV), a nonnucleoside reverse transcriptase (RT) inhibitor, also inhibits HIV-1 particle release through enhanced Gag/Gag-Pol processing by protease (PR). efavirenz 11-14 Pr55(Gag) Human immunodeficiency virus 1 125-128 23302874-1 2013 Efavirenz (EFV), a nonnucleoside reverse transcriptase (RT) inhibitor, also inhibits HIV-1 particle release through enhanced Gag/Gag-Pol processing by protease (PR). efavirenz 11-14 Gag-Pol Human immunodeficiency virus 1 129-136 23302874-2 2013 To better understand the mechanisms of the EFV-mediated enhancement of Gag processing, we examined the intracellular localization of Gag/Gag-Pol processing products and their precursors. efavirenz 43-46 Pr55(Gag) Human immunodeficiency virus 1 71-74 23302874-2 2013 To better understand the mechanisms of the EFV-mediated enhancement of Gag processing, we examined the intracellular localization of Gag/Gag-Pol processing products and their precursors. efavirenz 43-46 Pr55(Gag) Human immunodeficiency virus 1 133-136 23302874-2 2013 To better understand the mechanisms of the EFV-mediated enhancement of Gag processing, we examined the intracellular localization of Gag/Gag-Pol processing products and their precursors. efavirenz 43-46 Gag-Pol Human immunodeficiency virus 1 137-144 23302874-7 2013 Forster"s fluorescence resonance energy transfer assay revealed that Gag-Pol precursor dimerization occurred mainly at the PM and that EFV induced a significant increase of the Gag-Pol dimerization at the PM. efavirenz 135-138 Gag-Pol Human immunodeficiency virus 1 177-184 23254426-0 2013 Impact of pharmacogenetic markers of CYP2B6, clinical factors, and drug-drug interaction on efavirenz concentrations in HIV/tuberculosis-coinfected patients. efavirenz 92-101 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 37-43 22642697-9 2013 CONCLUSION: CYP3A inducers, rifampicin and efavirenz, can reduce telaprevir exposure to varying degrees based on their potency. efavirenz 43-52 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-17 23640958-0 2013 Efavirenz intoxication due to a new CYP2B6 constellation. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 36-42 23555843-4 2013 Additionally, EFV was found to activate glycogen synthase kinase 3 beta (GSK3beta) in platelets, and we now show that valproic acid (VPA), a known GSK3beta inhibitor, was able to attenuate the release of sCD40L in HIV infected individuals receiving EFV, and in isolated human platelets. efavirenz 14-17 glycogen synthase kinase 3 beta Homo sapiens 40-71 23555843-4 2013 Additionally, EFV was found to activate glycogen synthase kinase 3 beta (GSK3beta) in platelets, and we now show that valproic acid (VPA), a known GSK3beta inhibitor, was able to attenuate the release of sCD40L in HIV infected individuals receiving EFV, and in isolated human platelets. efavirenz 14-17 glycogen synthase kinase 3 beta Homo sapiens 73-81 23555843-4 2013 Additionally, EFV was found to activate glycogen synthase kinase 3 beta (GSK3beta) in platelets, and we now show that valproic acid (VPA), a known GSK3beta inhibitor, was able to attenuate the release of sCD40L in HIV infected individuals receiving EFV, and in isolated human platelets. efavirenz 14-17 glycogen synthase kinase 3 beta Homo sapiens 147-155 23555843-4 2013 Additionally, EFV was found to activate glycogen synthase kinase 3 beta (GSK3beta) in platelets, and we now show that valproic acid (VPA), a known GSK3beta inhibitor, was able to attenuate the release of sCD40L in HIV infected individuals receiving EFV, and in isolated human platelets. efavirenz 249-252 glycogen synthase kinase 3 beta Homo sapiens 73-81 23133441-3 2012 The aim of the study was to evaluate the role of polymorphisms in ABCB1 gene on plasma efavirenz levels and treatment response in the form of change in viral load and CD-4 cell count in HIV/AIDS patients receiving efavirenz-containing highly active antiretroviral treatment regimens. efavirenz 87-96 ATP binding cassette subfamily B member 1 Homo sapiens 66-71 23372824-8 2013 Children receiving EFV experienced increases in both CD4(+) T-cell percentage and weight-for-age z-score during follow-up, such that levels were comparable to children receiving NVP after two years of ART. efavirenz 19-22 CD4 molecule Homo sapiens 53-56 22950382-11 2012 CYP2B6-516G > T polymorphism was the only factor associated with high plasma EFV levels. efavirenz 80-83 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 22918158-2 2012 EFV is a known inducer of cytochrome P450 3A4, which converts artemether to dihydroartemisinin (DHA) that is also active and metabolizes longer acting lumefantrine (LR). efavirenz 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-45 22933296-5 2012 After three doses over 4 days of EFV monotherapy, 103N mutations (AAC and AAT) rapidly emerged and increased in the population to levels of ~20%, indicating that they were present prior to EFV exposure. efavirenz 33-36 serpin family A member 1 Homo sapiens 74-77 22678819-6 2012 Finally, we demonstrated that FAP48 over-expression was able to influence the capacity of some HIV drugs, Saquinavir and Efavirenz, but not Stavudine, Amprenavir, and Indinavir to inhibit adipocyte formation. efavirenz 121-130 glomulin, FKBP associated protein Homo sapiens 30-35 22933296-5 2012 After three doses over 4 days of EFV monotherapy, 103N mutations (AAC and AAT) rapidly emerged and increased in the population to levels of ~20%, indicating that they were present prior to EFV exposure. efavirenz 33-36 glycine-N-acyltransferase Homo sapiens 66-69 22309114-8 2012 In addition, adults initiating EFV-based cART at higher baseline CD4(+) cell count values had more favorable outcomes compared to those initiating NVP-based cART. efavirenz 31-34 CD4 molecule Homo sapiens 65-68 22050695-3 2012 In this study, we examined in naive HIV-infected patients the in vivo effects of a highly active antiretroviral therapy (HAART) regimen, containing tenofovir-DF/emtricitabine/efavirenz, on PAF metabolism. efavirenz 175-184 PCNA clamp associated factor Homo sapiens 189-192 22050695-11 2012 Apart from its classical antiretroviral activities the tenofovir-DF/emtricitabine/efavirenz regimen also exhibited favorable effects on PAF metabolism and therefore may also display beneficial effects in some HIV-related conditions, such as cardiovascular disease (CVD), in which PAF is implicated. efavirenz 82-91 PCNA clamp associated factor Homo sapiens 136-139 22050695-11 2012 Apart from its classical antiretroviral activities the tenofovir-DF/emtricitabine/efavirenz regimen also exhibited favorable effects on PAF metabolism and therefore may also display beneficial effects in some HIV-related conditions, such as cardiovascular disease (CVD), in which PAF is implicated. efavirenz 82-91 PCNA clamp associated factor Homo sapiens 280-283 21719718-5 2012 The lopinavir/ritonavir dose of 500/125 mg bid administered with efavirenz most closely approximates the pharmacokinetic exposure of lopinavir/ritonavir 400/100 mg bid administered alone. efavirenz 65-74 BH3 interacting domain death agonist Homo sapiens 43-46 22398970-8 2012 Efavirenz induced hepatocyte CYP2B6 and CYP3A4 expression, activity, and methadone N-demethylation. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 29-35 22759796-8 2012 Genetic polymorphisms affecting the activity and/or the expression of cytochromes P450 or UGT isozymes and membrane drug transport proteins are highlighted and include such examples as the association of neurotoxicity with efavirenz, nephrotoxicity with tenofovir, hepatotoxicity with nevirapine, and hyperbilirubinemia with indinavir and atazanavir. efavirenz 223-232 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 90-93 22415932-0 2012 Drug interaction of efavirenz and midazolam: efavirenz activates the CYP3A-mediated midazolam 1"-hydroxylation in vitro. efavirenz 20-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-74 22415932-0 2012 Drug interaction of efavirenz and midazolam: efavirenz activates the CYP3A-mediated midazolam 1"-hydroxylation in vitro. efavirenz 45-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-74 22415932-3 2012 In vivo data suggested a possible acute activation of CYP3A4-catalyzed midazolam metabolism by efavirenz. efavirenz 95-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-60 22588604-2 2012 In order to determine the in vivo effects of efavirenz, a CAR activator, the expression of target genes was determined in duodenal biopsies obtained from 12 healthy volunteers before treatment and after 10 days of treatment with efavirenz; concomitant administration of the cholesterol inhibitor ezetimibe produced no significant difference. efavirenz 45-54 nuclear receptor subfamily 1 group I member 3 Homo sapiens 58-61 22398970-8 2012 Efavirenz induced hepatocyte CYP2B6 and CYP3A4 expression, activity, and methadone N-demethylation. efavirenz 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-46 22252501-4 2012 Efavirenz potently inhibited UGT1A4-mediated trifluoperazine N-glucuronidation and UGT1A9-mediated propofol glucuronidation, with K(i) values of 2.0 and 9.4 muM, respectively. efavirenz 0-9 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 30-36 22318618-2 2012 We evaluated the effects of multiple doses of efavirenz on omeprazole 5-hydroxylation (CYP2C19) and sulfoxidation (CYP3A). efavirenz 46-55 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 87-94 22321026-7 2012 Trials investigating the efficacy of once-daily co-formulated elvitegravir/cobicistat/emtricitabine/tenofovir (EVG/COBI/FTC/TDF) demonstrate a high rate of virologic suppression with fewer CNS and psychiatric adverse events compared with co-formulated efavirenz/emtricitabine/tenofovir. efavirenz 252-261 sex determining region Y Homo sapiens 124-127 22297387-7 2012 Efavirenz (single dose) slightly increased ezetimibe absorption and markedly decreased exposure to ezetimibe-glucuronide (single dose and multiple dose), which may be explained by inhibition of UGT1A1 and ABCB1 (in vitro data). efavirenz 0-9 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 194-200 22297387-7 2012 Efavirenz (single dose) slightly increased ezetimibe absorption and markedly decreased exposure to ezetimibe-glucuronide (single dose and multiple dose), which may be explained by inhibition of UGT1A1 and ABCB1 (in vitro data). efavirenz 0-9 ATP binding cassette subfamily B member 1 Homo sapiens 205-210 22252501-4 2012 Efavirenz potently inhibited UGT1A4-mediated trifluoperazine N-glucuronidation and UGT1A9-mediated propofol glucuronidation, with K(i) values of 2.0 and 9.4 muM, respectively. efavirenz 0-9 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 84-90 22252501-4 2012 Efavirenz potently inhibited UGT1A4-mediated trifluoperazine N-glucuronidation and UGT1A9-mediated propofol glucuronidation, with K(i) values of 2.0 and 9.4 muM, respectively. efavirenz 0-9 latexin Homo sapiens 158-161 22252501-6 2012 Efavirenz also moderately inhibited UGT1A1-mediated 17beta-estradiol 3-glucuronidation, with a K(i) value of 40.3 muM, but did not inhibit UGT1A6-mediated 1-naphthol glucuronidation. efavirenz 0-9 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 36-42 22252501-6 2012 Efavirenz also moderately inhibited UGT1A1-mediated 17beta-estradiol 3-glucuronidation, with a K(i) value of 40.3 muM, but did not inhibit UGT1A6-mediated 1-naphthol glucuronidation. efavirenz 0-9 latexin Homo sapiens 114-117 21958719-0 2011 Efavirenz and 8-hydroxyefavirenz induce cell death via a JNK- and BimEL-dependent mechanism in primary human hepatocytes. efavirenz 0-9 mitogen-activated protein kinase 8 Homo sapiens 57-60 21561322-4 2012 RESULTS: The medications with the highest effects were efavirenz with an ROR of 196 (95% CI, 86 to 447), lamivudine with an ROR of 60.2 (95% CI, 14.25 to 148), the combination abacavir sulfate/lamivudine/zidovudine with an ROR of 59.3, and nelfinavir with and ROR of 50.5, followed by nevirapine, lopinavir/ritonavir, and lamivudine/zidovudine. efavirenz 55-64 long intergenic non-protein coding RNA, regulator of reprogramming Homo sapiens 73-76 23082557-3 2012 The present study examined the influence of ABCB-1 polymorphisms on plasma nevirapine and efavirenz levels when co-administered with rifampicin in 124 HIV/TB patients who received nevirapine- (400 mg/day) (n = 59) and efavirenz- (600 mg/day) (n = 65) based ART. efavirenz 90-99 ATP binding cassette subfamily B member 1 Homo sapiens 44-50 21958719-3 2011 In the present study, incubation of primary human hepatocytes with synthetic 8-hydroxyEFV (8-OHEFV), which is the primary metabolite of EFV, resulted in cell death, caspase-3 activation and reactive oxygen species formation. efavirenz 86-89 caspase 3 Homo sapiens 165-174 21958719-6 2011 Treatment of primary human hepatocytes with EFV and 8-OHEFV also stimulated phosphorylation of c-Jun N-terminal kinase (JNK) as well as phosphorylation of the JNK substrate c-Jun. efavirenz 44-47 mitogen-activated protein kinase 8 Homo sapiens 95-118 21958719-6 2011 Treatment of primary human hepatocytes with EFV and 8-OHEFV also stimulated phosphorylation of c-Jun N-terminal kinase (JNK) as well as phosphorylation of the JNK substrate c-Jun. efavirenz 44-47 mitogen-activated protein kinase 8 Homo sapiens 120-123 21958719-6 2011 Treatment of primary human hepatocytes with EFV and 8-OHEFV also stimulated phosphorylation of c-Jun N-terminal kinase (JNK) as well as phosphorylation of the JNK substrate c-Jun. efavirenz 44-47 mitogen-activated protein kinase 8 Homo sapiens 159-162 21958719-6 2011 Treatment of primary human hepatocytes with EFV and 8-OHEFV also stimulated phosphorylation of c-Jun N-terminal kinase (JNK) as well as phosphorylation of the JNK substrate c-Jun. efavirenz 44-47 Jun proto-oncogene, AP-1 transcription factor subunit Homo sapiens 95-100 21803024-3 2011 The breast cancer resistant protein (BCRP, ABCG2) is known to be inhibited by EFV in vitro. efavirenz 78-81 ATP binding cassette subfamily G member 2 Rattus norvegicus 43-48 21803024-4 2011 Since ABCG2 is profusely expressed in the gastrointestinal tract, the aim of the present work was to thoroughly investigate whether the intestinal permeability of EFV is modulated by ABCG2. efavirenz 163-166 ATP binding cassette subfamily G member 2 Rattus norvegicus 6-11 21803024-4 2011 Since ABCG2 is profusely expressed in the gastrointestinal tract, the aim of the present work was to thoroughly investigate whether the intestinal permeability of EFV is modulated by ABCG2. efavirenz 163-166 ATP binding cassette subfamily G member 2 Rattus norvegicus 183-188 21803024-7 2011 Since the intestinal permeability of a drug could be associated with its in vivo absorbability, we suggest that the oral absorption of EFV is affected by modifications in the ABCG2 intestinal expression contributing to the intra-individual bioavailability variations. efavirenz 135-138 ATP binding cassette subfamily G member 2 Rattus norvegicus 175-180 21821736-0 2011 Q172H replacement overcomes effects on the metabolism of cyclophosphamide and efavirenz caused by CYP2B6 variant with Arg262. efavirenz 78-87 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 98-104 21821736-1 2011 There are a number of reports indicating that CYP2B6*6 (c.516G>T and c.785A>G) is responsible for decreased clearance of efavirenz (EFV), although increased disposition of cyclophosphamide (CPA) in individuals with this polymorphism was observed. efavirenz 138-141 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 21395646-0 2011 In silico prediction of efavirenz and rifampicin drug-drug interaction considering weight and CYP2B6 phenotype. efavirenz 24-33 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 94-100 21301907-1 2011 Mounting evidence thus far indicates that human cytochrome P450 2B6 (CYP2B6), an enzyme expressed at a relatively low level functionally, is primarily responsible for the metabolism of several clinically relevant drugs, including propofol, efavirenz, bupropion, mephobarbital, and the propofol analog 2,6-di-sec-butyl phenol. efavirenz 240-249 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 48-67 21301907-1 2011 Mounting evidence thus far indicates that human cytochrome P450 2B6 (CYP2B6), an enzyme expressed at a relatively low level functionally, is primarily responsible for the metabolism of several clinically relevant drugs, including propofol, efavirenz, bupropion, mephobarbital, and the propofol analog 2,6-di-sec-butyl phenol. efavirenz 240-249 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 69-75 21659470-1 2011 In this study, metabolism of bupropion, efavirenz, and 7-ethoxy-4-trifluoromethylcoumarin (7-EFC) by CYP2B6 wild type (CYP2B6.1) and six polymorphic variants (CYP2B6.4 to CYP2B6.9) was investigated in a reconstituted system to gain a better understanding of the effects of the mutations on the catalytic properties of these naturally occurring variants. efavirenz 40-49 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 101-107 21659470-1 2011 In this study, metabolism of bupropion, efavirenz, and 7-ethoxy-4-trifluoromethylcoumarin (7-EFC) by CYP2B6 wild type (CYP2B6.1) and six polymorphic variants (CYP2B6.4 to CYP2B6.9) was investigated in a reconstituted system to gain a better understanding of the effects of the mutations on the catalytic properties of these naturally occurring variants. efavirenz 40-49 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 119-125 21659470-1 2011 In this study, metabolism of bupropion, efavirenz, and 7-ethoxy-4-trifluoromethylcoumarin (7-EFC) by CYP2B6 wild type (CYP2B6.1) and six polymorphic variants (CYP2B6.4 to CYP2B6.9) was investigated in a reconstituted system to gain a better understanding of the effects of the mutations on the catalytic properties of these naturally occurring variants. efavirenz 40-49 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 119-125 21659470-1 2011 In this study, metabolism of bupropion, efavirenz, and 7-ethoxy-4-trifluoromethylcoumarin (7-EFC) by CYP2B6 wild type (CYP2B6.1) and six polymorphic variants (CYP2B6.4 to CYP2B6.9) was investigated in a reconstituted system to gain a better understanding of the effects of the mutations on the catalytic properties of these naturally occurring variants. efavirenz 40-49 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 119-125 21659470-3 2011 The steady-state turnover rates for the hydroxylation of bupropion and efavirenz and the O-deethylation of 7-EFC showed that these mutations significantly alter the catalytic activities of CYP2B6. efavirenz 71-80 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 189-195 21659470-4 2011 It was found that CYP2B6.6 exhibits 4- and 27-fold increases in the K(m) values for the hydroxylation of bupropion and efavirenz, respectively, and CYP2B6.8 completely loses its ability to metabolize any of the substrates under normal turnover conditions. efavirenz 119-128 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 18-24 21659470-4 2011 It was found that CYP2B6.6 exhibits 4- and 27-fold increases in the K(m) values for the hydroxylation of bupropion and efavirenz, respectively, and CYP2B6.8 completely loses its ability to metabolize any of the substrates under normal turnover conditions. efavirenz 119-128 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 148-154 21080015-2 2011 We used the docking method to explore possible binding modes of an entry inhibitor (maraviroc) and non-nucleoside reverse transcriptase inhibitors (delavirdine, efavirenz and etravirine) to cytochrome P450 3A4 (CYP3A4). efavirenz 161-170 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 190-209 21080015-2 2011 We used the docking method to explore possible binding modes of an entry inhibitor (maraviroc) and non-nucleoside reverse transcriptase inhibitors (delavirdine, efavirenz and etravirine) to cytochrome P450 3A4 (CYP3A4). efavirenz 161-170 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 211-217 21080015-4 2011 We observed that efavirenz and etravirine induce metabolism of co-administered drugs by binding to a unique position in the active site of CYP3A4. efavirenz 17-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-145 21395646-8 2011 Increasing the efavirenz dose during concomitant rifampicin was predicted to be most successful in patients over 50 kg regardless of CYP2B6 status. efavirenz 15-24 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 133-139 21091096-7 2011 Protease inhibitor (PI) usage was similar in both M-IRS categories (43 vs. 38%; p = 0.38) but increased use of efavirenz was seen in M-IRS (47 vs. 36%; p = 0.07) and nevirapine in the non-M-IRS groups (10 vs. 20%; p = 0.05). efavirenz 111-120 isoleucyl-tRNA synthetase 1 Homo sapiens 135-138 21091096-7 2011 Protease inhibitor (PI) usage was similar in both M-IRS categories (43 vs. 38%; p = 0.38) but increased use of efavirenz was seen in M-IRS (47 vs. 36%; p = 0.07) and nevirapine in the non-M-IRS groups (10 vs. 20%; p = 0.05). efavirenz 111-120 isoleucyl-tRNA synthetase 1 Homo sapiens 135-138 20699409-6 2010 Cotreatment of avasimibe or efavirenz with 10 muM rifampicin was found to reduce CYP3A activities induced by rifampicin at a lower rate than treatment with rifampicin alone, whereas treatment with phenobarbital and carbamazepine had no effect. efavirenz 28-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-86 20861742-5 2010 Darunavir, fosamprenavir, lopinavir, nelfinavir, tipranavir, efavirenz, and abacavir increased CYP3A4 and/or CYP2B6 promoter activity, some through constitutive androstane receptor but mainly through PXR. efavirenz 61-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 20861742-5 2010 Darunavir, fosamprenavir, lopinavir, nelfinavir, tipranavir, efavirenz, and abacavir increased CYP3A4 and/or CYP2B6 promoter activity, some through constitutive androstane receptor but mainly through PXR. efavirenz 61-70 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 109-115 20861742-5 2010 Darunavir, fosamprenavir, lopinavir, nelfinavir, tipranavir, efavirenz, and abacavir increased CYP3A4 and/or CYP2B6 promoter activity, some through constitutive androstane receptor but mainly through PXR. efavirenz 61-70 nuclear receptor subfamily 1 group I member 3 Homo sapiens 148-180 20861742-5 2010 Darunavir, fosamprenavir, lopinavir, nelfinavir, tipranavir, efavirenz, and abacavir increased CYP3A4 and/or CYP2B6 promoter activity, some through constitutive androstane receptor but mainly through PXR. efavirenz 61-70 nuclear receptor subfamily 1 group I member 2 Homo sapiens 200-203 21090588-4 2010 The effect of efavirenz on the solution conformations of p66 and p51 monomers was studied by hydrogen-deuterium exchange mass spectrometry (HXMS) and Fourier transform ion cyclotron resonance mass spectrometry (FT-ICR MS). efavirenz 14-23 DNA polymerase delta 3, accessory subunit Homo sapiens 57-60 21090588-4 2010 The effect of efavirenz on the solution conformations of p66 and p51 monomers was studied by hydrogen-deuterium exchange mass spectrometry (HXMS) and Fourier transform ion cyclotron resonance mass spectrometry (FT-ICR MS). efavirenz 14-23 tumor protein p63 Homo sapiens 65-68 21073442-10 2010 In previously differentiated adipocytes, EFV caused a significant reduction in PPARgamma and adiponectin expression, whereas LPV/r did not. efavirenz 41-44 peroxisome proliferator activated receptor gamma Homo sapiens 79-88 20660679-2 2010 In vitro data indicate that efavirenz induces several ATP-binding cassette (ABC) transporters, and pharmacogenetic studies found an association between ABCB1(C3435T) and efavirenz exposure and between this polymorphism and improved virological outcomes. efavirenz 28-37 ATP binding cassette subfamily B member 6 (Langereis blood group) Homo sapiens 54-74 20660679-2 2010 In vitro data indicate that efavirenz induces several ATP-binding cassette (ABC) transporters, and pharmacogenetic studies found an association between ABCB1(C3435T) and efavirenz exposure and between this polymorphism and improved virological outcomes. efavirenz 28-37 ATP binding cassette subfamily B member 6 (Langereis blood group) Homo sapiens 76-79 20660679-2 2010 In vitro data indicate that efavirenz induces several ATP-binding cassette (ABC) transporters, and pharmacogenetic studies found an association between ABCB1(C3435T) and efavirenz exposure and between this polymorphism and improved virological outcomes. efavirenz 28-37 ATP binding cassette subfamily B member 1 Homo sapiens 152-157 21073442-10 2010 In previously differentiated adipocytes, EFV caused a significant reduction in PPARgamma and adiponectin expression, whereas LPV/r did not. efavirenz 41-44 adiponectin, C1Q and collagen domain containing Homo sapiens 93-104 19674747-10 2010 Chemical JNK inhibitor and dominant negative mutant JNK and IkappaBalpha adenoviruses effectively blocked the effects of EFV on HCAECs. efavirenz 121-124 mitogen-activated protein kinase 8 Homo sapiens 9-12 20090545-0 2010 Prospective, randomized, open label trial of Efavirenz vs Lopinavir/Ritonavir in HIV+ treatment-naive subjects with CD4+<200 cell/mm3 in Mexico. efavirenz 45-54 CD4 molecule Homo sapiens 116-119 20338069-1 2010 BACKGROUND: Cytochrome P450 2B6 (CYP2B6) metabolizes efavirenz and nevirapine, the major core antiretroviral drugs for HIV in Thailand. efavirenz 53-62 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 12-31 20338069-1 2010 BACKGROUND: Cytochrome P450 2B6 (CYP2B6) metabolizes efavirenz and nevirapine, the major core antiretroviral drugs for HIV in Thailand. efavirenz 53-62 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 33-39 20408889-6 2010 RESULTS: Efavirenz induced growth in MCF-7 cells with an estimated effective concentration for half-maximal growth (EC(50)) of 15.7 muM. efavirenz 9-18 latexin Homo sapiens 132-135 20408889-8 2010 Further, efavirenz binds directly to the ER [inhibitory concentration for half maximal binding (IC(50)) of ~52 muM] at a roughly 1000-fold higher concentration than observed with 17beta-oestradiol. efavirenz 9-18 latexin Homo sapiens 111-114 20404738-4 2010 Mean change in baseline CD4 count was 240 and 225 cells per cubic millimeter in the raltegravir and efavirenz groups, respectively [Delta (95% confidence interval) = 15 (-13 to 42)]. efavirenz 100-109 CD4 molecule Homo sapiens 24-27 20860463-12 2010 CONCLUSION: Our study corroborates previous findings indicating that knowledge of CYP2B6 genetic status should be taken into account for an EFV treatment. efavirenz 140-143 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 82-88 19674747-10 2010 Chemical JNK inhibitor and dominant negative mutant JNK and IkappaBalpha adenoviruses effectively blocked the effects of EFV on HCAECs. efavirenz 121-124 mitogen-activated protein kinase 8 Homo sapiens 52-55 19674747-10 2010 Chemical JNK inhibitor and dominant negative mutant JNK and IkappaBalpha adenoviruses effectively blocked the effects of EFV on HCAECs. efavirenz 121-124 NFKB inhibitor alpha Homo sapiens 60-72 19702527-4 2009 CYP2B6 can metabolise approximately 8% of clinically used drugs (n > 60), including cyclophosphamide, ifosfamide, tamoxifen, ketamine, artemisinin, nevirapine, efavirenz, bupropion, sibutramine, and propofol. efavirenz 163-172 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 20002083-4 2009 WHAT THIS STUDY ADDS: * In the present work, we studied the effect of EFV on the activity of PON-1 and showed, for the first time, that EFV-based antiretroviral therapy is associated with a better antioxidant function, i.e. with a higher PON-1 activity. efavirenz 70-73 paraoxonase 1 Homo sapiens 93-98 20002083-4 2009 WHAT THIS STUDY ADDS: * In the present work, we studied the effect of EFV on the activity of PON-1 and showed, for the first time, that EFV-based antiretroviral therapy is associated with a better antioxidant function, i.e. with a higher PON-1 activity. efavirenz 136-139 paraoxonase 1 Homo sapiens 93-98 20002083-4 2009 WHAT THIS STUDY ADDS: * In the present work, we studied the effect of EFV on the activity of PON-1 and showed, for the first time, that EFV-based antiretroviral therapy is associated with a better antioxidant function, i.e. with a higher PON-1 activity. efavirenz 136-139 paraoxonase 1 Homo sapiens 238-243 20002083-10 2009 The influence of treatment with EFV, HDL-c and CD4 cell count on PON-1 activity was analysed. efavirenz 32-35 paraoxonase 1 Homo sapiens 65-70 20002083-13 2009 CONCLUSIONS: EFV-based antiretroviral regimens are associated with HDL particles with a better antioxidant function, i.e. with a higher PON-1 activity. efavirenz 13-16 paraoxonase 1 Homo sapiens 136-141 20386083-2 2010 We studied MRP1 expression and function in healthy volunteers treated with darunavir/ritonavir and efavirenz. efavirenz 99-108 CD9 molecule Homo sapiens 11-15 20386083-10 2010 MRP1 efflux function was increased after efavirenz administration (GMR 3.13, 95% CI 2.73-3.59; P<0.001) and darunavir/ritonavir plus efavirenz coadministration (GMR 4.35, 95% CI 3.35-5.68; P<0.001), but not after darunavir/ritonavir administration (GMR 1.06, 95% CI 0.80-1.42; P=0.42). efavirenz 41-50 CD9 molecule Homo sapiens 0-4 20201776-3 2010 Since EFV is most commonly used with ATV and RTV, the known CYP inhibitors, we evaluated the effects of combinations of these agents on the CYP3A4 induction by EFV. efavirenz 160-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 140-146 20201776-4 2010 We determined the induction of CYP3A4 by EFV, RTV, ATV, EFV+RTV, EFV+ATV, EFV+RTV+ATV and rifampicin (RIF) employing primary human hepatocytes from 3 donors. efavirenz 41-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 20201776-4 2010 We determined the induction of CYP3A4 by EFV, RTV, ATV, EFV+RTV, EFV+ATV, EFV+RTV+ATV and rifampicin (RIF) employing primary human hepatocytes from 3 donors. efavirenz 56-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 20201776-4 2010 We determined the induction of CYP3A4 by EFV, RTV, ATV, EFV+RTV, EFV+ATV, EFV+RTV+ATV and rifampicin (RIF) employing primary human hepatocytes from 3 donors. efavirenz 56-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 20201776-4 2010 We determined the induction of CYP3A4 by EFV, RTV, ATV, EFV+RTV, EFV+ATV, EFV+RTV+ATV and rifampicin (RIF) employing primary human hepatocytes from 3 donors. efavirenz 56-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 20201776-6 2010 CYP3A4 activity (testosterone-6beta-hydroxylation) was induced by EFV (3 fold) and RIF (4 fold), but was significantly suppressed in the presence of RTV and ATV. efavirenz 66-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 20201776-8 2010 hPXR activation data in LS180 cells were consistent with the induction of transcripts and the estimated EC(50) values were 0.87 microM, 0.44 microM and 3.7 microM for RIF, RTV and EFV, respectively. efavirenz 180-183 nuclear receptor subfamily 1 group I member 2 Homo sapiens 0-4 20201776-10 2010 This observation corresponds to the clinical observations of attenuated CYP3A4 induction by EFV induction in the presence of RTV and other protease inhibitors (PIs). efavirenz 92-95 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 20001610-6 2010 The CYP2B6 G to T polymorphism at position 516 is shown to be associated with elevated plasma concentrations and an increase in neurotoxicity of EFV, while the wild-type genotype has been associated with sub-therapeutic concentrations of EFV, potentially leading to the development of viral resistance. efavirenz 145-148 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 4-10 20001610-6 2010 The CYP2B6 G to T polymorphism at position 516 is shown to be associated with elevated plasma concentrations and an increase in neurotoxicity of EFV, while the wild-type genotype has been associated with sub-therapeutic concentrations of EFV, potentially leading to the development of viral resistance. efavirenz 238-241 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 4-10 19487252-2 2009 The glucuronidation of EFV was screened with UGT1A and UGT2B enzymes expressed in a heterologous system, and UGT2B7 was shown to be the only reactive enzyme. efavirenz 23-26 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 45-50 19487252-1 2009 The non-nucleoside reverse transcriptase inhibitor efavirenz (EFV) is directly conjugated by the UDP-glucuronosyltransferase (UGT) pathway to form EFV-N-glucuronide (EFV-G), but the enzyme(s) involved has not yet been identified. efavirenz 51-60 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 97-124 19487252-1 2009 The non-nucleoside reverse transcriptase inhibitor efavirenz (EFV) is directly conjugated by the UDP-glucuronosyltransferase (UGT) pathway to form EFV-N-glucuronide (EFV-G), but the enzyme(s) involved has not yet been identified. efavirenz 51-60 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 126-129 19487252-1 2009 The non-nucleoside reverse transcriptase inhibitor efavirenz (EFV) is directly conjugated by the UDP-glucuronosyltransferase (UGT) pathway to form EFV-N-glucuronide (EFV-G), but the enzyme(s) involved has not yet been identified. efavirenz 62-65 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 97-124 19487252-1 2009 The non-nucleoside reverse transcriptase inhibitor efavirenz (EFV) is directly conjugated by the UDP-glucuronosyltransferase (UGT) pathway to form EFV-N-glucuronide (EFV-G), but the enzyme(s) involved has not yet been identified. efavirenz 62-65 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 126-129 19487252-2 2009 The glucuronidation of EFV was screened with UGT1A and UGT2B enzymes expressed in a heterologous system, and UGT2B7 was shown to be the only reactive enzyme. efavirenz 23-26 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 109-115 19487252-4 2009 Because 3"-azido-3"-deoxythymidine (AZT), one of the most current nucleotide reverse transcriptase inhibitors prescribed in combination with EFV, is also conjugated by UGT2B7, the potential metabolic interaction between EFV and AZT has been studied using human liver microsomes. efavirenz 141-144 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 168-174 19487252-4 2009 Because 3"-azido-3"-deoxythymidine (AZT), one of the most current nucleotide reverse transcriptase inhibitors prescribed in combination with EFV, is also conjugated by UGT2B7, the potential metabolic interaction between EFV and AZT has been studied using human liver microsomes. efavirenz 220-223 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 168-174 19531981-1 2009 Cytochrome P450 2B6 (CYP2B6) is the main metabolizing pathway for efavirenz (EFV), the prescription of which is associated with neurologic side effects. efavirenz 66-75 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-19 19531981-1 2009 Cytochrome P450 2B6 (CYP2B6) is the main metabolizing pathway for efavirenz (EFV), the prescription of which is associated with neurologic side effects. efavirenz 66-75 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 21-27 19531981-1 2009 Cytochrome P450 2B6 (CYP2B6) is the main metabolizing pathway for efavirenz (EFV), the prescription of which is associated with neurologic side effects. efavirenz 77-80 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-19 19531981-1 2009 Cytochrome P450 2B6 (CYP2B6) is the main metabolizing pathway for efavirenz (EFV), the prescription of which is associated with neurologic side effects. efavirenz 77-80 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 21-27 18990393-5 2009 RESULTS: LDLr-/- and hA-I transgenic mice treated with nevirapine and efavirenz had a significant increase in HDL-C level (up to 23% in hA-I transgenic) at 4 weeks. efavirenz 70-79 low density lipoprotein receptor Mus musculus 9-13 18990393-5 2009 RESULTS: LDLr-/- and hA-I transgenic mice treated with nevirapine and efavirenz had a significant increase in HDL-C level (up to 23% in hA-I transgenic) at 4 weeks. efavirenz 70-79 serine peptidase inhibitor, Kunitz type 1 Homo sapiens 21-25 18990393-5 2009 RESULTS: LDLr-/- and hA-I transgenic mice treated with nevirapine and efavirenz had a significant increase in HDL-C level (up to 23% in hA-I transgenic) at 4 weeks. efavirenz 70-79 serine peptidase inhibitor, Kunitz type 1 Homo sapiens 136-140 18990393-9 2009 Incubation of plasma from hA-I transgenic mice treated for 4 weeks with [(3)H]-cholesterol-labeled macrophages revealed increased cholesterol efflux to plasma from mice treated with efavirenz and nevirapine. efavirenz 182-191 serine peptidase inhibitor, Kunitz type 1 Homo sapiens 26-30 23675126-4 2009 Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6) and the metabolic effects of EFV have been described previously. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 44-63 23675126-4 2009 Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6) and the metabolic effects of EFV have been described previously. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 65-71 23675126-4 2009 Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6) and the metabolic effects of EFV have been described previously. efavirenz 11-14 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 44-63 23675126-4 2009 Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6) and the metabolic effects of EFV have been described previously. efavirenz 11-14 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 65-71 23675126-4 2009 Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6) and the metabolic effects of EFV have been described previously. efavirenz 102-105 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 65-71 19239339-1 2009 BACKGROUND: Polymorphisms in CYP2B6 affect the steady-state plasma concentrations of nevirapine and efavirenz. efavirenz 100-109 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 29-35 19286836-9 2009 The vitamin D(3) 25-hydroxylase activity in fibroblasts was suppressed by both calcitriol and efavirenz. efavirenz 94-103 cytochrome P450 family 27 subfamily A member 1 Homo sapiens 4-31 19371316-10 2009 Multiple linear regression analysis indicated that the CYP2B6 c.516G-->T polymorphism and CYP2A6 slow-metabolizing variants accounted for as much as 36 and 12% of the total variance in efavirenz concentrations, respectively. efavirenz 188-197 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 55-61 19371316-10 2009 Multiple linear regression analysis indicated that the CYP2B6 c.516G-->T polymorphism and CYP2A6 slow-metabolizing variants accounted for as much as 36 and 12% of the total variance in efavirenz concentrations, respectively. efavirenz 188-197 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 93-99 19238117-4 2009 We hypothesize that genetic variability in this gene may contribute to the particularly high, unexplained variability in EFV exposure in individuals with limited CYP2B6 function. efavirenz 121-124 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 162-168 19866531-4 2009 His EFV plasma concentrations were always above normal and he was homozygous for a deficient function-allele of CYP2D6; for this reason, his EFV dose was reduced to 400mg=d. efavirenz 4-7 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 112-118 19866531-4 2009 His EFV plasma concentrations were always above normal and he was homozygous for a deficient function-allele of CYP2D6; for this reason, his EFV dose was reduced to 400mg=d. efavirenz 141-144 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 112-118 19239339-10 2009 The composite CYP2B6 516/983 genotype was significantly associated with plasma drug exposure and clearance for efavirenz but not nevirapine. efavirenz 111-120 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 14-20 19018877-3 2009 METHODS: Insulin resistance was assessed at 96 weeks of treatment with nonnucleoside reverse transcriptase inhibitor (NNRTI)-based HAART (nevirapine or efavirenz with stavudine and lamivudine) among children in Chiang Mai, Thailand. efavirenz 152-161 insulin Homo sapiens 9-16 19234366-1 2009 Efavirenz, an important component of human immunodeficiency virus 1 (HIV-1) therapy, causes substantial drug interactions as an inducer of cytochromes and the transporter ABCB1. efavirenz 0-9 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 171-176 18784455-12 2008 As HIV-infected hemodialysis patients are disproportionately black, the increased frequency of the CYP2B6 516G>T polymorphism may lead to higher EFV levels. efavirenz 148-151 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 99-105 19474465-2 2009 Single nucleotide polymorphisms of the hepatic cytochrome P450 isoenzyme 2B6 (CYP2B6) gene have been associated with high interindividual variations in EFV plasma concentrations. efavirenz 152-155 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 47-76 19474465-2 2009 Single nucleotide polymorphisms of the hepatic cytochrome P450 isoenzyme 2B6 (CYP2B6) gene have been associated with high interindividual variations in EFV plasma concentrations. efavirenz 152-155 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 78-84 19474465-3 2009 Our objective was to determine the adequacy of EFV dosing and explore the influence of CYP2B6-516G>T polymorphisms on EFV plasma concentrations in Thai HIV-infected children. efavirenz 121-124 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 87-93 19474465-15 2009 CYP2B6-516G>T polymorphisms significantly affect the drug metabolism of EFV in children. efavirenz 75-78 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 18989234-0 2008 Efavirenz induces CYP2B6-mediated hydroxylation of bupropion in healthy subjects. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 18-24 18989234-9 2008 CONCLUSIONS: Our results confirm that efavirenz induces CYP2B6 enzyme activity in vivo, as demonstrated by an increase in bupropion hydroxylation after 2 weeks of efavirenz administration. efavirenz 38-47 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 56-62 18989234-9 2008 CONCLUSIONS: Our results confirm that efavirenz induces CYP2B6 enzyme activity in vivo, as demonstrated by an increase in bupropion hydroxylation after 2 weeks of efavirenz administration. efavirenz 163-172 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 56-62 19834271-10 2009 EFV, ritonavir (RTV) and nelfinavir (NFV) inhibited the expression of adiponectin mRNA in mature 3T3-L1 and to a greater extent in pre-mature 3T3-L1. efavirenz 0-3 adiponectin, C1Q and collagen domain containing Homo sapiens 70-81 18640157-5 2008 Treatment with efavirenz resulted in an increased MAPPIT signal, with an EC50 value of 64nM for the p66/p51 interaction, and allowed detection of the p51/p51 homodimerization, confirming the context-dependent asymmetric contribution of both subunits. efavirenz 15-24 DNA polymerase delta 3, accessory subunit Homo sapiens 100-103 18640157-5 2008 Treatment with efavirenz resulted in an increased MAPPIT signal, with an EC50 value of 64nM for the p66/p51 interaction, and allowed detection of the p51/p51 homodimerization, confirming the context-dependent asymmetric contribution of both subunits. efavirenz 15-24 tumor protein p63 Homo sapiens 104-107 18640157-5 2008 Treatment with efavirenz resulted in an increased MAPPIT signal, with an EC50 value of 64nM for the p66/p51 interaction, and allowed detection of the p51/p51 homodimerization, confirming the context-dependent asymmetric contribution of both subunits. efavirenz 15-24 tumor protein p63 Homo sapiens 150-153 18640157-5 2008 Treatment with efavirenz resulted in an increased MAPPIT signal, with an EC50 value of 64nM for the p66/p51 interaction, and allowed detection of the p51/p51 homodimerization, confirming the context-dependent asymmetric contribution of both subunits. efavirenz 15-24 tumor protein p63 Homo sapiens 150-153 18781911-5 2008 These individual differences may result in variable systemic exposure to drugs metabolized by CYP2B6, including the antineoplastics cyclophosphamide and ifosfamide, the antiretrovirals nevirapine and efavirenz, the anesthetics propofol and ketamine, the synthetic opioid methadone, and the anti-Parkinsonian selegiline. efavirenz 200-209 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 94-100 18620493-5 2008 Among the drugs tested, several inhibited PAF-induced platelet aggregation in a concentration-depended manner, with tenofovir, efavirenz, and ritonavir exhibiting the higher inhibitory effect. efavirenz 127-136 PCNA clamp associated factor Homo sapiens 42-45 18620493-8 2008 In addition, in naive patients treated with one of the most potent anti-PAF HAART regimens (efavirenz/emtricitabine/tenofovir-DF) for a period of 1 month, a significant reduction of the specific activity of PAF-CPT of washed human leukocytes of these patients was also observed, compared with its levels before the HAART treatment. efavirenz 92-101 PCNA clamp associated factor Homo sapiens 72-75 18620493-8 2008 In addition, in naive patients treated with one of the most potent anti-PAF HAART regimens (efavirenz/emtricitabine/tenofovir-DF) for a period of 1 month, a significant reduction of the specific activity of PAF-CPT of washed human leukocytes of these patients was also observed, compared with its levels before the HAART treatment. efavirenz 92-101 PCNA clamp associated factor Homo sapiens 207-210 18458892-3 2008 Efavirenz is an inducer of CYP3A, whereas the ritonavir-boosted regimens are net inhibitors of CYP3A. efavirenz 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-32 18458892-7 2008 CONCLUSION: Changes in plasma 4beta-hydroxycholesterol following the initiation of efavirenz- or atazanavir/ritonavir-based antiretroviral therapy reflected the respective net increase and decrease of CYP3A activity of these regimens. efavirenz 83-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 201-206 18667933-6 2008 Most EFV patients (92%) were already on EFV before starting IFN (mean 26 months). efavirenz 5-8 interferon alpha 1 Homo sapiens 60-63 18728241-1 2008 The goal of this study was to determine the effect of CYP2B6 genetic variation on the steady-state pharmacokinetics of efavirenz (600 mg/d) in TB/HIV co-infected patients receiving concomitant rifampin, a potent CYP inducer. efavirenz 119-128 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 54-60 18728241-1 2008 The goal of this study was to determine the effect of CYP2B6 genetic variation on the steady-state pharmacokinetics of efavirenz (600 mg/d) in TB/HIV co-infected patients receiving concomitant rifampin, a potent CYP inducer. efavirenz 119-128 peptidylprolyl isomerase G Homo sapiens 54-57 18351578-7 2008 Indeed, renal carcinoma cells exposed to efavirenz induced a CD8(+)CCR7-CD45RA(-) effector memory T-cell phenotype, whereas untreated RCC cells induced a CD8(+)CCR7(+)CD45RA(-) central memory T-cell phenotype. efavirenz 41-50 CD8a molecule Homo sapiens 61-64 18351578-7 2008 Indeed, renal carcinoma cells exposed to efavirenz induced a CD8(+)CCR7-CD45RA(-) effector memory T-cell phenotype, whereas untreated RCC cells induced a CD8(+)CCR7(+)CD45RA(-) central memory T-cell phenotype. efavirenz 41-50 CD8a molecule Homo sapiens 154-157 18332078-8 2008 CYP3A4 and CYP2B6 induction in Fa2N-4 cells were also low for phenytoin, phenobarbital, and efavirenz, which are dual activators of PXR/CAR. efavirenz 92-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 19338072-12 2008 In summary, TDF is a widely used drug in clinical practice due to its excellent combination of effectiveness, durability and tolerability, in addition to its ease of administration in a single daily dose, whether in its individual formation (Viread), or associated with FTC (Truvada), or with FTC and efavirenz (Atripla). efavirenz 301-310 sex determining region Y Homo sapiens 12-15 18332078-8 2008 CYP3A4 and CYP2B6 induction in Fa2N-4 cells were also low for phenytoin, phenobarbital, and efavirenz, which are dual activators of PXR/CAR. efavirenz 92-101 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 11-17 18332078-8 2008 CYP3A4 and CYP2B6 induction in Fa2N-4 cells were also low for phenytoin, phenobarbital, and efavirenz, which are dual activators of PXR/CAR. efavirenz 92-101 nuclear receptor subfamily 1 group I member 2 Homo sapiens 132-135 18332078-8 2008 CYP3A4 and CYP2B6 induction in Fa2N-4 cells were also low for phenytoin, phenobarbital, and efavirenz, which are dual activators of PXR/CAR. efavirenz 92-101 nuclear receptor subfamily 1 group I member 3 Homo sapiens 136-139 18057928-9 2008 Pharmacokinetic parameter estimates indicate that a dose reduction to 400 mg efavirenz per day is possible in patients homozygous for the CYP2B6*6 genotype without compromising therapeutic efficacy. efavirenz 77-86 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 138-144 18333864-28 2008 CONCLUSION: As expected with a CYP3A4 substrate, maraviroc exposure (C(max) and AUC(12)) was significantly reduced by the known CYP3A4 inducers, rifampicin and EFV, by approximately 70% and 50%, respectively. efavirenz 160-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 18333864-28 2008 CONCLUSION: As expected with a CYP3A4 substrate, maraviroc exposure (C(max) and AUC(12)) was significantly reduced by the known CYP3A4 inducers, rifampicin and EFV, by approximately 70% and 50%, respectively. efavirenz 160-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-134 17918089-8 2007 All EFV-treated CYP2B6 *6/*6 and *6/*26 carriers had extremely high plasma EFV concentrations (>6000 ng/mL) while receiving the standard dosage. efavirenz 4-7 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 16-22 18419537-0 2008 Efavirenz-based regimens in treatment-naive patients with a range of pretreatment HIV-1 RNA levels and CD4 cell counts. efavirenz 0-9 CD4 molecule Homo sapiens 103-106 18171905-1 2008 CYP2B6 is a polymorphic human drug metabolizing cytochrome P450 with clinical relevance for several drug substrates including cyclophosphamide, bupropion, and efavirenz. efavirenz 159-168 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 18025525-8 2008 The 200 mg bid voriconazole increased the steady-state mean AUC0-24 and Cmax of efavirenz by 43% (90% CI, 36%-51%) and 37% (90% CI, 29%-46%), respectively. efavirenz 80-89 BH3 interacting domain death agonist Homo sapiens 11-14 18097230-6 2008 Median CD4 cell counts increased above respective baselines by 292 cells/mul (efavirenz, zidovudine, lamivudine and indinavir, zidovudine, lamivudine) and 300 cells/mul (efavirenz plus indinavir). efavirenz 78-87 CD4 molecule Homo sapiens 7-10 18097230-6 2008 Median CD4 cell counts increased above respective baselines by 292 cells/mul (efavirenz, zidovudine, lamivudine and indinavir, zidovudine, lamivudine) and 300 cells/mul (efavirenz plus indinavir). efavirenz 170-179 CD4 molecule Homo sapiens 7-10 18783297-9 2008 Using this equation, the ICCYP3A4 was calculated for seven inducers (bosentan, carbamazepine, efavirenz, phenytoin, pioglitazone, rifampicin [rifampin], and St John"s wort [hypericum]) on the basis of the reduction in the AUC of a coadministered standard substrate of CYP3A4, such as simvastatin, in ten DDI studies. efavirenz 94-103 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-33 17918089-1 2007 BACKGROUND: Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6), and high plasma concentrations of the drug are associated with a G-->T polymorphism at position 516 (516G-->T) of CYP2B6 and frequent central nervous system (CNS)-related side effects. efavirenz 12-21 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 56-75 17918089-1 2007 BACKGROUND: Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6), and high plasma concentrations of the drug are associated with a G-->T polymorphism at position 516 (516G-->T) of CYP2B6 and frequent central nervous system (CNS)-related side effects. efavirenz 12-21 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 77-83 17918089-1 2007 BACKGROUND: Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6), and high plasma concentrations of the drug are associated with a G-->T polymorphism at position 516 (516G-->T) of CYP2B6 and frequent central nervous system (CNS)-related side effects. efavirenz 12-21 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 206-212 17918089-1 2007 BACKGROUND: Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6), and high plasma concentrations of the drug are associated with a G-->T polymorphism at position 516 (516G-->T) of CYP2B6 and frequent central nervous system (CNS)-related side effects. efavirenz 23-26 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 56-75 17918089-1 2007 BACKGROUND: Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6), and high plasma concentrations of the drug are associated with a G-->T polymorphism at position 516 (516G-->T) of CYP2B6 and frequent central nervous system (CNS)-related side effects. efavirenz 23-26 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 77-83 17918089-1 2007 BACKGROUND: Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6), and high plasma concentrations of the drug are associated with a G-->T polymorphism at position 516 (516G-->T) of CYP2B6 and frequent central nervous system (CNS)-related side effects. efavirenz 23-26 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 206-212 17918089-4 2007 EFV dose was reduced in CYP2B6 516G-->T carriers who had high plasma EFV concentrations while receiving the standard dosage (600 mg). efavirenz 0-3 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 24-30 17918089-8 2007 All EFV-treated CYP2B6 *6/*6 and *6/*26 carriers had extremely high plasma EFV concentrations (>6000 ng/mL) while receiving the standard dosage. efavirenz 75-78 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 16-22 17918089-10 2007 EFV-containing treatment was initiated at 400 mg in 4 CYP2B6 *6/*6 carriers and one *6/*26 carrier. efavirenz 0-3 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 54-60 17918089-13 2007 CONCLUSIONS: Genotype-based EFV dose reduction is feasible in CYP2B6 *6/*6 and *6/*26 carriers, which can reduce EFV-associated CNS symptoms. efavirenz 28-31 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 62-68 17918089-13 2007 CONCLUSIONS: Genotype-based EFV dose reduction is feasible in CYP2B6 *6/*6 and *6/*26 carriers, which can reduce EFV-associated CNS symptoms. efavirenz 113-116 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 62-68 17713424-9 2007 Some cohort studies and randomized clinical trials support the use of efavirenz-based antiretroviral therapy for the treatment of advanced HIV-1-infected patients; however, recent randomized controlled data suggest, in a moderately advanced HIV population, a better CD4 cell recovery for lopinavir-ritonavir than for efavirenz-treated patients, but a greater virological suppression in the efavirenz arm. efavirenz 70-79 CD4 molecule Homo sapiens 266-269 17235330-1 2007 To assess the association of CYP2B6 allelic diversity with efavirenz (EFV) pharmacokinetics, we performed extensive genotyping of 15 relevant single nucleotide polymorphism in 169 study participants, and full resequencing of CYP2B6 in individuals with abnormal EFV plasma levels. efavirenz 59-68 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 29-35 17667341-7 2007 Women had lower CD4 counts when starting EFV (median [interquartile range [IQR] = 126 [36, 220] cells/mm for women vs. 190 [109, 268] cells/mm for men; P = 0.0003). efavirenz 41-44 CD4 molecule Homo sapiens 16-19 17361129-6 2007 Considering drugs likely to be coadministered with AQ, the antiretroviral drugs efavirenz, saquinavir, lopinavir, and tipranavir were potent CYP2C8 inhibitors at clinically relevant concentrations. efavirenz 80-89 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 141-147 17686225-0 2007 Efavirenz-induced neurological symptoms in rare homozygote CYP2B6 *2/*2 (C64T). efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 59-65 17686225-3 2007 For example, CYP2B6 *6 (G516T and A785G) and *7 (G516T, A785G and C1459T) prolonged the EFV half-life despite discontinuation of EFV. efavirenz 88-91 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 13-19 17683706-0 2007 [Insulin resistance in HIV-infected patients receiving long-term therapy with efavirenz, lopinavir/ritonavir and atazanavir]. efavirenz 78-87 insulin Homo sapiens 1-8 17683706-7 2007 Insulin resistance was found in 5 (10.6%) patients, 4 among those receiving lopinavir/ritonavir, one among those treated with efavirenz and none among subjects receiving atazanavir (p = 0.065). efavirenz 126-135 insulin Homo sapiens 0-7 17653450-8 2007 The mean CD4 cell count increase after a 12-month period was also greater in the efavirenz group (195 x 10(6) cells/L) than in the nelfinavir group (119 x 10(6) cells/L; P = 0.002). efavirenz 81-90 CD4 molecule Homo sapiens 9-12 17356468-1 2007 BACKGROUND: The CYP2B6-G516T polymorphism has been shown to alter plasma efavirenz (EFV) concentrations in adults. efavirenz 84-87 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 16-22 17235330-1 2007 To assess the association of CYP2B6 allelic diversity with efavirenz (EFV) pharmacokinetics, we performed extensive genotyping of 15 relevant single nucleotide polymorphism in 169 study participants, and full resequencing of CYP2B6 in individuals with abnormal EFV plasma levels. efavirenz 70-73 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 29-35 17045554-7 2007 Several studies on efavirenz, a commonly used antiretroviral drug, have reported higher plasma exposure and early side effects with the homozygous variant of the hepatic cytochrome P450 enzyme CYP2B6 G516T polymorphism, which are more frequently found in African-American subjects. efavirenz 19-28 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 193-199 17082249-1 2007 BACKGROUND: CYP2B6 is a highly variable and polymorphic cytochrome P450 (CYP) enzyme involved in the biotransformation of an increasing number of drugs, including cyclophosphamide, bupropion, and the nonnucleosidic reverse transcriptase inhibitor efavirenz. efavirenz 247-256 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 12-18 17202245-6 2007 RESULTS: According to the IC(50) estimation, the rank order for BCRP inhibition was lopinavir > nelfinavir > delavirdine > efavirenz > saquinavir > atazanavir > amprenavir > abacavir. efavirenz 132-141 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 64-68 17082249-1 2007 BACKGROUND: CYP2B6 is a highly variable and polymorphic cytochrome P450 (CYP) enzyme involved in the biotransformation of an increasing number of drugs, including cyclophosphamide, bupropion, and the nonnucleosidic reverse transcriptase inhibitor efavirenz. efavirenz 247-256 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 56-71 17082249-1 2007 BACKGROUND: CYP2B6 is a highly variable and polymorphic cytochrome P450 (CYP) enzyme involved in the biotransformation of an increasing number of drugs, including cyclophosphamide, bupropion, and the nonnucleosidic reverse transcriptase inhibitor efavirenz. efavirenz 247-256 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 12-15 17162316-15 2006 CONCLUSION: In this pilot study of patients suppressed on abacavir/lamivudine/zidovudine bid plus EFV, 94% of participants switching to abacavir/lamivudine/zidovudine qd plus EFV maintained virologic suppression, compared to 89% of participants continuing abacavir/lamivudine/zidovudine bid plus EFV. efavirenz 98-101 BH3 interacting domain death agonist Homo sapiens 287-290 17539249-12 2007 Serum TC and LDL-c levels were also significantly higher in subjects taking efavirenz. efavirenz 76-85 component of oligomeric golgi complex 2 Homo sapiens 13-18 17101742-1 2006 Cytochrome P450 2B6 (CYP2B6) is involved in the metabolism of drugs such as bupropion, efavirenz, propofol, and selegiline, among others. efavirenz 87-96 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-19 17101742-1 2006 Cytochrome P450 2B6 (CYP2B6) is involved in the metabolism of drugs such as bupropion, efavirenz, propofol, and selegiline, among others. efavirenz 87-96 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 21-27 17047492-10 2006 Among 155 participants who received efavirenz without nelfinavir, virologic failure was associated with a two-locus interaction between ABCB1 2677G>T and CYP2B6 516G>T (65% accuracy, P<0.001). efavirenz 36-45 ATP binding cassette subfamily B member 1 Homo sapiens 136-141 17047492-10 2006 Among 155 participants who received efavirenz without nelfinavir, virologic failure was associated with a two-locus interaction between ABCB1 2677G>T and CYP2B6 516G>T (65% accuracy, P<0.001). efavirenz 36-45 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 157-163 17057609-7 2006 The TDF + FTC + EFV group demonstrated a significantly greater increase in CD4 count (270 vs. 237 cells/mm; P = 0.036). efavirenz 16-19 CD4 molecule Homo sapiens 75-78 17334006-8 2006 In the random effects model, there was an increase of 40.97 (p < 0.05) units of CD4 cell counts with an unit increase in time in the NVP arm as against a 44.75 (p < 0.05) units of increase in CD4 cell counts in the EFV group with a unit increase in time, which is significant for both groups. efavirenz 221-224 CD4 molecule Homo sapiens 83-86 17100373-14 2006 CONCLUSION: Initiation of EFV-based HAART regimen in HIV-infected patients at CD4 < 100 and > or = 100 cells/ mm3 gains similar immunological and virological response. efavirenz 26-29 CD4 molecule Homo sapiens 78-81 17009933-16 2006 Pivotal study 934 evidenced superior efficacy of the combination TDF/FTC/efavirenz (EFV) versus zidovudine/FTC/EFV. efavirenz 84-87 sex determining region Y Homo sapiens 65-68 16720753-8 2006 [(3)H]Taurocholate transport by recombinant NTCP and Ntcp was inhibited by ritonavir (IC(50) = 2.1 and 6.4 microM in human and rat, respectively), saquinavir (IC(50) = 6.7 and 20 microM, respectively), and efavirenz (IC(50) = 43 and 97 microM, respectively). efavirenz 206-215 solute carrier family 10 member 1 Rattus norvegicus 44-48 16720753-8 2006 [(3)H]Taurocholate transport by recombinant NTCP and Ntcp was inhibited by ritonavir (IC(50) = 2.1 and 6.4 microM in human and rat, respectively), saquinavir (IC(50) = 6.7 and 20 microM, respectively), and efavirenz (IC(50) = 43 and 97 microM, respectively). efavirenz 206-215 solute carrier family 10 member 1 Rattus norvegicus 53-57 16906281-10 2006 Urinary NO3 excretion was significantly lower in IDV-treated patients (809 +/- 181 microM NO3-/mg creatinine) than in efavirenz-treated patients (2247 +/- 648 microM NO3-/mg creatinine, P < 0.01). efavirenz 118-127 NBL1, DAN family BMP antagonist Homo sapiens 8-11 16779703-2 2006 METHODS: The uptake of EFV was measured in whole brains of rat and mdr1a-/- and mdr1a+/+ mice, and in GPNT cells (rat brain endothelial cell line) with and without P-gp inhibitors (PSC833, S9788, Quinidine). efavirenz 23-26 ATP binding cassette subfamily B member 1A Rattus norvegicus 67-72 16779703-2 2006 METHODS: The uptake of EFV was measured in whole brains of rat and mdr1a-/- and mdr1a+/+ mice, and in GPNT cells (rat brain endothelial cell line) with and without P-gp inhibitors (PSC833, S9788, Quinidine). efavirenz 23-26 ATP binding cassette subfamily B member 1A Rattus norvegicus 80-85 16779703-3 2006 The effect of a single dose or multiple doses of EFV on the P-gp functionality was evaluated in vivo and in vitro by measuring the brain and cell uptake of digoxin, completed by the analysis of the P-gp expression at the rat BBB after repeated administrations of EFV. efavirenz 49-52 phosphoglycolate phosphatase Rattus norvegicus 60-64 16779703-3 2006 The effect of a single dose or multiple doses of EFV on the P-gp functionality was evaluated in vivo and in vitro by measuring the brain and cell uptake of digoxin, completed by the analysis of the P-gp expression at the rat BBB after repeated administrations of EFV. efavirenz 49-52 phosphoglycolate phosphatase Rattus norvegicus 198-202 16267764-1 2005 BACKGROUND: Efavirenz and nelfinavir are metabolized by cytochrome P-450 (CYP) 2B6 and CYP2C19, respectively, with some involvement by CYP3A. efavirenz 12-21 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 56-82 16779703-10 2006 On the other hand, EFV did not induce P-gp, allowing to sustain the brain accumulation of associated P-gp substrates such as protease inhibitors. efavirenz 19-22 phosphoglycolate phosphatase Rattus norvegicus 101-105 16495778-1 2006 The non-nucleoside reverse transcriptase inhibitor efavirenz is mainly metabolised by the polymorphic cytochrome P450 enzyme CYP2B6. efavirenz 51-60 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 125-131 16495778-2 2006 Genomic DNA from four subjects in a group of 51 patients being treated with efavirenz and having surprisingly high plasma concentrations were screened by direct sequencing for mutations in the CYP2B6 gene. efavirenz 76-85 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 193-199 16495778-9 2006 The steady-state level of efavirenz was significantly higher in the five carriers of CYP2B6*16, being of African origin, compared to the other patients. efavirenz 26-35 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 85-91 16495778-10 2006 Higher efavirenz concentrations were also seen in carriers of 516G>T (CYP2B6*6 and CYP2B6*9). efavirenz 7-16 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 70-76 16495778-10 2006 Higher efavirenz concentrations were also seen in carriers of 516G>T (CYP2B6*6 and CYP2B6*9). efavirenz 7-16 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 83-89 16495778-11 2006 In conclusion, a novel CYP2B6*16 allele causing less expression of the corresponding enzyme was identified and found to influence the metabolism of efavirenz in vivo, a finding that is of potential impact for anti-HIV therapy in black populations. efavirenz 148-157 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 23-29 16392089-11 2006 CONCLUSIONS: The CYP2B6 position 516 TT genotype or a prolonged measured elimination half-life may predict increased risk of developing drug resistance among patients who discontinue efavirenz-containing regimens. efavirenz 183-192 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 17-23 16267764-1 2005 BACKGROUND: Efavirenz and nelfinavir are metabolized by cytochrome P-450 (CYP) 2B6 and CYP2C19, respectively, with some involvement by CYP3A. efavirenz 12-21 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 87-94 16267764-1 2005 BACKGROUND: Efavirenz and nelfinavir are metabolized by cytochrome P-450 (CYP) 2B6 and CYP2C19, respectively, with some involvement by CYP3A. efavirenz 12-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 135-140 16267764-9 2005 Plasma exposure to efavirenz and nelfinavir in each population was significantly associated with the polymorphisms CYP2B6 516G-->T and CYP2C19 681G-->A, respectively. efavirenz 19-28 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 115-121 16267764-9 2005 Plasma exposure to efavirenz and nelfinavir in each population was significantly associated with the polymorphisms CYP2B6 516G-->T and CYP2C19 681G-->A, respectively. efavirenz 19-28 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 138-145 16452064-3 2005 RESULTS: The two study groups were comparable, except for the lower baseline CD4+ count found in the EFV group. efavirenz 101-104 CD4 molecule Homo sapiens 77-80 16124934-4 2005 METHODS: (i) The effect of EFV on rat intestinal P-gp function was studied on everted gut sacs and in situ intestinal perfusion. efavirenz 27-30 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 49-53 15769884-1 2005 The polymorphic human cytochrome P450 (P450) 2B6 is primarily responsible for the metabolism of several clinically relevant drugs including bupropion, cyclophosphamide, propofol, and efavirenz. efavirenz 183-192 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 22-48 15980690-2 2005 EFV is a mixed inducer/inhibitor of cytochrome P450 (CYP) 3A4 isozyme and may interact with hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors that are primarily metabolized via CYP3A4. efavirenz 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-61 15980690-2 2005 EFV is a mixed inducer/inhibitor of cytochrome P450 (CYP) 3A4 isozyme and may interact with hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors that are primarily metabolized via CYP3A4. efavirenz 0-3 3-hydroxy-3-methylglutaryl-CoA reductase Homo sapiens 92-144 15980690-2 2005 EFV is a mixed inducer/inhibitor of cytochrome P450 (CYP) 3A4 isozyme and may interact with hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors that are primarily metabolized via CYP3A4. efavirenz 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 191-197 15657782-7 2005 CYP3A activity was lower in the efavirenz + ritonavir group (P = 0.01) and in the ritonavir group (P = 0.04) than in the nelfinavir group, although already strongly inhibited in the latter. efavirenz 32-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 15718846-0 2005 The efavirenz-induced increase in HDL-cholesterol is influenced by the multidrug resistance gene 1 C3435T polymorphism. efavirenz 4-13 ATP binding cassette subfamily B member 1 Homo sapiens 71-98 15718846-1 2005 Efavirenz treatment has been associated with increases in HDL-cholesterol concentrations, and the circulating levels of the drug have been related to the multidrug resistance gene 1 (MDR-1) C3435T polymorphism. efavirenz 0-9 ATP binding cassette subfamily B member 1 Homo sapiens 183-188 15657782-11 2005 The inhibition of CYP3A by ritonavir or nelfinavir offsets the inductive effects of efavirenz or nevirapine administered concomitantly. efavirenz 84-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-23 15657782-9 2005 Efavirenz strongly induces CYP3A activity, while ritonavir almost completely inhibits it. efavirenz 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-32 15864119-6 2005 RESULTS AND CONCLUSIONS: CYP2B6 516TT was associated with greater plasma and intracellular exposure to EFV, and greater plasma exposure to NVP. efavirenz 103-106 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 25-31 15563361-7 2004 During days 11-20 (period 2) efavirenz 600 mg q.d. efavirenz 29-38 period circadian regulator 2 Homo sapiens 19-27 14628297-13 2004 Our data could explain why the plasma concentration ratio of R/S methadone is variable and why drugs that induce CYP2B6 such as nevirapine and efavirenz also induce methadone metabolism, while the CYP3A4 inducer rifabutin has no effect on methadone pharmacokinetics. efavirenz 143-152 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 113-119 15194512-1 2004 Efavirenz (EFV) is metabolized by cytochrome P450 2B6 (CYP2B6) in the liver. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 34-53 15194512-1 2004 Efavirenz (EFV) is metabolized by cytochrome P450 2B6 (CYP2B6) in the liver. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 55-61 15194512-1 2004 Efavirenz (EFV) is metabolized by cytochrome P450 2B6 (CYP2B6) in the liver. efavirenz 11-14 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 34-53 15194512-1 2004 Efavirenz (EFV) is metabolized by cytochrome P450 2B6 (CYP2B6) in the liver. efavirenz 11-14 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 55-61 15864119-1 2005 BACKGROUND: Efavirenz (EFV) and nevirapine (NVP) are metabolized by cytochrome P450 2B6 (CYP2B6). efavirenz 23-26 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 68-87 15864119-1 2005 BACKGROUND: Efavirenz (EFV) and nevirapine (NVP) are metabolized by cytochrome P450 2B6 (CYP2B6). efavirenz 23-26 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 89-95 15496645-4 2004 Employing primary cultures of human hepatocytes, they compared the CYP3A4 inductive effects of efavirenz (1-10 microM) to rifampin (10 microM) and phenobarbital (2 mM). efavirenz 95-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 15496645-6 2004 The authors observed that efavirenz caused a concentration-dependent CYP3A4 induction and hPXR activation. efavirenz 26-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 15496645-6 2004 The authors observed that efavirenz caused a concentration-dependent CYP3A4 induction and hPXR activation. efavirenz 26-35 nuclear receptor subfamily 1 group I member 2 Homo sapiens 90-94 15496645-7 2004 Based on the CYP3A4 activity assay, the average magnitude of induction by efavirenz (5-10 microM) was approximately 3- to 4-fold. efavirenz 74-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-19 15167626-1 2004 Efavirenz is a drug subject to extensive metabolism, mainly by the cytochrome P-450 isoenzyme CYP2B6, known to exhibit extensive interindividual variability. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 94-100 15134483-8 2004 Nevirapine and efavirenz, the commonly prescribed non-nucleoside reverse transcriptase inhibitors, can readily enter the CSF, however, it remains to be seen if a transport system is involved in their distribution. efavirenz 15-24 colony stimulating factor 2 Homo sapiens 121-124 34873089-0 2022 Impact of CYP2B6 genotype, TB therapy and formulation on efavirenz pharmacokinetics in infants and children under 40 months of age. efavirenz 57-66 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 10-16 14711599-1 2003 BACKGROUND: In a retrospective study of HIV patients under antiretroviral therapy, we investigated the influence of the MDR1 genotype (C3435T) on plasma levels of lopinavir (LPV) and efavirenz (EFV). efavirenz 194-197 ATP binding cassette subfamily B member 1 Homo sapiens 120-124 12153332-6 2002 Upon review of available data, the antiretroviral agents zidovudine, stavudine, lamivudine, nevirapine, efavirenz and indinavir demonstrate consistent penetration into the CSF. efavirenz 104-113 colony stimulating factor 2 Homo sapiens 172-175 11590528-9 2001 There was a statistically significant reduction in relative CD8+CD38+ from 62.2+/-16.3% at time of switching to EFV to 55.1+/-15.0% at week 36. efavirenz 112-115 CD8a molecule Homo sapiens 60-63 11225565-2 2001 Delavirdine, nevirapine, and efavirenz produced negligible inhibition of phenacetin O-deethylation (CYP1A2) or dextromethorphan O-demethylation (CYP2D6). efavirenz 29-38 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 100-106 11225565-2 2001 Delavirdine, nevirapine, and efavirenz produced negligible inhibition of phenacetin O-deethylation (CYP1A2) or dextromethorphan O-demethylation (CYP2D6). efavirenz 29-38 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 145-151 10622035-3 1999 Efavirenz is a mild inducer of CYP 3A4. efavirenz 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-38 10082072-7 1999 Delaviridine is an inhibitor of CYP3A4, but nevirapine and efavirenz are inducers of CYP3A4. efavirenz 59-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-91 9878993-7 1998 Once-daily efavirenz in combination with zidovudine plus lamivudine or indinavir or nelfinavir increased CD4+ cell counts and reduced HIV RNA plasma levels to below quantifiable levels (< 400 copies/ml) in HIV-infected patients. efavirenz 11-20 CD4 molecule Homo sapiens 105-108 34945777-9 2021 On multivariate analysis, CYP2B6*6 and ABCB1c.3435 C > T genotypes and low pre-treatment low-density lipoprotein (LDL) were significantly associated with higher plasma efavirenz concentration regardless of treatment duration. efavirenz 168-177 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 26-32 34945777-9 2021 On multivariate analysis, CYP2B6*6 and ABCB1c.3435 C > T genotypes and low pre-treatment low-density lipoprotein (LDL) were significantly associated with higher plasma efavirenz concentration regardless of treatment duration. efavirenz 168-177 ATP binding cassette subfamily B member 1 Homo sapiens 39-44 34945777-11 2021 (4) Conclusion: Pre-treatment LDL cholesterol and CYP2B6*6 and ABCB1c.3435 C > T genotypes predict efavirenz plasma exposure among HIV-infected children, but treatment-duration-dependent changes in plasma efavirenz exposure due to auto-induction are not statistically significant. efavirenz 99-108 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 50-56 34945777-11 2021 (4) Conclusion: Pre-treatment LDL cholesterol and CYP2B6*6 and ABCB1c.3435 C > T genotypes predict efavirenz plasma exposure among HIV-infected children, but treatment-duration-dependent changes in plasma efavirenz exposure due to auto-induction are not statistically significant. efavirenz 99-108 ATP binding cassette subfamily B member 1 Homo sapiens 63-68 12705974-2 2003 Therefore, a highly specific method is presented, which is capable of quantifying the different proteinase inhibitors (amprenavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir) and non-nucleoside reverse transcriptase inhibitors (efavirenz, nelfinavir). efavirenz 241-250 endogenous retrovirus group K member 25 Homo sapiens 96-106 12151999-1 2002 OBJECTIVE: The capacity of the non-nucleoside reverse transcriptase inhibitor efavirenz to induce either liver CYP3A4 or intestinal CYP3A4, or both, as well as intestinal P-glycoprotein, was evaluated in healthy volunteers during and after a 10-day treatment course with two different daily doses. efavirenz 78-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 111-117 12151999-1 2002 OBJECTIVE: The capacity of the non-nucleoside reverse transcriptase inhibitor efavirenz to induce either liver CYP3A4 or intestinal CYP3A4, or both, as well as intestinal P-glycoprotein, was evaluated in healthy volunteers during and after a 10-day treatment course with two different daily doses. efavirenz 78-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 132-138 12405865-13 2002 Rifampicin (rifampin), phenobarbital, phenytoin, carbamazepine, nevirapine, and efavirenz decrease methadone blood concentrations, probably by induction of CYP3A4 activity, which can result in severe withdrawal symptoms. efavirenz 80-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 156-162 11159797-0 2001 Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion. efavirenz 11-20 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 45-51 11073762-6 2000 Six months after switching to efavirenz, there was a reduction in triglyceride levels (a decrease of 31%; P=.03) and fasting insulin resistance index (a decrease of 28%; P=.03), but total and high-density lipoprotein cholesterol and glucose did not change. efavirenz 30-39 insulin Homo sapiens 125-132 34768081-10 2021 These results imply that long-term EFV treatment causes synaptic dysfunction resulting in cognitive deficits, which might be induced by the enhanced pro-inflammatory cytokines IL-1beta and TNF-alpha via activating NF-kappaB pathway. efavirenz 35-38 interleukin 1 alpha Mus musculus 176-184 34768081-10 2021 These results imply that long-term EFV treatment causes synaptic dysfunction resulting in cognitive deficits, which might be induced by the enhanced pro-inflammatory cytokines IL-1beta and TNF-alpha via activating NF-kappaB pathway. efavirenz 35-38 tumor necrosis factor Mus musculus 189-198 34768081-10 2021 These results imply that long-term EFV treatment causes synaptic dysfunction resulting in cognitive deficits, which might be induced by the enhanced pro-inflammatory cytokines IL-1beta and TNF-alpha via activating NF-kappaB pathway. efavirenz 35-38 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 214-223 34474119-0 2021 Effect of Albumin and CYP2B6 Polymorphisms on Exposure of Efavirenz: A Population Pharmacokinetic Analysis in Chinese HIV-infected Adults. efavirenz 58-67 albumin Homo sapiens 10-17 34474119-0 2021 Effect of Albumin and CYP2B6 Polymorphisms on Exposure of Efavirenz: A Population Pharmacokinetic Analysis in Chinese HIV-infected Adults. efavirenz 58-67 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 22-28 34474119-9 2021 Efavirenz clearance was significantly influenced by CYP2B6 variants, including rs2099361, rs3745274, and rs2279343, along with albumin and weight. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 52-58 34474119-11 2021 Based on the CYP2B6 polymorphisms of patients, the recommended daily doses of efavirenz were 100 mg for CYP2B6 slow metabolizers, 400 or 600 mg for intermediate metabolizers, and 800 or 1000 mg for extensive metabolizers. efavirenz 78-87 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 13-19 34474119-11 2021 Based on the CYP2B6 polymorphisms of patients, the recommended daily doses of efavirenz were 100 mg for CYP2B6 slow metabolizers, 400 or 600 mg for intermediate metabolizers, and 800 or 1000 mg for extensive metabolizers. efavirenz 78-87 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 104-110 34474119-12 2021 CONCLUSIONS: Polymorphisms of CYP2B6, along with albumin and weight, resulted as the predictors of efavirenz pharmacokinetic variability, which could be used in prescribing optimal efavirenz doses. efavirenz 99-108 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 30-36 34474119-12 2021 CONCLUSIONS: Polymorphisms of CYP2B6, along with albumin and weight, resulted as the predictors of efavirenz pharmacokinetic variability, which could be used in prescribing optimal efavirenz doses. efavirenz 99-108 albumin Homo sapiens 49-56 34474119-12 2021 CONCLUSIONS: Polymorphisms of CYP2B6, along with albumin and weight, resulted as the predictors of efavirenz pharmacokinetic variability, which could be used in prescribing optimal efavirenz doses. efavirenz 181-190 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 30-36 34474119-12 2021 CONCLUSIONS: Polymorphisms of CYP2B6, along with albumin and weight, resulted as the predictors of efavirenz pharmacokinetic variability, which could be used in prescribing optimal efavirenz doses. efavirenz 181-190 albumin Homo sapiens 49-56 34235635-3 2021 Brain sterol flux is decreased in Cyp46a1-/- mice compared to wild-type mice and increased in 5XFAD mice (a model of Alzheimer"s disease) when they are treated with a small dose of efavirenz, a CYP46A1 activator. efavirenz 181-190 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 34-41 34882770-2 2021 Efavirenz is primarily metabolized by cytochrome P450 2B6 (CYP2B6), with CYP2A6 as an accessory pathway. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 38-57 34882770-2 2021 Efavirenz is primarily metabolized by cytochrome P450 2B6 (CYP2B6), with CYP2A6 as an accessory pathway. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 59-65 34882770-2 2021 Efavirenz is primarily metabolized by cytochrome P450 2B6 (CYP2B6), with CYP2A6 as an accessory pathway. efavirenz 0-9 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 73-79 34882770-6 2021 Genetic polymorphisms known to be associated with increased efavirenz plasma concentrations in CYP2B6 (rs3745274, rs28399499, rs4803419) and CYP2A6 (rs28399433) were selected and used to determine proportions of slow metabolizers. efavirenz 60-69 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 141-147 34127577-8 2021 CLHIV on efavirenz (EFV) had consistently lower TNF-alpha and IL-6 compared with those on ritonavir-boosted lopinavir (LPV/r) at all time points. efavirenz 9-18 tumor necrosis factor Homo sapiens 48-57 34127577-8 2021 CLHIV on efavirenz (EFV) had consistently lower TNF-alpha and IL-6 compared with those on ritonavir-boosted lopinavir (LPV/r) at all time points. efavirenz 9-18 interleukin 6 Homo sapiens 62-66 34127577-8 2021 CLHIV on efavirenz (EFV) had consistently lower TNF-alpha and IL-6 compared with those on ritonavir-boosted lopinavir (LPV/r) at all time points. efavirenz 20-23 tumor necrosis factor Homo sapiens 48-57 34127577-8 2021 CLHIV on efavirenz (EFV) had consistently lower TNF-alpha and IL-6 compared with those on ritonavir-boosted lopinavir (LPV/r) at all time points. efavirenz 20-23 interleukin 6 Homo sapiens 62-66 34415664-0 2021 Large variability in plasma efavirenz concentration in Papua New Guinea HIV/AIDS patients associated with high frequency of CYP2B6 516T allele. efavirenz 28-37 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 124-130 34495458-9 2021 Co-administration of moderate CYP3A4 inducers (efavirenz, carbamazepine, phenytoin) was predicted to result in an average decrease in entrectinib exposure between 45 and 79%, with corresponding average decreases for M5 of approximately 50%. efavirenz 47-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 34524919-2 2021 Our objective was to study the effects of switching from a protease inhibitor (PI) or efavirenz (EFV) to RAL on liver fat, body composition, and metabolic parameters among people living with HIV (PLWH) with high risk for nonalcoholic fatty liver disease (NAFLD). efavirenz 86-95 FAT atypical cadherin 1 Homo sapiens 118-121 34524919-2 2021 Our objective was to study the effects of switching from a protease inhibitor (PI) or efavirenz (EFV) to RAL on liver fat, body composition, and metabolic parameters among people living with HIV (PLWH) with high risk for nonalcoholic fatty liver disease (NAFLD). efavirenz 97-100 FAT atypical cadherin 1 Homo sapiens 118-121 34335044-0 2021 Influence of SULT1A1*2 Polymorphism on Plasma Efavirenz Concentration in Thai HIV-1 Patients. efavirenz 46-55 sulfotransferase family 1A member 1 Homo sapiens 13-20 34335044-5 2021 Results: Patients with three or more copies of SULT1A1 had significantly lower median plasma EFV concentrations than those carrying two copies at week 12 (p=0.046) and SULT1A1*2 (c.638G>A) carriers had significantly lower median plasma EFV concentrations compared to those not carrying the variant at week 24 (p=0.048). efavirenz 93-96 sulfotransferase family 1A member 1 Homo sapiens 47-54 34335044-5 2021 Results: Patients with three or more copies of SULT1A1 had significantly lower median plasma EFV concentrations than those carrying two copies at week 12 (p=0.046) and SULT1A1*2 (c.638G>A) carriers had significantly lower median plasma EFV concentrations compared to those not carrying the variant at week 24 (p=0.048). efavirenz 236-239 sulfotransferase family 1A member 1 Homo sapiens 47-54 34335044-5 2021 Results: Patients with three or more copies of SULT1A1 had significantly lower median plasma EFV concentrations than those carrying two copies at week 12 (p=0.046) and SULT1A1*2 (c.638G>A) carriers had significantly lower median plasma EFV concentrations compared to those not carrying the variant at week 24 (p=0.048). efavirenz 236-239 sulfotransferase family 1A member 1 Homo sapiens 168-175 34115651-9 2021 CYP2B6 516G > T, (P < 0.001) and CYP2B6 983T > C (P = 0.001) were each associated with hair efavirenz concentrations. efavirenz 92-101 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 34115651-9 2021 CYP2B6 516G > T, (P < 0.001) and CYP2B6 983T > C (P = 0.001) were each associated with hair efavirenz concentrations. efavirenz 92-101 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 33-39 34115651-13 2021 CONCLUSION: This study demonstrated approximately 3-fold and 2-fold higher efavirenz plasma and hair concentrations, respectively, among CYP2B6 516TT compared to 516GG. efavirenz 75-84 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 137-143 34235635-3 2021 Brain sterol flux is decreased in Cyp46a1-/- mice compared to wild-type mice and increased in 5XFAD mice (a model of Alzheimer"s disease) when they are treated with a small dose of efavirenz, a CYP46A1 activator. efavirenz 181-190 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 194-201 34939063-0 2021 Prolonged efavirenz exposure reduces peripheral oxytocin and vasopressin comparable to known drugs of addiction in male Sprague Dawley rats. efavirenz 10-19 arginine vasopressin Rattus norvegicus 61-72 34939063-4 2021 This study investigated whether sub-chronic EFV exposure, at a previously-determined rewarding dose, alters peripheral OT and VP levels versus that of a control, 9-tetrahydrocannabinol ( 9-THC), methamphetamine (MA) and cocaine. efavirenz 44-47 arginine vasopressin Rattus norvegicus 126-128 34100170-3 2021 To address this, we developed CD44 receptor-targeted, novel hyaluronic acid (HA)-coated nanostructured lipid carriers (NLCs) of efavirenz via washless layer-by-layer (LbL) assembly of HA and polyallylamine hydrochloride (PAH). efavirenz 128-137 CD44 molecule (Indian blood group) Homo sapiens 30-34 34093191-0 2021 Pharmacogenetic Associations Between Atazanavir/UGT1A1*28 and Efavirenz/rs3745274 (CYP2B6) Account for Specific Adverse Reactions in Chilean Patients Undergoing Antiretroviral Therapy. efavirenz 62-71 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 83-89 34093191-3 2021 UGT1A1*28 and CYP2B6 c.516G>T have been proposed to be related with higher toxicity by ATV and EFV, respectively. efavirenz 95-98 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 0-6 34093191-3 2021 UGT1A1*28 and CYP2B6 c.516G>T have been proposed to be related with higher toxicity by ATV and EFV, respectively. efavirenz 95-98 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 14-20 34280356-8 2021 Efavirenz use can negatively influence vitamin D levels and supplementation is necessary as a likely adjunct to improving CD4+ T cells, resulting in greater effectiveness of the treatment. efavirenz 0-9 CD4 molecule Homo sapiens 122-125 35489779-12 2022 The results suggest that the hydroxylated efavirenz metabolites may differ from efavirenz in how they interact with the CYP46A1 allosteric and active sites. efavirenz 42-51 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 120-127 35461087-0 2022 Exposure of human immune cells, to the antiretrovirals efavirenz and lopinavir, leads to lower glucose uptake and altered bioenergetic cell profiles through interactions with SLC2A1. efavirenz 55-64 solute carrier family 2 member 1 Homo sapiens 175-181 35461087-10 2022 Putative in silico analysis indicated the antiretrovirals, apart from efavirenz, associated with the binding site of highest binding affinity to SLC2A1, similar to that of glucose. efavirenz 70-79 solute carrier family 2 member 1 Homo sapiens 145-151 35428895-8 2022 Additionally, in the presence of strong or moderate CYP3A4 inducers, rifampicin and efavirenz, ipatasertib exposures were predicted to decrease by 86% and 74%, respectively. efavirenz 84-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 35149540-10 2022 Significance Statement The in vivo Kp,uu,fetal of nelfinavir (P-gp substrate), efavirenz (BCRP substrate), and imatinib (P-gp and BCRP substrate) was successfully estimated using m-f- PBPK modeling. efavirenz 79-88 BCR pseudogene 1 Homo sapiens 90-94 35512066-5 2022 One of the polymorphism in the CYP2B6 gene, 516G>T, particularly the 516T allele, is known to confer poor metabolism of EFV and NVP. efavirenz 120-123 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 31-37 35489779-0 2022 The hydroxylation position rather than chirality determines how efavirenz metabolites activate CYP46A1 in vitro. efavirenz 64-73 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 95-102 35489779-2 2022 In addition, (S)-EFV can interact off target with CYP46A1, the major cholesterol hydroxylating enzyme in the mammalian brain, and allosterically activate CYP46A1 at a small dose in mice and humans. efavirenz 13-20 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 50-57 35489779-12 2022 The results suggest that the hydroxylated efavirenz metabolites may differ from efavirenz in how they interact with the CYP46A1 allosteric and active sites. efavirenz 80-89 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 120-127 35489779-2 2022 In addition, (S)-EFV can interact off target with CYP46A1, the major cholesterol hydroxylating enzyme in the mammalian brain, and allosterically activate CYP46A1 at a small dose in mice and humans. efavirenz 13-20 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 154-161 35489779-9 2022 This difference in binding to the allosteric sites determined, in turn, how CYP46A1 activity was changed in the co-incubations with (S)-EFV and either its metabolite or L-Glu. efavirenz 132-139 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 76-83 35489779-10 2022 The results suggest EFV metabolites that could be more potent for CYP46A1 activation in vivo than (S)-EFV. efavirenz 98-105 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 66-73 35099526-0 2022 Corrigendum to: CYP2B6 Genotype and Weight Gain Differences Between Dolutegravir and Efavirenz. efavirenz 85-94 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 16-22 35489779-11 2022 Significance Statement We found that not only efavirenz but also all its hydroxylated metabolites allosterically activate CYP46A1 in vitro The enzyme activation depended on the hydroxylation position but not the metabolite spatial configuration, and involved either one or two allosteric sites - for efavirenz, L-Glu or both. efavirenz 46-55 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 122-129 35489779-11 2022 Significance Statement We found that not only efavirenz but also all its hydroxylated metabolites allosterically activate CYP46A1 in vitro The enzyme activation depended on the hydroxylation position but not the metabolite spatial configuration, and involved either one or two allosteric sites - for efavirenz, L-Glu or both. efavirenz 300-309 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 122-129 35090905-5 2022 Additionally, efavirenz and rilpivirine increased ROS generation, disrupted Deltapsim and upregulated the mRNA and protein expression of CHOP and GRP78, key markers of endoplasmic reticulum stress. efavirenz 14-23 DNA-damage inducible transcript 3 Rattus norvegicus 137-141 35090905-5 2022 Additionally, efavirenz and rilpivirine increased ROS generation, disrupted Deltapsim and upregulated the mRNA and protein expression of CHOP and GRP78, key markers of endoplasmic reticulum stress. efavirenz 14-23 heat shock protein family A (Hsp70) member 5 Rattus norvegicus 146-151 35107462-6 2022 Finally, the metabolite identification opportunities were also explored using efavirenz as an example drug with complex primary and secondary metabolism involving a combination of CYP, UGT and sulfotransferase enzymes. efavirenz 78-87 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 180-183 35107462-6 2022 Finally, the metabolite identification opportunities were also explored using efavirenz as an example drug with complex primary and secondary metabolism involving a combination of CYP, UGT and sulfotransferase enzymes. efavirenz 78-87 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 185-188 35235559-0 2022 Effects of cytochrome P450 2B6 and constitutive androstane receptor genetic variation on Efavirenz plasma concentrations among HIV patients in Kenya. efavirenz 89-98 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 11-30 35235559-0 2022 Effects of cytochrome P450 2B6 and constitutive androstane receptor genetic variation on Efavirenz plasma concentrations among HIV patients in Kenya. efavirenz 89-98 nuclear receptor subfamily 1 group I member 3 Homo sapiens 35-67 35235559-1 2022 The effects of genetic variation of cytochrome P450 2B6 (CYP2B6) and constitutive androstane receptor (CAR) on efavirenz (EFV) plasma concentration was evaluated among 312 HIV patients in Nairobi Kenya. efavirenz 122-125 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 36-55 35235559-1 2022 The effects of genetic variation of cytochrome P450 2B6 (CYP2B6) and constitutive androstane receptor (CAR) on efavirenz (EFV) plasma concentration was evaluated among 312 HIV patients in Nairobi Kenya. efavirenz 122-125 nuclear receptor subfamily 1 group I member 3 Homo sapiens 69-101 35194103-1 2022 Human CYP2B6 enzyme although constitutes relatively low proportion (1-4%) of hepatic cytochrome P450 content, it is the major catalyst of metabolism of several clinically important drugs (efavirenz, cyclophosphamide, bupropion, methadone). efavirenz 188-197 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 6-12 35194103-1 2022 Human CYP2B6 enzyme although constitutes relatively low proportion (1-4%) of hepatic cytochrome P450 content, it is the major catalyst of metabolism of several clinically important drugs (efavirenz, cyclophosphamide, bupropion, methadone). efavirenz 188-197 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 85-100 35052789-0 2022 Macrophages Modulate Hepatic Injury Involving NLRP3 Inflammasome: The Example of Efavirenz. efavirenz 81-90 NLR family pyrin domain containing 3 Homo sapiens 46-51 35115810-0 2022 The Cyp2b6 Gene Polymorphism and Phenotypic Correlation of Efavirenz-Based Combination Therapy Among the Niger Delta Ethnic Population: Implications in Modern Pharmacogenomics. efavirenz 59-68 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 4-10 35115810-12 2022 Genetic polymorphism of the CYP2B6 gene is prevalent among HIV/AIDs patients in the Niger Delta ethnic population on efavirenz-based HAART treatment, as the population having homozygous mutant gene or PM are >1% (6%). efavirenz 117-126 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 28-34 35052789-2 2022 Efavirenz, an anti-HIV drug, induces deleterious actions in hepatocytes that could underlie induction of the NLRP3 inflammasome, an important regulator of inflammatory responses during liver injury. efavirenz 0-9 NLR family pyrin domain containing 3 Homo sapiens 109-114 35052789-5 2022 Efavirenz triggered inflammation in hepatocytes, in a process that involved NF-kappaB and the NLRP3 inflammasome, and activated hepatic stellate cells (HSCs), thereby enhancing expression of inflammatory and fibrogenic markers. efavirenz 0-9 nuclear factor kappa B subunit 1 Homo sapiens 76-85 35052789-5 2022 Efavirenz triggered inflammation in hepatocytes, in a process that involved NF-kappaB and the NLRP3 inflammasome, and activated hepatic stellate cells (HSCs), thereby enhancing expression of inflammatory and fibrogenic markers. efavirenz 0-9 NLR family pyrin domain containing 3 Homo sapiens 94-99 35052789-8 2022 Efavirenz elicits a cell-specific activation of the NLRP3 inflammasome in hepatocytes and HSCs, but macrophages appear to counteract efavirenz-induced liver injury. efavirenz 0-9 NLR family pyrin domain containing 3 Homo sapiens 52-57 33421254-0 2021 A novel association of efavirenz induced severe cutaneous adverse reactions with HLA- DRB1*03:01: A case-control study from North-East India. efavirenz 23-32 major histocompatibility complex, class II, DR beta 1 Homo sapiens 81-90 33833550-0 2021 Erratum: Association of CYP2B6 Genetic Variation with Efavirenz and Nevirapine Drug Resistance in HIV-1 Patients from Botswana [Corrigendum]. efavirenz 54-63 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 24-30 33758532-0 2021 Association of CYP2B6 Genetic Variation with Efavirenz and Nevirapine Drug Resistance in HIV-1 Patients from Botswana. efavirenz 45-54 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 15-21 33758532-1 2021 Purpose: CYP2B6 liver enzyme metabolizes the two non-nucleoside reverse transcriptase inhibitors Efavirenz (EFV) and Nevirapine (NVP) used in the antiretroviral therapy (ART) regimens for HIV-infected individuals. efavirenz 97-106 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 9-15 33758532-1 2021 Purpose: CYP2B6 liver enzyme metabolizes the two non-nucleoside reverse transcriptase inhibitors Efavirenz (EFV) and Nevirapine (NVP) used in the antiretroviral therapy (ART) regimens for HIV-infected individuals. efavirenz 108-111 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 9-15 33336382-6 2021 In the clinical study, we confirmed a moderate induction of CYP2B6 (decrease in the efavirenz AUC by 79%) and 3A4 (decrease in the midazolam AUC by 68%) by metamizole. efavirenz 84-93 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 60-66 33872945-1 2021 Human hepatic cytochrome P450 2B6 (CYP2B6) expressed is responsible for the metabolism of many drugs, such as cyclophosphamide, ifosfamid, and efavirenz. efavirenz 143-152 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 14-33 33872945-1 2021 Human hepatic cytochrome P450 2B6 (CYP2B6) expressed is responsible for the metabolism of many drugs, such as cyclophosphamide, ifosfamid, and efavirenz. efavirenz 143-152 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 35-41 32667979-2 2021 In a Phase 1 dolutegravir-efavirenz interaction study, mean dolutegravir Cmin decreased by 60% and 85% among CYP2B6 normal and slow/intermediate metabolizers, respectively. efavirenz 26-35 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 109-115 32909316-6 2021 Isoniazid decreased efavirenz clearance by 7% in CYP2B6 normal metabolizers and 13% in slow and intermediate metabolizers. efavirenz 20-29 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 49-55 32813881-2 2021 In 2016, the label of LNG was updated based on a drug-drug interaction (DDI) study showing a significant decrease in LNG exposure when co-administered with efavirenz, a known CYP3A4 inducer. efavirenz 156-165 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 175-181 33421254-3 2021 To evaluate HLA class I and II allele frequencies in HIV patients on HAART who develop SCARs due to nevirapine (NVP] or efavirenz (EFZ] containing regime and compare this genotype composition with HAART tolerant patients and healthy organ donors. efavirenz 120-129 major histocompatibility complex, class II, DR beta 1 Homo sapiens 12-15 33599403-2 2021 Drugs metabolized mainly by CYP2B6 include artemisinin, bupropion, cyclophosphamide, efavirenz, ketamine, and methadone. efavirenz 85-94 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 28-34 33390085-7 2021 Drug resistance mutation M184V (ATG to GTA) (63.15%) associated with lamivudine and abacavir and K103N (AAG or AAA to AAU) (36.84%) associated with efavirenz and nevirapine were predominantly identified in first line ART failure patients. efavirenz 148-157 N-methylpurine DNA glycosylase Homo sapiens 104-107 33305262-0 2020 CYP46A1-dependent and independent effects of efavirenz treatment. efavirenz 45-54 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 0-7 33526292-0 2021 Erratum to: Non-nucleoside reverse transcriptase inhibitor efavirenz activates PXR to induce hypercholesterolemia and hepatic steatosis [J Hepatol (2019); 70 (5): 930-940]. efavirenz 59-68 nuclear receptor subfamily 1 group I member 2 Homo sapiens 79-82 31942947-9 2021 The differences in GMR (90%CI) of TFV AUC, C24, and EFV C24 at week 5 versus week 8 were 0.86 (0.80-0.93), p=0.002; 0.83 (0.75-0.93), p=0.006; and EFV C24 was 0.91 (0.85-0.97), p=0.02, respectively. efavirenz 52-55 colony stimulating factor 2 receptor subunit alpha Homo sapiens 19-22 31942947-9 2021 The differences in GMR (90%CI) of TFV AUC, C24, and EFV C24 at week 5 versus week 8 were 0.86 (0.80-0.93), p=0.002; 0.83 (0.75-0.93), p=0.006; and EFV C24 was 0.91 (0.85-0.97), p=0.02, respectively. efavirenz 147-150 colony stimulating factor 2 receptor subunit alpha Homo sapiens 19-22 32815870-6 2021 In multivariable analyses, NAT2 slow acetylators had greater week 4 plasma concentrations of rifapentine (P = 2.6 x 10) and 25-desacetyl rifapentine (P = 7.0 x 10) among all participants, and in efavirenz and nevirapine subgroups. efavirenz 195-204 N-acetyltransferase 2 Homo sapiens 27-31 32815870-7 2021 NAT2 slow acetylators also had greater plasma efavirenz and nevirapine concentration increases from baseline to week 4, and greater decreases from baseline in clearance. efavirenz 46-55 N-acetyltransferase 2 Homo sapiens 0-4 32815870-8 2021 CYP2B6 poor metabolizers had greater efavirenz concentrations at all weeks and greater nevirapine concentrations at baseline. efavirenz 37-46 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 32815870-10 2021 CONCLUSIONS: Among HIV-positive individuals receiving efavirenz or nevirapine, and who then initiated rifapentine plus isoniazid in A5279, NAT2 slow acetylators had greater rifapentine and 25-desacetyl rifapentine concentrations, and greater increases from baseline in plasma efavirenz and nevirapine concentrations. efavirenz 54-63 N-acetyltransferase 2 Homo sapiens 139-143 32815870-10 2021 CONCLUSIONS: Among HIV-positive individuals receiving efavirenz or nevirapine, and who then initiated rifapentine plus isoniazid in A5279, NAT2 slow acetylators had greater rifapentine and 25-desacetyl rifapentine concentrations, and greater increases from baseline in plasma efavirenz and nevirapine concentrations. efavirenz 276-285 N-acetyltransferase 2 Homo sapiens 139-143 33452585-10 2021 Amlodipine apparent clearance was influenced by both CYP3A4 inhibitors and efavirenz (CYP3A4 inducer). efavirenz 75-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-92 33217171-7 2021 The combined LNG-EE PBPK model was verified regarding CYP3A4-mediated interaction by comparing to published clinical DDI study data with carbamazepine, rifampicin, and efavirenz (CYP3A4 inducers). efavirenz 168-177 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 179-185 33355828-1 2020 Background: Africans exhibit great diversity in cytochrome P450 2B6 isoenzyme (CYP2B6), the major enzyme in efavirenz metabolism. efavirenz 108-117 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 48-77 33355828-1 2020 Background: Africans exhibit great diversity in cytochrome P450 2B6 isoenzyme (CYP2B6), the major enzyme in efavirenz metabolism. efavirenz 108-117 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 79-85 33355828-2 2020 Aim: We examined the frequency of two functional single nucleotide polymorphisms (SNPs) of the CYP2B6 pharmacogene in HIV-infected Nigerians on efavirenz-based antiretroviral therapy. efavirenz 144-153 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 95-101 33305262-5 2020 Previously we found that treatment of 5XFAD mice, an Alzheimer"s disease model, with a small dose of anti-HIV drug efavirenz allosterically activated cytochrome P450 46A1 in the brain and mitigated several disease manifestations. efavirenz 115-124 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 150-170 33305262-7 2020 Efavirenz-treated versus control Cyp46a1-/- 5XFAD and 5XFAD mice were compared for the brain sterol and steroid hormone content, amyloid beta burden, protein and mRNA expression as well as synaptic ultrastructure. efavirenz 0-9 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 33-40 33305262-8 2020 We found that the cytochrome P450 46A1-dependent efavirenz effects included changes in the levels of brain sterols, steroid hormones, and such proteins as glial fibrillary acidic protein, Iba1, Munc13-1, post-synaptic density-95, gephyrin, synaptophysin and synapsin-1. efavirenz 49-58 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 18-38 33305262-8 2020 We found that the cytochrome P450 46A1-dependent efavirenz effects included changes in the levels of brain sterols, steroid hormones, and such proteins as glial fibrillary acidic protein, Iba1, Munc13-1, post-synaptic density-95, gephyrin, synaptophysin and synapsin-1. efavirenz 49-58 glial fibrillary acidic protein Mus musculus 155-186 33305262-8 2020 We found that the cytochrome P450 46A1-dependent efavirenz effects included changes in the levels of brain sterols, steroid hormones, and such proteins as glial fibrillary acidic protein, Iba1, Munc13-1, post-synaptic density-95, gephyrin, synaptophysin and synapsin-1. efavirenz 49-58 induction of brown adipocytes 1 Mus musculus 188-192 33305262-8 2020 We found that the cytochrome P450 46A1-dependent efavirenz effects included changes in the levels of brain sterols, steroid hormones, and such proteins as glial fibrillary acidic protein, Iba1, Munc13-1, post-synaptic density-95, gephyrin, synaptophysin and synapsin-1. efavirenz 49-58 unc-13 homolog A Mus musculus 194-202 33305262-8 2020 We found that the cytochrome P450 46A1-dependent efavirenz effects included changes in the levels of brain sterols, steroid hormones, and such proteins as glial fibrillary acidic protein, Iba1, Munc13-1, post-synaptic density-95, gephyrin, synaptophysin and synapsin-1. efavirenz 49-58 gephyrin Mus musculus 230-238 33305262-8 2020 We found that the cytochrome P450 46A1-dependent efavirenz effects included changes in the levels of brain sterols, steroid hormones, and such proteins as glial fibrillary acidic protein, Iba1, Munc13-1, post-synaptic density-95, gephyrin, synaptophysin and synapsin-1. efavirenz 49-58 synaptophysin Mus musculus 240-253 33305262-8 2020 We found that the cytochrome P450 46A1-dependent efavirenz effects included changes in the levels of brain sterols, steroid hormones, and such proteins as glial fibrillary acidic protein, Iba1, Munc13-1, post-synaptic density-95, gephyrin, synaptophysin and synapsin-1. efavirenz 49-58 synapsin I Mus musculus 258-268 33305262-15 2020 This study further confirmed that cytochrome P450 46A1 is a key enzyme for cholesterol homeostasis in the brain and that the therapeutic efavirenz effects on 5XFAD mice are likely realized via cytochrome P450 46A1 activation. efavirenz 137-146 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 34-54 33305262-15 2020 This study further confirmed that cytochrome P450 46A1 is a key enzyme for cholesterol homeostasis in the brain and that the therapeutic efavirenz effects on 5XFAD mice are likely realized via cytochrome P450 46A1 activation. efavirenz 137-146 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 193-213 32960272-0 2021 CYP2B6 Genotype and Weight Gain Differences Between Dolutegravir and Efavirenz. efavirenz 69-78 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 33155233-10 2020 Efavirenz acts as a serotonin 5-HT2A receptor antagonist, a serotonin-dopamine reuptake inhibitor, an inhibitor of monoamine oxidase (MAO) and a vesicular monoamine transporter 2 (VMAT2) inhibitor, which are mechanisms common with many psychotropic drugs. efavirenz 0-9 5-hydroxytryptamine receptor 2A Homo sapiens 20-45 33155233-10 2020 Efavirenz acts as a serotonin 5-HT2A receptor antagonist, a serotonin-dopamine reuptake inhibitor, an inhibitor of monoamine oxidase (MAO) and a vesicular monoamine transporter 2 (VMAT2) inhibitor, which are mechanisms common with many psychotropic drugs. efavirenz 0-9 solute carrier family 18 member A2 Homo sapiens 180-185 33116922-12 2020 Health-care providers should give attention to patients on efavirenz therapy to monitor for CNS adverse events, especially for patients who have low CD4 count, advanced disease, comorbidities, low income and are older in age. efavirenz 59-68 CD4 molecule Homo sapiens 149-152 32960272-2 2021 Loss-of-function polymorphisms in CYP2B6 result in higher efavirenz concentrations, which we hypothesized would impair weight gain among people living with human immunodeficiency virus (HIV; PLWH) starting efavirenz-based antiretroviral therapy (ART). efavirenz 58-67 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 34-40 32960272-2 2021 Loss-of-function polymorphisms in CYP2B6 result in higher efavirenz concentrations, which we hypothesized would impair weight gain among people living with human immunodeficiency virus (HIV; PLWH) starting efavirenz-based antiretroviral therapy (ART). efavirenz 206-215 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 34-40 32960272-11 2021 CONCLUSIONS: CYP2B6 metaboliser genotype was associated with weight gain in PLWH starting efavirenz-based ART. efavirenz 90-99 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 13-19 32590137-8 2020 Osteocalcin (ng/mL) was higher in the LPV/r than efavirenz group both at 8 weeks (88.6 vs. 67.3, p = 0.001) and 2 years (67.6 vs. 49.8, p = 0.001). efavirenz 49-58 bone gamma-carboxyglutamate protein Homo sapiens 0-11 32451120-2 2020 Polymorphism of CYP2B6 516G > T has been found to predominantly contribute to efavirenz variability. efavirenz 78-87 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 16-22 32905132-5 2020 Notable examples include oseltamivir which may act as MAO inhibitor and efavirenz, which has an affinity for serotonin 5-HT2 and GABA-A receptors, the serotonin transporter, the MAO enzyme, and the vesicular monoamine transporter, with subjective effects which may be similar to those of the psychedelic hallucinogen lysergic acid diethylamide (LSD). efavirenz 72-81 solute carrier family 6 member 4 Homo sapiens 151-172 32702281-5 2020 Compared to regimens containing lopinavir, we found that atazanavir-, efavirenz-, and raltegravir-based regimens were superior in achieving both outcomes after adjustment for age, social vulnerability index, time under ART, baseline CD4+ cell count, and baseline HIV VL. efavirenz 70-79 CD4 molecule Homo sapiens 233-236 32310900-8 2020 In adjusted models, children exposed to efavirenz at any time during pregnancy had higher risk of neurologic case status (aRR = 1.53, 95% CI 0.94--2.51). efavirenz 40-49 arrestin beta 1 Homo sapiens 122-129 32310900-9 2020 This association was stronger when comparing efavirenz exposure at conception to no exposure during pregnancy (aRR = 1.92, 95% CI 1.09--3.36) and considering follow-up and case diagnosis only through age 2 (aRR = 2.14, 95% CI 1.11--4.12). efavirenz 45-54 arrestin beta 1 Homo sapiens 111-118 32310900-9 2020 This association was stronger when comparing efavirenz exposure at conception to no exposure during pregnancy (aRR = 1.92, 95% CI 1.09--3.36) and considering follow-up and case diagnosis only through age 2 (aRR = 2.14, 95% CI 1.11--4.12). efavirenz 45-54 arrestin beta 2 Homo sapiens 207-214 32829410-5 2021 Associations were characterized with CYP2B6 and UGT1A1 genotypes that affect efavirenz and INSTI metabolism, respectively. efavirenz 77-86 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 37-43 32829410-5 2021 Associations were characterized with CYP2B6 and UGT1A1 genotypes that affect efavirenz and INSTI metabolism, respectively. efavirenz 77-86 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 48-54 32829410-10 2021 In the clinical trials cohort (N=462), CYP2B6 slow metabolizers had lesser weight gain at week 48 among participants receiving efavirenz with tenofovir disoproxil fumarate (p=0.001) but not those receiving efavirenz with abacavir (p=0.65). efavirenz 127-136 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 39-45 32829410-10 2021 In the clinical trials cohort (N=462), CYP2B6 slow metabolizers had lesser weight gain at week 48 among participants receiving efavirenz with tenofovir disoproxil fumarate (p=0.001) but not those receiving efavirenz with abacavir (p=0.65). efavirenz 206-215 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 39-45 32829410-12 2021 CONCLUSIONS: Among patients who switched from efavirenz- to INSTI-based therapy, CYP2B6 genotype was associated with weight gain, possibly reflecting withdrawal of the inhibitory effect of higher efavirenz concentrations on weight gain. efavirenz 46-55 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 81-87 32829410-12 2021 CONCLUSIONS: Among patients who switched from efavirenz- to INSTI-based therapy, CYP2B6 genotype was associated with weight gain, possibly reflecting withdrawal of the inhibitory effect of higher efavirenz concentrations on weight gain. efavirenz 196-205 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 81-87 32377759-0 2020 Prediction of the exposure to a 400-mg daily dose of efavirenz in pregnancy: is this dose adequate in extensive metabolisers of CYP2B6? efavirenz 53-62 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 128-134 32838647-5 2020 CYP2B6 516G>T, 785A>G, 18492C>T and ABCB1 3435C>T T/C were associated with higher efavirenz plasma levels in the standard but not the lower-dose group. efavirenz 82-91 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 32838647-5 2020 CYP2B6 516G>T, 785A>G, 18492C>T and ABCB1 3435C>T T/C were associated with higher efavirenz plasma levels in the standard but not the lower-dose group. efavirenz 82-91 ATP binding cassette subfamily B member 1 Homo sapiens 36-41 32451120-4 2020 This study aimed to develop a population model of the pharmacokinetic properties of efavirenz, and to investigate the impact of patients" characteristics and CYP2B6 516G > T polymorphism on the pharmacokinetic properties of efavirenz. efavirenz 224-233 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 158-164 32451120-7 2020 A 1-compartment model with first-order absorption and elimination was used for describing the pharmacokinetic properties of efavirenz. efavirenz 124-133 BCL2 related protein A1 Homo sapiens 0-3 32451120-9 2020 The efavirenz oral clearance were 11.9, 8.0, and 2.8 L/h in patients weighing 57 kg and having the CYP2B6 516 GG, 516 GT, and 516 TT genotypes, respectively. efavirenz 4-13 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 99-105 32451120-12 2020 IMPLICATION: The results from this study provide a rationale for efavirenz dose adjustment based on CYP2B6 516G > T polymorphism in Thai HIV-infected patients, which could help to improve treatment outcomes in this population. efavirenz 65-74 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 100-106 31617715-0 2020 In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. efavirenz 57-66 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 23-43 31617715-0 2020 In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds. efavirenz 57-66 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 45-52 31617715-2 2020 Currently CYP46A1 is being evaluated in a clinical trial for activation by small doses of the anti-HIV drug efavirenz. efavirenz 108-117 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 10-17 31617715-3 2020 Eight efavirenz-related compounds were investigated for CYP46A1 activation in vitro, induction of a CYP46A1 spectral response and spectral Kd values, interaction with the P450 allosteric sites, and a model of binding to the enzyme active site. efavirenz 6-15 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 100-107 31617715-4 2020 We gained insight into structure-activity relationships of efavirenz for CYP46A1 activation and found that the investigated efavirenz primary metabolites are stronger and better activators of CYP46A1 than efavirenz. efavirenz 59-68 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 73-80 31617715-4 2020 We gained insight into structure-activity relationships of efavirenz for CYP46A1 activation and found that the investigated efavirenz primary metabolites are stronger and better activators of CYP46A1 than efavirenz. efavirenz 59-68 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 192-199 31617715-4 2020 We gained insight into structure-activity relationships of efavirenz for CYP46A1 activation and found that the investigated efavirenz primary metabolites are stronger and better activators of CYP46A1 than efavirenz. efavirenz 124-133 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 73-80 31617715-4 2020 We gained insight into structure-activity relationships of efavirenz for CYP46A1 activation and found that the investigated efavirenz primary metabolites are stronger and better activators of CYP46A1 than efavirenz. efavirenz 124-133 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 192-199 31617715-4 2020 We gained insight into structure-activity relationships of efavirenz for CYP46A1 activation and found that the investigated efavirenz primary metabolites are stronger and better activators of CYP46A1 than efavirenz. efavirenz 124-133 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 73-80 31617715-4 2020 We gained insight into structure-activity relationships of efavirenz for CYP46A1 activation and found that the investigated efavirenz primary metabolites are stronger and better activators of CYP46A1 than efavirenz. efavirenz 124-133 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 192-199 31617715-6 2020 The results suggest structural modifications of efavirenz to further increase CYP46A1 activation without inhibition at high compound concentrations. efavirenz 48-57 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 78-85 31617715-7 2020 It is possible that not only efavirenz but its metabolites activate CYP46A1 in vivo. efavirenz 29-38 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 68-75 31845585-3 2020 The anti-HIV drug efavirenz activates CYP46A1 at low drug levels while inhibiting the enzyme activity at the high dose used in clinical practice. efavirenz 18-27 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 38-45 31845585-4 2020 Synthetic analogs and hydroxylated metabolites of efavirenz enhance CYP46A1 activity, with reduced unwanted enzyme inhibition at higher concentrations. efavirenz 50-59 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 68-75 31845585-5 2020 These observations provide a platform for structural modifications of efavirenz to modulate CYP46A1 activity as a therapeutic target of brain disorders such as Alzheimer"s disease, for which currently no treatment is available. efavirenz 70-79 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 92-99 31324697-0 2019 Efavirenz Metabolism: Influence of Polymorphic CYP2B6 Variants and Stereochemistry. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 47-53 31628422-0 2020 Influence of CYP2B6 activity score on the pharmacokinetics and safety of single dose efavirenz in healthy volunteers. efavirenz 85-94 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 13-19 31628422-2 2020 Cytochrome P450 (CYP) CYP2B6 G516T (rs3745274) is a well-known predictor of efavirenz disposition. efavirenz 76-85 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 0-15 31628422-2 2020 Cytochrome P450 (CYP) CYP2B6 G516T (rs3745274) is a well-known predictor of efavirenz disposition. efavirenz 76-85 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 17-20 31628422-2 2020 Cytochrome P450 (CYP) CYP2B6 G516T (rs3745274) is a well-known predictor of efavirenz disposition. efavirenz 76-85 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 22-28 31628422-5 2020 In this study, we evaluated the influence of 11 single-nucleotide polymorphisms (SNPs) in CYP2B6, CYP2A6, CYP3A and ABCB1 (ATP-binding cassette sub-family B member 1) on the pharmacokinetics and safety of efavirenz after single oral dose administration to 47 healthy volunteers. efavirenz 205-214 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 90-96 31628422-5 2020 In this study, we evaluated the influence of 11 single-nucleotide polymorphisms (SNPs) in CYP2B6, CYP2A6, CYP3A and ABCB1 (ATP-binding cassette sub-family B member 1) on the pharmacokinetics and safety of efavirenz after single oral dose administration to 47 healthy volunteers. efavirenz 205-214 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-111 31628422-5 2020 In this study, we evaluated the influence of 11 single-nucleotide polymorphisms (SNPs) in CYP2B6, CYP2A6, CYP3A and ABCB1 (ATP-binding cassette sub-family B member 1) on the pharmacokinetics and safety of efavirenz after single oral dose administration to 47 healthy volunteers. efavirenz 205-214 ATP binding cassette subfamily B member 1 Homo sapiens 116-121 31628422-5 2020 In this study, we evaluated the influence of 11 single-nucleotide polymorphisms (SNPs) in CYP2B6, CYP2A6, CYP3A and ABCB1 (ATP-binding cassette sub-family B member 1) on the pharmacokinetics and safety of efavirenz after single oral dose administration to 47 healthy volunteers. efavirenz 205-214 ATP binding cassette subfamily B member 1 Homo sapiens 123-165 31628422-6 2020 We designed and validated a CYP2B6 activity score model based on two CYP2B6 SNPs (G516T and rs4803419) that predicted efavirenz disposition better than G516T alone. efavirenz 118-127 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 28-34 31628422-6 2020 We designed and validated a CYP2B6 activity score model based on two CYP2B6 SNPs (G516T and rs4803419) that predicted efavirenz disposition better than G516T alone. efavirenz 118-127 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 69-75 32106141-8 2020 At day 21 in the efavirenz group, CYP2B6 genotype was associated with increased plasma efavirenz exposure (P = 3.2 x 10), decreased plasma concentrations of etonogestrel (P = 1.7 x 10), and decreased ethinyl estradiol (P = 6.7 x 10). efavirenz 17-26 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 34-40 32106141-8 2020 At day 21 in the efavirenz group, CYP2B6 genotype was associated with increased plasma efavirenz exposure (P = 3.2 x 10), decreased plasma concentrations of etonogestrel (P = 1.7 x 10), and decreased ethinyl estradiol (P = 6.7 x 10). efavirenz 87-96 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 34-40 32106141-9 2020 Compared to controls, efavirenz reduced median etonogestrel concentrations by at least 93% in CYP2B6 slow metabolizers versus approximately 75% in normal and intermediate metabolizers. efavirenz 22-31 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 94-100 32106141-10 2020 Efavirenz reduced median ethinyl estradiol concentrations by 75% in CYP2B6 slow metabolizers versus approximately 41% in normal and intermediate metabolizers. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 68-74 32106141-11 2020 CONCLUSION: CYP2B6 slow metabolizer genotype worsens the pharmacokinetic interaction of efavirenz with hormonal contraceptives administered by vaginal ring. efavirenz 88-97 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 12-18 32106141-12 2020 Efavirenz dose reduction in CYP2B6 slow metabolizers may reduce, but will likely not eliminate, this interaction. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 28-34 31777202-7 2020 Efavirenz, an activator of CYP46A1 that is known to penetrate the blood-brain barrier, inhibited GBM growth in vivo. efavirenz 0-9 cytochrome P450 family 46 subfamily A member 1 Homo sapiens 27-34 31339646-1 2019 We investigated the effect of efavirenz on the activities of cytochrome P450 (CYP)1A2, CYP2A6, xanthine oxidase (XO), and N-acetyltransferase 2 (NAT2), using caffeine as a probe. efavirenz 30-39 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 61-85 31339646-1 2019 We investigated the effect of efavirenz on the activities of cytochrome P450 (CYP)1A2, CYP2A6, xanthine oxidase (XO), and N-acetyltransferase 2 (NAT2), using caffeine as a probe. efavirenz 30-39 N-acetyltransferase 2 Homo sapiens 122-143 31006110-2 2019 Efavirenz is predominantly metabolized into inactive metabolites by cytochrome P450 (CYP)2B6, and patients with certain CYP2B6 genetic variants may be at increased risk for adverse effects, particularly central nervous system toxicity and treatment discontinuation. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 68-92 31006110-2 2019 Efavirenz is predominantly metabolized into inactive metabolites by cytochrome P450 (CYP)2B6, and patients with certain CYP2B6 genetic variants may be at increased risk for adverse effects, particularly central nervous system toxicity and treatment discontinuation. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 120-126 31006110-3 2019 We summarize the evidence from the literature and provide therapeutic recommendations for efavirenz prescribing based on CYP2B6 genotypes. efavirenz 90-99 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 121-127 31324697-4 2019 CYP2B6 genetics and drug interactions are major determinants of clinical efavirenz disposition and dose adjustment. efavirenz 73-82 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 31324697-6 2019 Metabolism of R-efavirenz by CYP2B6 remains unexplored. efavirenz 14-25 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 29-35 31324697-8 2019 This investigation also evaluated R-efavirenz hydroxylation by wild-type CYP2B6.1 and CYP2B6 variants. efavirenz 34-45 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 73-79 31324697-11 2019 Rates of R-efavirenz metabolism were approximately 1/10 those of S-efavirenz for wild-type CYP2B6.1 and variants. efavirenz 9-20 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 91-97 31324697-12 2019 On the basis of Clmax values, there was 14-fold enantioselectivity (S > R-efavirenz) for wild-type CYP2B6.1, and 5- to 22-fold differences for other CYP2B6 variants. efavirenz 72-83 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 99-105 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 186-195 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 29-35 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 186-195 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 186-195 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 186-195 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 186-195 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 291-300 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 29-35 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 291-300 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 291-300 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 291-300 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 31324697-13 2019 These results show that both CYP2B6 516G > T (CYP2B6*6 and CYP2B6*9) and 983T > C (CYP2B6*16 and CYP2B6*18) polymorphisms cause canonical diminishment or loss-of-function variants for S-efavirenz 8-hydroxylation, provide a mechanistic basis for known clinical pharmacogenetic differences in efavirenz disposition, and may predict additional clinically important variant alleles. efavirenz 291-300 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 31324697-14 2019 Efavirenz is the most stereoselective CYP2B6 drug substrate yet identified and may be a useful probe for the CYP2B6 active site and catalytic mechanisms. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 38-44 31324697-14 2019 Efavirenz is the most stereoselective CYP2B6 drug substrate yet identified and may be a useful probe for the CYP2B6 active site and catalytic mechanisms. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 109-115 31324697-16 2019 Expressed CYP2B6 with 516G>T (CYP2B6*6 and CYP2B6*9), and 983T>C (CYP2B6*16 and CYP2B6*18) polymorphisms had a diminishment or loss of function for efavirenz 8-hydroxylation. efavirenz 148-157 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 10-16 31324697-19 2019 With greater than 10-fold enantioselectivity (S- vs. R- metabolism), efavirenz is the most stereoselective CYP2B6 drug substrate yet identified. efavirenz 69-78 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 107-113 31299074-7 2019 In the efavirenz group CYP2B6 516 G>T was associated with 43% lower etonogestrel Cmin and 34% lower AUC0-24weeks. efavirenz 7-16 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 23-29 31299074-10 2019 Efavirenz plus the etonogestrel contraceptive implant results in a detrimental drug-drug interaction irrespective of patient genetics, which is worsened in women possessing variant alleles for these CYP2B6 SNPs. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 199-205 31409277-10 2019 Median body mass index and CD4 count at efavirenz commencement was 21 (IQR: 19-23) and 260 cells/mm3 (IQR: 126-412) respectively. efavirenz 40-49 CD4 molecule Homo sapiens 27-30 31243456-2 2019 Our objectives are to characterize the effects of rifampicin- and isoniazid-containing anti-TB therapy and CYP2B6 activity on efavirenz concentrations in children, using non-linear mixed-effects modelling. efavirenz 126-135 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 107-113 31075350-9 2019 Also, in EFV-treated cells, p62 was associated with mitochondria, which may be related to the mito-protective function of this autophagic protein. efavirenz 9-12 sequestosome 1 Homo sapiens 28-31 31063705-0 2019 The key genes, phosphoproteins, processes, and pathways affected by efavirenz-activated CYP46A1 in the amyloid-decreasing paradigm of efavirenz treatment. efavirenz 68-77 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 88-95 31063705-0 2019 The key genes, phosphoproteins, processes, and pathways affected by efavirenz-activated CYP46A1 in the amyloid-decreasing paradigm of efavirenz treatment. efavirenz 134-143 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 88-95 31063705-1 2019 Efavirenz (EFV) is an anti-HIV drug, and cytochrome P450 46A1 (CYP46A1) is the major brain cholesterol hydroxylase. efavirenz 0-9 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 63-70 31063705-1 2019 Efavirenz (EFV) is an anti-HIV drug, and cytochrome P450 46A1 (CYP46A1) is the major brain cholesterol hydroxylase. efavirenz 11-14 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 63-70 31063705-9 2019 The key genes, phosphoproteins, processes, and pathways affected by efavirenz-activated CYP46A1 in the amyloid-decreasing paradigm of efavirenz treatment. efavirenz 68-77 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 88-95 31241542-1 2019 BACKGROUND: CYP2B6 516 genotype-directed dosing improves efavirenz (EFV) exposures in HIV-infected children younger than 36 months, but such data are lacking in those with tuberculosis (TB) coinfection. efavirenz 57-66 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 12-18 31241542-1 2019 BACKGROUND: CYP2B6 516 genotype-directed dosing improves efavirenz (EFV) exposures in HIV-infected children younger than 36 months, but such data are lacking in those with tuberculosis (TB) coinfection. efavirenz 68-71 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 12-18 30859284-17 2019 EFV on nongated-NCCT may serve as an independent biomarker for predicting coronary artery disease with accuracy equivalent to that of EFV on gated CCTA. efavirenz 0-3 solute carrier family 12 member 3 Homo sapiens 16-20 31062296-0 2019 CYP46A1 Activation by Efavirenz Leads to Behavioral Improvement without Significant Changes in Amyloid Plaque Load in the Brain of 5XFAD Mice. efavirenz 22-31 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 0-7 31062296-2 2019 Efavirenz is assessed for activation of cytochrome P450 46A1 (CYP46A1), a CNS-specific enzyme that converts cholesterol to 24-hydroxycholesterol. efavirenz 0-9 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 40-60 31062296-2 2019 Efavirenz is assessed for activation of cytochrome P450 46A1 (CYP46A1), a CNS-specific enzyme that converts cholesterol to 24-hydroxycholesterol. efavirenz 0-9 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 62-69 30918485-14 2019 As reduced dose EFV has a lower toxicity profile, we predicted the reduction in HIV infection when 400 mg EFV-PrEP was poorly adhered to, when it was taken "on demand" and as post-exposure prophylaxis (PEP). efavirenz 16-19 prolyl endopeptidase Homo sapiens 202-205 31223608-14 2019 EFV reduced RANKL-mediated osteoclast formation and activation by inhibiting expression of nuclear factor of activated T cells 1, a key factor of osteoclastogenesis. efavirenz 0-3 TNF superfamily member 11 Homo sapiens 12-17 30677459-2 2019 Herein, we investigated the role of pregnane X receptor (PXR) in mediating the adverse effects of efavirenz on lipid homeostasis. efavirenz 98-107 nuclear receptor subfamily 1, group I, member 2 Mus musculus 36-55 30677459-2 2019 Herein, we investigated the role of pregnane X receptor (PXR) in mediating the adverse effects of efavirenz on lipid homeostasis. efavirenz 98-107 nuclear receptor subfamily 1, group I, member 2 Mus musculus 57-60 30677459-5 2019 RESULTS: We found that efavirenz is a potent PXR-selective agonist that can efficiently activate PXR and induce its target gene expression in vitro and in vivo. efavirenz 23-32 nuclear receptor subfamily 1, group I, member 2 Mus musculus 45-48 30677459-5 2019 RESULTS: We found that efavirenz is a potent PXR-selective agonist that can efficiently activate PXR and induce its target gene expression in vitro and in vivo. efavirenz 23-32 nuclear receptor subfamily 1, group I, member 2 Mus musculus 97-100 30220106-7 2019 The HIV-1-proteins Tat, Gp120 and Nef in particular, the proinflammatory cytokine, TNF-alpha, and the antiretroviral drugs Efavirenz and Lopinavir, most commonly postulated to be primary causal agents of endothelial dysfunction, are also discussed. efavirenz 123-132 S100 calcium binding protein B Homo sapiens 34-37 29635009-0 2018 The impact of CYP2B6 polymorphisms on the interactions of efavirenz with lumefantrine: Implications for paediatric antimalarial therapy. efavirenz 58-67 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 14-20 30535366-8 2019 CYP2A6 -48A C was independently associated with higher CSF 8-hydroxy-efavirenz:efavirenz ratio (beta = 0.54, P = 0.048). efavirenz 69-78 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 0-6 30535366-9 2019 CYP2B6 rs2279345 polymorphism was associated with lower plasma 7-hydroxy-efavirenz:efavirenz ratio in multivariate analyses (P < 0.05). efavirenz 73-82 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 30201214-1 2018 Genetic variations within cytochrome P450 2B6 (CYP2B6) contribute to inter-individual variation in the metabolism of clinically important drugs, including cyclophosphamide, bupropion, methadone and efavirenz (EFZ). efavirenz 198-207 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 26-45 30201214-1 2018 Genetic variations within cytochrome P450 2B6 (CYP2B6) contribute to inter-individual variation in the metabolism of clinically important drugs, including cyclophosphamide, bupropion, methadone and efavirenz (EFZ). efavirenz 198-207 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 47-53 30201214-1 2018 Genetic variations within cytochrome P450 2B6 (CYP2B6) contribute to inter-individual variation in the metabolism of clinically important drugs, including cyclophosphamide, bupropion, methadone and efavirenz (EFZ). efavirenz 209-212 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 26-45 30201214-1 2018 Genetic variations within cytochrome P450 2B6 (CYP2B6) contribute to inter-individual variation in the metabolism of clinically important drugs, including cyclophosphamide, bupropion, methadone and efavirenz (EFZ). efavirenz 209-212 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 47-53 29868865-12 2018 Conclusions: In a highly admixed Brazilian cohort, the CYP2B6 slow metabolizer genotype was associated with an increased risk of efavirenz adverse effects. efavirenz 129-138 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 55-61 31039134-3 2019 Both rifampicin and efavirenz are activators of the pregnane X receptor (PXR), a transcription factor with significant inter-species differences in ligand-dependent activation. efavirenz 20-29 nuclear receptor subfamily 1 group I member 2 Homo sapiens 52-71 31039134-3 2019 Both rifampicin and efavirenz are activators of the pregnane X receptor (PXR), a transcription factor with significant inter-species differences in ligand-dependent activation. efavirenz 20-29 nuclear receptor subfamily 1 group I member 2 Homo sapiens 73-76 30442673-2 2019 Here we demonstrate that EFV stimulates the activation in primary hepatocytes of key cell stress regulators: inositol-requiring 1alpha (IRE1alpha) and X-box binding protein 1 (XBP1). efavirenz 25-28 endoplasmic reticulum (ER) to nucleus signalling 1 Mus musculus 109-134 30442673-2 2019 Here we demonstrate that EFV stimulates the activation in primary hepatocytes of key cell stress regulators: inositol-requiring 1alpha (IRE1alpha) and X-box binding protein 1 (XBP1). efavirenz 25-28 endoplasmic reticulum (ER) to nucleus signalling 1 Mus musculus 136-145 30442673-2 2019 Here we demonstrate that EFV stimulates the activation in primary hepatocytes of key cell stress regulators: inositol-requiring 1alpha (IRE1alpha) and X-box binding protein 1 (XBP1). efavirenz 25-28 X-box binding protein 1 Mus musculus 151-174 30442673-2 2019 Here we demonstrate that EFV stimulates the activation in primary hepatocytes of key cell stress regulators: inositol-requiring 1alpha (IRE1alpha) and X-box binding protein 1 (XBP1). efavirenz 25-28 X-box binding protein 1 Mus musculus 176-180 30442673-3 2019 Following EFV exposure, XBP1 splicing (indicating activation) was increased 35.7-fold in primary human hepatocytes. efavirenz 10-13 X-box binding protein 1 Homo sapiens 24-28 30442673-5 2019 Of note, with EFV treatment, 47.2% of mouse hepatocytes were apoptotic; which was decreased to 23.9% in the presence of STF 083010, an inhibitor of XBP1 splicing. efavirenz 14-17 X-box binding protein 1 Mus musculus 148-152 30442673-7 2019 Interestingly, incubation with the primary metabolite of EFV, 8-hydroxyefavirenz (8-OHEFV), only resulted in 10.3- and 2.9-fold increased XBP1 splicing in human and mouse hepatocytes and no change in levels of p-IRE1alpha in mouse hepatocytes. efavirenz 57-60 X-box binding protein 1 Homo sapiens 138-142 30442673-7 2019 Interestingly, incubation with the primary metabolite of EFV, 8-hydroxyefavirenz (8-OHEFV), only resulted in 10.3- and 2.9-fold increased XBP1 splicing in human and mouse hepatocytes and no change in levels of p-IRE1alpha in mouse hepatocytes. efavirenz 57-60 endoplasmic reticulum to nucleus signaling 1 Homo sapiens 212-221 30442673-8 2019 To further probe the structure-activity relationship of IRE1alpha-XBP1 activation by EFV, 16 EFV analogs were employed. efavirenz 85-88 endoplasmic reticulum (ER) to nucleus signalling 1 Mus musculus 56-65 30442673-8 2019 To further probe the structure-activity relationship of IRE1alpha-XBP1 activation by EFV, 16 EFV analogs were employed. efavirenz 85-88 X-box binding protein 1 Mus musculus 66-70 31654514-8 2019 In the EFV-regimen group, TC, HDL-C, and LDL-C were increased compared to baseline, while the TC/HDL-C ratio decreased, and TG did not change significantly. efavirenz 7-10 component of oligomeric golgi complex 2 Homo sapiens 41-46 31256164-9 2019 RESULTS: We observed significantly decreased CYP21A2 activity in both in vitro testing systems after treatment with efavirenz at therapeutic concentrations. efavirenz 116-125 cytochrome P450 family 21 subfamily A member 2 Homo sapiens 45-52 29191071-4 2018 Efavirenz exhibited a type II spectral change with binding to CYP3A4 indicating a possible inhibitor. efavirenz 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 29855606-5 2018 Composite CYP2B-mediated EFV metabolism was significantly associated with CNS toxicity (p = 0.04), with extensive metabolizers reporting more and slow and very slow metabolizers reporting less toxicity after 1 month compared to intermediate metabolizers. efavirenz 25-28 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 10-15 30114293-6 2018 Efavirenz also reduced the efflux of calcein from MDCK-MRP2 cells, but had a rather weak inhibitory effect on Hoechst 33342 accumulation in MDCK-MDR1 and MDCK-BCRP cells. efavirenz 0-9 ATP binding cassette subfamily C member 2 Canis lupus familiaris 55-59 30114293-6 2018 Efavirenz also reduced the efflux of calcein from MDCK-MRP2 cells, but had a rather weak inhibitory effect on Hoechst 33342 accumulation in MDCK-MDR1 and MDCK-BCRP cells. efavirenz 0-9 ATP binding cassette subfamily B member 1 Canis lupus familiaris 145-149 30114293-6 2018 Efavirenz also reduced the efflux of calcein from MDCK-MRP2 cells, but had a rather weak inhibitory effect on Hoechst 33342 accumulation in MDCK-MDR1 and MDCK-BCRP cells. efavirenz 0-9 ATP binding cassette subfamily G member 2 Canis lupus familiaris 159-163 30135687-4 2018 In this work, a longitudinal analysis was performed to evaluate APOBEC3G/3A expression in peripheral blood mononuclear cells of antiretroviral-naive HIV-1-infected individuals treated with cenicriviroc (CVC) or efavirenz (EFV) at baseline and 4, 12, 24, and 48 weeks post-treatment follow-up. efavirenz 222-225 apolipoprotein B mRNA editing enzyme catalytic subunit 3G Homo sapiens 64-72 29875890-8 2018 From EFV+AZT+3TC group, the mean CD4 cell count difference from baseline was 205(95% CI 155.404-235.623, p< 0.001). efavirenz 5-8 CD4 molecule Homo sapiens 33-36 29661866-8 2018 In human hepatocytes and adipocytes, known target cells of FGF21 action, efavirenz, elvitegravir, and the lopinavir-ritonavir combination exerted inhibitory effects on KLB gene expression. efavirenz 73-82 klotho beta Homo sapiens 168-171 29430850-1 2018 Efavirenz (EFV), an antiretroviral that interacts clinically with co-administered drugs via activation of the pregnane X receptor (PXR), is extensively metabolized by the cytochromes P450. efavirenz 0-9 nuclear receptor subfamily 1, group I, member 2 Mus musculus 110-129 29430850-1 2018 Efavirenz (EFV), an antiretroviral that interacts clinically with co-administered drugs via activation of the pregnane X receptor (PXR), is extensively metabolized by the cytochromes P450. efavirenz 0-9 nuclear receptor subfamily 1, group I, member 2 Mus musculus 131-134 29430850-1 2018 Efavirenz (EFV), an antiretroviral that interacts clinically with co-administered drugs via activation of the pregnane X receptor (PXR), is extensively metabolized by the cytochromes P450. efavirenz 11-14 nuclear receptor subfamily 1, group I, member 2 Mus musculus 110-129 29430850-1 2018 Efavirenz (EFV), an antiretroviral that interacts clinically with co-administered drugs via activation of the pregnane X receptor (PXR), is extensively metabolized by the cytochromes P450. efavirenz 11-14 nuclear receptor subfamily 1, group I, member 2 Mus musculus 131-134 29430850-2 2018 We tested whether its primary metabolite, 8-hydroxyEFV (8-OHEFV) can activate PXR and potentially contribute to PXR-mediated drug-drug interactions attributed to EFV. efavirenz 51-54 nuclear receptor subfamily 1, group I, member 2 Mus musculus 78-81 29430850-2 2018 We tested whether its primary metabolite, 8-hydroxyEFV (8-OHEFV) can activate PXR and potentially contribute to PXR-mediated drug-drug interactions attributed to EFV. efavirenz 51-54 nuclear receptor subfamily 1, group I, member 2 Mus musculus 112-115 29430850-4 2018 Corroborating this, treatment with EFV for 72 h elevated the mRNA abundance of the PXR target gene, Cyp3a11, by approximately 28-fold in primary hepatocytes isolated from PXR-humanized mice, whereas treatment with 8-OHEFV did not result in a change in Cyp3A11 mRNA levels. efavirenz 35-38 nuclear receptor subfamily 1, group I, member 2 Mus musculus 83-86 29430850-4 2018 Corroborating this, treatment with EFV for 72 h elevated the mRNA abundance of the PXR target gene, Cyp3a11, by approximately 28-fold in primary hepatocytes isolated from PXR-humanized mice, whereas treatment with 8-OHEFV did not result in a change in Cyp3A11 mRNA levels. efavirenz 35-38 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 100-107 29430850-4 2018 Corroborating this, treatment with EFV for 72 h elevated the mRNA abundance of the PXR target gene, Cyp3a11, by approximately 28-fold in primary hepatocytes isolated from PXR-humanized mice, whereas treatment with 8-OHEFV did not result in a change in Cyp3A11 mRNA levels. efavirenz 35-38 nuclear receptor subfamily 1, group I, member 2 Mus musculus 171-174 29430850-4 2018 Corroborating this, treatment with EFV for 72 h elevated the mRNA abundance of the PXR target gene, Cyp3a11, by approximately 28-fold in primary hepatocytes isolated from PXR-humanized mice, whereas treatment with 8-OHEFV did not result in a change in Cyp3A11 mRNA levels. efavirenz 35-38 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 252-259 29430850-5 2018 FRET-based competitive binding assays and isothermal calorimetry demonstrated that even with the lack of ability to activate PXR, 8-OHEFV displays an affinity for PXR (IC50 12.1 mum; KD 7.9 mum) nearly identical to that of EFV (IC50 18.7 mum; KD 12.5 mum). efavirenz 134-137 nuclear receptor subfamily 1, group I, member 2 Mus musculus 163-166 29629676-2 2018 EFV is metabolised in the liver via CYP2B6, and genetic polymorphism of CYP2B6 is known to result in slowed metabolism of the drug. efavirenz 0-3 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 36-42 29098603-8 2018 The moderate CYP3A4 inducer efavirenz 400 mg or 600 mg q.d. efavirenz 28-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-19 29629676-2 2018 EFV is metabolised in the liver via CYP2B6, and genetic polymorphism of CYP2B6 is known to result in slowed metabolism of the drug. efavirenz 0-3 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 72-78 29636682-1 2018 Poor metabolisers of CYP2B6 (PM) require a lower dose of efavirenz because of serious adverse reactions resulting from the higher plasma concentrations associated with a standard dose. efavirenz 57-66 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 21-27 28616806-3 2017 However, it is unknown whether SGLT2 inhibitors could reduce EFV in non-obese patients (BMI <25 kg/m2) with type 2 diabetes. efavirenz 61-64 solute carrier family 5 member 2 Homo sapiens 31-36 29190729-0 2017 Increased MMAB level in mitochondria as a novel biomarker of hepatotoxicity induced by Efavirenz. efavirenz 87-96 metabolism of cobalamin associated B Homo sapiens 10-14 29190729-8 2017 The expression levels of MMAB and ROS were detected in EFV-treated Huh-7 cells with and without shRNA used to knock down MMAB, and in primary hepatocytes (PHC). efavirenz 55-58 metabolism of cobalamin associated B Homo sapiens 25-29 29190729-15 2017 In addition, the liver of EFV-treated HIV infected patients showed substantially higher levels of MMAB expression compared to the livers of untreated or protease inhibitor (PI)-treated HIV-infected patients. efavirenz 26-29 metabolism of cobalamin associated B Homo sapiens 98-102 29190729-17 2017 MMAB was increased in EFV-treated Huh-7 cells and primary hepatocytes. efavirenz 22-25 metabolism of cobalamin associated B Homo sapiens 0-4 29534103-8 2018 RESULTS: In the CD4+ T-cell population, HIVpt affected 13/30 of patients on EFV versus 10/21 on ATV. efavirenz 76-79 CD4 molecule Homo sapiens 16-19 29534103-9 2018 In the CD4+CD45RO+ T-cell population, HIVpt was present in 14/30 of patients on EFV versus 15/21 on ATV. efavirenz 80-83 CD4 molecule Homo sapiens 7-10 29308748-6 2018 RESULTS: Both groups demonstrated a significant increase in their CD4+ T cell count which was greater in Zidovudine/Lamivudine and Efavirenz treated group. efavirenz 131-140 CD4 molecule Homo sapiens 66-69 29308748-8 2018 CONCLUSION: A rapid CD4+ Tcell increase occurred shortly after beginning ART consisting either Vonavir or combination of Zidovudine, Lamivudine and Efavirenz. efavirenz 148-157 CD4 molecule Homo sapiens 20-23 29308748-9 2018 Late increases in CD4+ T cell counts were more pronounced in therapy using Zidovudine/ Lamivudine and Efavirenz. efavirenz 102-111 CD4 molecule Homo sapiens 18-21 28874142-9 2017 In multivariate analysis, the variables independently associated with increased IFN-gamma production in response to PPD antigen were CD4+ T cell counts <200 cells/mm3 at baseline, age, site of tuberculosis, 800 mg efavirenz dose and follow-up CD4+ T cell counts. efavirenz 217-226 interferon gamma Homo sapiens 80-89 28655608-3 2017 We enhanced CYP46A1 activity pharmacologically by treating 5XFAD mice, a model of rapid amyloidogenesis, with a low dose of the anti-HIV medication efavirenz. efavirenz 148-157 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 12-19 28655608-6 2017 Nevertheless, efavirenz activated CYP46A1 and mouse cerebral cholesterol turnover during the first four months of administration. efavirenz 14-23 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 34-41 28655608-11 2017 We suggest that CYP46A1 activation by efavirenz could be a new anti-Alzheimer"s disease treatment and a tool to study and identify normal and pathological brain processes affected by cholesterol maintenance. efavirenz 38-47 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 16-23 28718515-8 2017 CYP2B6 516G T was significantly associated with EFV concentrations (p<0.001). efavirenz 48-51 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 28559276-4 2017 EFV concentration data were well described by a two-compartment model with first-order absorption (Ka ) and absorption lag time (Alag) (Ka = 0.2 h-1; Alag = 0.83 h; central compartment clearance [CLc/F] for CYP2B6*1/*1 = 18 liters/h, for CYP2B6*1/*6 = 14 liters/h, and for CYP2B6*6/*6 = 8.6 liters/h) and PBMCs as a peripheral compartment. efavirenz 0-3 Charcot-Leyden crystal galectin Homo sapiens 196-199 28481785-2 2017 Our objective was to investigate the relationship between the CYP2B6 516G>T genotype and late virologic failure in patients treated with EFV in Gaborone, Botswana. efavirenz 140-143 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 62-68 28481785-10 2017 CONCLUSION: The CYP2B6 516 T-allele was protective against late virologic breakthrough in patients with initial (6 month) HIV RNA suppression on EFV-based ART. efavirenz 145-148 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 16-22 28559276-9 2017 CYP2B6*6 genotype polymorphisms were associated with decreased EFV and 8OHEFV clearance. efavirenz 63-66 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 28456686-3 2017 Efavirenz was recently reported to interact in a similar concentration range with a number of receptors, transporters and ion channels including recombinant rat alpha1beta2gamma2 GABAA receptors whose actions were potentiated (Gatch et al., 2013; Dalwadi et al., 2016). efavirenz 0-9 adrenoceptor alpha 1D Homo sapiens 161-178 28194792-2 2017 In 12 healthy participants individual CYP3A activity was quantified using a semisimultaneous methodology (midazolam orally and 6 hours later intravenously) both alone and during a period of 22 days after a single oral dose of 400 mg efavirenz. efavirenz 233-242 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 28403028-4 2017 RECENT FINDINGS: Dose adjustments of standard dose efavirenz are not necessary with rifampicin, because auto-induction of CYP2B6 by efavirenz counteracts the induction of rifampicin. efavirenz 132-141 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 122-128 27599706-4 2017 METHODS: This study predicted the magnitude of the DDI between efavirenz, an inducer of CYP3A4 and inhibitor of CYP2C8, and dual CYP3A4/CYP2C8 substrates (repaglinide, montelukast, pioglitazone, paclitaxel) using a physiologically based pharmacokinetic (PBPK) modeling approach integrating concurrent effects on CYPs. efavirenz 63-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 28642370-5 2017 We also found that l-Glu and other activating neurotransmitters bind to the same site on the CYP46A1 surface, which differs from the EFV-binding site. efavirenz 133-136 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 93-100 28642370-6 2017 The other principal differences between EFV and l-Glu in CYP46A1 activation include an apparent lack of l-Glu binding to the P450 active site and different pathways of signal transduction from the allosteric site to the active site. efavirenz 40-43 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 57-64 28642370-7 2017 EFV and l-Glu similarly increased the CYP46A1 kcat, the rate of the "fast" phase of the enzyme reduction by the redox partner NADPH-cytochrome P450 oxidoreductase, and the amount of P450 reduced. efavirenz 0-3 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 38-45 28642370-8 2017 Spectral titrations with cholesterol, in the presence of EFV or l-Glu, suggest that water displacement from the heme iron can be affected in activator-bound CYP46A1. efavirenz 57-60 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 157-164 28642370-9 2017 Moreover, EFV and l-Glu synergistically activated CYP46A1. efavirenz 10-13 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 50-57 27599706-4 2017 METHODS: This study predicted the magnitude of the DDI between efavirenz, an inducer of CYP3A4 and inhibitor of CYP2C8, and dual CYP3A4/CYP2C8 substrates (repaglinide, montelukast, pioglitazone, paclitaxel) using a physiologically based pharmacokinetic (PBPK) modeling approach integrating concurrent effects on CYPs. efavirenz 63-72 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 112-118 27599706-4 2017 METHODS: This study predicted the magnitude of the DDI between efavirenz, an inducer of CYP3A4 and inhibitor of CYP2C8, and dual CYP3A4/CYP2C8 substrates (repaglinide, montelukast, pioglitazone, paclitaxel) using a physiologically based pharmacokinetic (PBPK) modeling approach integrating concurrent effects on CYPs. efavirenz 63-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 27599706-4 2017 METHODS: This study predicted the magnitude of the DDI between efavirenz, an inducer of CYP3A4 and inhibitor of CYP2C8, and dual CYP3A4/CYP2C8 substrates (repaglinide, montelukast, pioglitazone, paclitaxel) using a physiologically based pharmacokinetic (PBPK) modeling approach integrating concurrent effects on CYPs. efavirenz 63-72 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 136-142 27799216-5 2017 Wistar rats were administered efavirenz (10 mg kg of body weight-1) once daily over 5 weeks. efavirenz 30-39 Body weight QTL 17 Rattus norvegicus 58-66 28321215-3 2017 We found that IFN-lambdas synergistically enhanced anti-HIV activity of antiretrovirals [azidothymidine (AZT), efavirenz, indinavir, and enfuvirtide] in infected macrophages. efavirenz 111-120 interferon alpha 1 Homo sapiens 14-17 27639578-6 2017 EFV-mediated toxicity is initiated with the permeabilization of mitochondrial outer membrane and change in mitochondrial membrane potential (Deltapsim) which triggers a series of events like cytochrome c release, alteration in mitochondrial morphology and mitochondria-mediated apoptosis. efavirenz 0-3 cytochrome c, somatic Homo sapiens 191-203 28143541-14 2017 The predicted CD4+ count for TDF/3TC/EFV was (B = +347.65 cells/mm3, P < 0.001) whereas that of AZT/3TC/EFV was (B = +281.54 cells/mm3, P < 0.001). efavirenz 37-40 CD4 molecule Homo sapiens 14-17 27872069-3 2017 While doravirine is a cytochrome P450 3A4 (CYP3A4) substrate, efavirenz induces CYP3A4; therefore, the pharmacokinetics of both drugs following a switch from efavirenz to doravirine were assessed. efavirenz 62-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 27872069-6 2017 Following a 7-day washout, efavirenz was administered at 600 mg QD for 14 days (period 2). efavirenz 27-36 period circadian regulator 2 Homo sapiens 80-88 27404500-9 2017 Efavirenz, stavudine and ritonavir significantly down-regulated the bioactivating CYP2R1 and up-regulated the catabolic CYP24A1. efavirenz 0-9 cytochrome P450 family 2 subfamily R member 1 Homo sapiens 82-88 27404500-9 2017 Efavirenz, stavudine and ritonavir significantly down-regulated the bioactivating CYP2R1 and up-regulated the catabolic CYP24A1. efavirenz 0-9 cytochrome P450 family 24 subfamily A member 1 Homo sapiens 120-127 27799204-8 2017 Apparent oral clearance of efavirenz was reduced by 25% and 51% in subjects predicted to have intermediate and slow CYP2B6 metabolizer status, respectively. efavirenz 27-36 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 116-122 28836850-7 2016 Further, we found that EFV promoted increased lactate dehydrogenase (LDH) release, activation of p38 mitogen-activated protein kinase (MAPK), and increased Bax expression in cultured NSCs. efavirenz 23-26 BCL2-associated X protein Mus musculus 156-159 27903949-4 2017 The authors report 2 cases in which a possible drug-herb interaction may have led to virological breakthrough in patients who were maintained on the same regimen for many years, including lamivudine (3TC)/zidovudine (ZDV)/efavirenz (EFV) and emtricitabine (FTC)/tenofovir (TDF)/EFV, respectively. efavirenz 222-231 sex determining region Y Homo sapiens 273-276 27903949-4 2017 The authors report 2 cases in which a possible drug-herb interaction may have led to virological breakthrough in patients who were maintained on the same regimen for many years, including lamivudine (3TC)/zidovudine (ZDV)/efavirenz (EFV) and emtricitabine (FTC)/tenofovir (TDF)/EFV, respectively. efavirenz 233-236 sex determining region Y Homo sapiens 273-276 27903949-4 2017 The authors report 2 cases in which a possible drug-herb interaction may have led to virological breakthrough in patients who were maintained on the same regimen for many years, including lamivudine (3TC)/zidovudine (ZDV)/efavirenz (EFV) and emtricitabine (FTC)/tenofovir (TDF)/EFV, respectively. efavirenz 278-281 sex determining region Y Homo sapiens 273-276 27779789-4 2016 CNS toxicity occurring with the recommended standard dose of EFV remains a challenge and may in part be attributable to polymorphisms in cytochrome P450 (CYP) 2B6, the enzyme involved in the major metabolic pathway for converting EFV to inactive metabolites. efavirenz 61-64 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 137-162 27779789-5 2016 Functionally deficient alleles of CYP2B6 such as CYP2B6*6, *18, and *22 may be responsible for significantly higher therapeutic concentrations of EFV at a standard dose of 600 mg/day. efavirenz 146-149 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 34-40 27779789-5 2016 Functionally deficient alleles of CYP2B6 such as CYP2B6*6, *18, and *22 may be responsible for significantly higher therapeutic concentrations of EFV at a standard dose of 600 mg/day. efavirenz 146-149 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 49-55 27098343-10 2016 When administered together with endogenous vitamin D metabolites, dexamethasone and efavirenz counteracted the 1,25D3 -mediated up-regulation of CYP24A1, which inactivates 1,25D3 . efavirenz 84-93 cytochrome P450 family 24 subfamily A member 1 Homo sapiens 145-152 27704562-8 2016 Subjects received a single oral dose of 1200 mg raltegravir co-administered with 600 mg efavirenz on Day 12 of Period 2. efavirenz 88-97 period circadian regulator 2 Homo sapiens 111-119 27125860-9 2016 The study also calls for caution related to higher exposure to 8-OH-EFV during simultaneous coadministration of EFV and RIF-based anti-TB regimens, which may be associated with neurotoxicity, particularly in female patients and CYP2B6*6 carriers. efavirenz 68-71 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 228-234 27422672-6 2016 Although bupropion and efavirenz have been used and are recommended by regulatory agencies as clinical CYP2B6 probe substrates for DDI studies, CYP3A4 contributes to the metabolism of both probes and is induced by all reference CYP2B6 inducers. efavirenz 23-32 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 103-109 27600044-3 2016 Efavirenz, a nonnucleoside HIV-1 reverse transcriptase inhibitor, is mainly cleared by CYP2B6, an enzyme strongly inhibited in vitro by voriconazole. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 87-93 27333947-2 2016 Since EFV is metabolized by the cytochrome P450 (CYP) 2B6 enzyme, we hypothesized that EFV would lengthen the rate-corrected QT (QTcF) interval in carriers of the CYP2B6*6 decreased functional allele. efavirenz 6-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 32-57 27333947-2 2016 Since EFV is metabolized by the cytochrome P450 (CYP) 2B6 enzyme, we hypothesized that EFV would lengthen the rate-corrected QT (QTcF) interval in carriers of the CYP2B6*6 decreased functional allele. efavirenz 6-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 163-169 27333947-2 2016 Since EFV is metabolized by the cytochrome P450 (CYP) 2B6 enzyme, we hypothesized that EFV would lengthen the rate-corrected QT (QTcF) interval in carriers of the CYP2B6*6 decreased functional allele. efavirenz 87-90 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 32-57 27333947-2 2016 Since EFV is metabolized by the cytochrome P450 (CYP) 2B6 enzyme, we hypothesized that EFV would lengthen the rate-corrected QT (QTcF) interval in carriers of the CYP2B6*6 decreased functional allele. efavirenz 87-90 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 163-169 27333947-7 2016 RESULTS: EFV demonstrated a gene-dose effect and exceeded the FDA criteria for QTcF interval prolongation in CYP2B6*6/*6 carriers. efavirenz 9-12 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 109-115 27646953-5 2016 CASES PRESENTATION: A first case was a 33 years-old female newly diagnosed HIV patient with CD4 count of 4 cells/muL (0 %), normal complete blood count, liver and renal function tests was started on co-formulated tenofovir/emtricitabine/efavirenz and prophylactic cotrimoxazole. efavirenz 237-246 CD4 molecule Homo sapiens 92-95 27333947-9 2016 EFV concentrations exceeding 0.4 mug/mL significantly inhibited outward hERG tail currents (P < 0.05). efavirenz 0-3 ETS transcription factor ERG Homo sapiens 72-76 27333947-10 2016 CONCLUSIONS: This study demonstrates that homozygous carriers of CYP2B6*6 allele may be at increased risk for EFV-induced QTcF interval prolongation via inhibition of hERG. efavirenz 110-113 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 65-71 27333947-10 2016 CONCLUSIONS: This study demonstrates that homozygous carriers of CYP2B6*6 allele may be at increased risk for EFV-induced QTcF interval prolongation via inhibition of hERG. efavirenz 110-113 ETS transcription factor ERG Homo sapiens 167-171 27124896-0 2016 Longitudinal increase in vitamin D binding protein levels after initiation of tenofovir/lamivudine/efavirenz among individuals with HIV. efavirenz 99-108 GC vitamin D binding protein Homo sapiens 25-50 27709010-5 2016 CYP2B6 has been demonstrated to play a role in the metabolism of 2%-10% of clinically used drugs including widely used antineoplastic agents cyclophosphamide and ifosfamide, anesthetics propofol and ketamine, synthetic opioids pethidine and methadone, and the antiretrovirals nevirapine and efavirenz, among others. efavirenz 291-300 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 27216995-7 2016 Efavirenz induced a marked concentration-dependent increase in interleukin-8 expression and release whereas elvitregravir had little effect. efavirenz 0-9 C-X-C motif chemokine ligand 8 Homo sapiens 63-76 27627692-9 2016 On the other hand, HIV patients of African origin are predisposed to developing EFV-induced neuropsychiatric AEs due to specific CYP2B6 genetic variants causing impaired metabolism of EFV. efavirenz 80-83 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 129-135 27627692-9 2016 On the other hand, HIV patients of African origin are predisposed to developing EFV-induced neuropsychiatric AEs due to specific CYP2B6 genetic variants causing impaired metabolism of EFV. efavirenz 184-187 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 129-135 26655325-9 2016 Compared to noncarriers, individuals homozygous for CYP2B6*6 had ~109% increased EFV levels in hair (p = .016) and CYP2B6*18 heterozygotes demonstrated 82% higher EFV hair levels (p = .0006). efavirenz 81-84 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 52-58 26655325-9 2016 Compared to noncarriers, individuals homozygous for CYP2B6*6 had ~109% increased EFV levels in hair (p = .016) and CYP2B6*18 heterozygotes demonstrated 82% higher EFV hair levels (p = .0006). efavirenz 163-166 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 115-121 27067333-3 2016 The objective of this analysis was to support the selection of an appropriate dose for this younger pediatric population and to explore the impact of CYP2B6 genetic polymorphisms on EFV systemic exposures. efavirenz 182-185 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 150-156 26797214-6 2016 Subjects receiving EFV-based cART had 47% and 44% lower atovaquone AUCtau than subjects not receiving cART at atovaquone doses of 750 mg BID and 1500 mg BID, respectively (P<= .01). efavirenz 19-22 BH3 interacting domain death agonist Homo sapiens 153-156 27151598-0 2016 Triple combination MPT vaginal microbicide using curcumin and efavirenz loaded lactoferrin nanoparticles. efavirenz 62-71 lactotransferrin Rattus norvegicus 79-90 26307135-4 2016 Median intact FGF23 tended to increase with past use of both nonnucleoside reverse-transcriptase inhibitors and protease inhibitors, but tended to decrease with recent use of either tenofovir, efavirenz or lopinavir. efavirenz 193-202 fibroblast growth factor 23 Homo sapiens 14-19 26307135-8 2016 Lower levels of intact FGF23 with recent use of tenofovir, efavirenz or lopinavir may reflect their adverse effects on bone and vitamin D metabolism relative to other drugs in their respective drug classes. efavirenz 59-68 fibroblast growth factor 23 Homo sapiens 23-28 26906233-4 2016 He was receiving treatment with efavirenz, emtricitabine and tenofovir, his CD4 count was 580/mm3 and HIV viral load was undetectable. efavirenz 32-41 CD4 molecule Homo sapiens 76-79 26891286-5 2016 Efavirenz (EFV) and nevirapine (NVP) are the major components of HAART both metabolized by CYP2B6, an enzyme that can potentially be inhibited or induced by compounds found in medicinal plant extracts. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 91-97 26891286-5 2016 Efavirenz (EFV) and nevirapine (NVP) are the major components of HAART both metabolized by CYP2B6, an enzyme that can potentially be inhibited or induced by compounds found in medicinal plant extracts. efavirenz 11-14 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 91-97 27045425-4 2016 RESULTS: Simulated AUCs for 600 mg EFV dose were 1.2- and 2.4-times greater than the product label for Ugandans in general and CYP2B6*6/*6 genotypes respectively. efavirenz 35-38 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 127-133 27045425-5 2016 EFV daily doses of 450 and 250 mg for Ugandans and CYP2B6*6/*6 genotypes, respectively, yielded simulated exposures comparable to the product label. efavirenz 0-3 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 51-57 26945366-9 2016 Treatment with efavirenz rather than nevirapine was associated with increased risk of developing diabetes (hazard ratio 1.27 (95% confidence interval (CI): 1.10-1.46)) in a multivariate analysis adjusting for age, sex, body mass index, baseline CD4 count, viral load, NRTI backbone, and exposure to other diabetogenic medicines. efavirenz 15-24 CD4 molecule Homo sapiens 245-248 26681005-1 2015 CYP2B6 is a highly polymorphic isoenzyme involved in the metabolism of many drugs including cyclophosphamide, bupropion, and efavirenz. efavirenz 125-134 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 26599973-8 2016 CYP2B6 activity was inhibited by 19 tryptamines, but weakly compared to efavirenz. efavirenz 72-81 cytochrome P450, family 2, subfamily b, polypeptide 3 Rattus norvegicus 0-6 26779253-4 2015 The drug metabolizing enzyme (DME), CYP2B6, is primarily responsible for EFV metabolism with minor contributions by CYP1A2, CYP2A6, CYP3A4, CYP3A5, and UGT2B7. efavirenz 73-76 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 36-42 26779253-7 2015 METHODS: SNPs in CYP1A2, CYP2B6, UGT2B7, and NR1I2 (PXR) were selected for genotyping among 222 Bantu-speaking South African HIV-infected patients receiving EFV-containing HAART. efavirenz 157-160 nuclear receptor subfamily 1 group I member 2 Homo sapiens 52-55 26531764-8 2016 CONCLUSION: In our study, naive patients starting tenofovir/emtricitabine or abacavir/lamivudine plus efavirenz showed after 48 weeks a significant and comparable decrease in serum concentrations of IL-6, TNF-alpha, ICAM-1, VCAM-1, Eselectin and P-selectin, while the mean level of hs-CRP did not change significantly in any group. efavirenz 102-111 interleukin 6 Homo sapiens 199-203 26531764-8 2016 CONCLUSION: In our study, naive patients starting tenofovir/emtricitabine or abacavir/lamivudine plus efavirenz showed after 48 weeks a significant and comparable decrease in serum concentrations of IL-6, TNF-alpha, ICAM-1, VCAM-1, Eselectin and P-selectin, while the mean level of hs-CRP did not change significantly in any group. efavirenz 102-111 tumor necrosis factor Homo sapiens 205-214 26531764-8 2016 CONCLUSION: In our study, naive patients starting tenofovir/emtricitabine or abacavir/lamivudine plus efavirenz showed after 48 weeks a significant and comparable decrease in serum concentrations of IL-6, TNF-alpha, ICAM-1, VCAM-1, Eselectin and P-selectin, while the mean level of hs-CRP did not change significantly in any group. efavirenz 102-111 intercellular adhesion molecule 1 Homo sapiens 216-222 26531764-8 2016 CONCLUSION: In our study, naive patients starting tenofovir/emtricitabine or abacavir/lamivudine plus efavirenz showed after 48 weeks a significant and comparable decrease in serum concentrations of IL-6, TNF-alpha, ICAM-1, VCAM-1, Eselectin and P-selectin, while the mean level of hs-CRP did not change significantly in any group. efavirenz 102-111 vascular cell adhesion molecule 1 Homo sapiens 224-230 26531764-8 2016 CONCLUSION: In our study, naive patients starting tenofovir/emtricitabine or abacavir/lamivudine plus efavirenz showed after 48 weeks a significant and comparable decrease in serum concentrations of IL-6, TNF-alpha, ICAM-1, VCAM-1, Eselectin and P-selectin, while the mean level of hs-CRP did not change significantly in any group. efavirenz 102-111 selectin E Homo sapiens 232-241 26531764-8 2016 CONCLUSION: In our study, naive patients starting tenofovir/emtricitabine or abacavir/lamivudine plus efavirenz showed after 48 weeks a significant and comparable decrease in serum concentrations of IL-6, TNF-alpha, ICAM-1, VCAM-1, Eselectin and P-selectin, while the mean level of hs-CRP did not change significantly in any group. efavirenz 102-111 selectin P Homo sapiens 246-256 26553012-1 2016 Efavirenz (EFV) is principally metabolized by CYP2B6 to 8-hydroxy-efavirenz (8OH-EFV) and to a lesser extent by CYP2A6 to 7-hydroxy-efavirenz (7OH-EFV). efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 26553012-1 2016 Efavirenz (EFV) is principally metabolized by CYP2B6 to 8-hydroxy-efavirenz (8OH-EFV) and to a lesser extent by CYP2A6 to 7-hydroxy-efavirenz (7OH-EFV). efavirenz 11-14 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 26553012-6 2016 In individuals (n = 67) genotyped for CYP2B6, 2A6, and CYP3A metabolic pathways, 8OH-EFV/EFV ratios in plasma were an index of CYP2B6 phenotypic activity (P < 0.0001), which was also reflected by phase II metabolites 8OH-EFV-glucuronide/EFV and 8OH-EFV-sulfate/EFV ratios. efavirenz 85-88 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 127-133 26831894-2 2016 We describe four children presenting with serious, persistent central nervous system adverse events who were found to have elevated plasma efavirenz concentrations as a result of carrying CYP2B6 single nucleotide polymorphisms, known to play a role in the metabolism of EFV. efavirenz 270-273 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 188-194 25988279-2 2015 In the present study, we explored facilitated transport of efavirenz (EFV, a non-nucleoside reverse transcriptase inhibitor) across BBB using phenylalanine anchored solid lipid nanoparticles (PA-SLN). efavirenz 59-68 sarcolipin Homo sapiens 195-198 26183311-7 2015 In vitro the triple medication efavirenz, tenofovir and emtricitabine leads to a reduced survival fraction and an increased activation of the DNA repair proteins H2AX, Nbs, Atm and 53BP1 in combination with ionizing radiation. efavirenz 31-40 H2A.X variant histone Homo sapiens 162-166 26183311-7 2015 In vitro the triple medication efavirenz, tenofovir and emtricitabine leads to a reduced survival fraction and an increased activation of the DNA repair proteins H2AX, Nbs, Atm and 53BP1 in combination with ionizing radiation. efavirenz 31-40 nibrin Homo sapiens 168-171 26183311-7 2015 In vitro the triple medication efavirenz, tenofovir and emtricitabine leads to a reduced survival fraction and an increased activation of the DNA repair proteins H2AX, Nbs, Atm and 53BP1 in combination with ionizing radiation. efavirenz 31-40 ATM serine/threonine kinase Homo sapiens 173-176 26183311-7 2015 In vitro the triple medication efavirenz, tenofovir and emtricitabine leads to a reduced survival fraction and an increased activation of the DNA repair proteins H2AX, Nbs, Atm and 53BP1 in combination with ionizing radiation. efavirenz 31-40 tumor protein p53 binding protein 1 Homo sapiens 181-186 26050957-4 2015 We treated apolipoprotein E-null (ApoE(-/-)) mice with EFV (75 mg/kg/day) or vehicle, via oral gavage, for 35 days and quantified commonly measured preclinical markers of CVD (intima-media thickening, arterial stiffening) and plaque area. efavirenz 55-58 apolipoprotein E Mus musculus 11-27 26050957-4 2015 We treated apolipoprotein E-null (ApoE(-/-)) mice with EFV (75 mg/kg/day) or vehicle, via oral gavage, for 35 days and quantified commonly measured preclinical markers of CVD (intima-media thickening, arterial stiffening) and plaque area. efavirenz 55-58 apolipoprotein E Mus musculus 34-38 25948712-8 2015 Although efavirenz is known as a marker substrate for human CYP2B6, efavirenz was not oxidized by CYP2B6 but by CYP2C9 in monkeys. efavirenz 9-18 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 60-66 25948712-8 2015 Although efavirenz is known as a marker substrate for human CYP2B6, efavirenz was not oxidized by CYP2B6 but by CYP2C9 in monkeys. efavirenz 68-77 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 98-104 25948712-8 2015 Although efavirenz is known as a marker substrate for human CYP2B6, efavirenz was not oxidized by CYP2B6 but by CYP2C9 in monkeys. efavirenz 68-77 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 112-118 25782332-8 2015 In EFV-based regimens (n = 1162), TDF was significantly associated with higher rates of virologic suppression than AZT (93.8% vs. 88.1%; weighted odds ratio: 2.15 (95% CI: 1.29-3.58; P = 0.003)). efavirenz 3-6 sex determining region Y Homo sapiens 34-37 26107645-12 2015 The frequency of CCTG (0.524) in patients with EFV plasma concentrations < 1 mug/mL was significantly higher than that in other patient groups, while that of ACCT (0.733) was significantly higher in patients with EFV concentrations > 4 mug/mL, relative to other patient groups. efavirenz 47-50 chaperonin containing TCP1 subunit 3 Homo sapiens 17-21 25914645-8 2015 Cellular accumulation of efavirenz and darunavir was also assessed in SLC22A1-expressing KCL22 cells and reversibility of this accumulation was assessed using prazosin. efavirenz 25-34 solute carrier family 22 member 1 Homo sapiens 70-77 26415139-6 2015 Thus, CYP2B6 is a crucial enzyme in the metabolism of antiretroviral drugs, efavirenz and nevirapine. efavirenz 76-85 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 6-12 26288843-4 2015 METHODS: We genotyped CYP2A6, CYP2B6 and CYP3A4, which encode enzymes principally involved in EFV metabolism, from patients enrolled in the multinational SMART, FIRST and ESPRIT studies, for whom outcome data of treatment adherence was available. efavirenz 94-97 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 22-28 26288843-4 2015 METHODS: We genotyped CYP2A6, CYP2B6 and CYP3A4, which encode enzymes principally involved in EFV metabolism, from patients enrolled in the multinational SMART, FIRST and ESPRIT studies, for whom outcome data of treatment adherence was available. efavirenz 94-97 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 30-36 26288843-4 2015 METHODS: We genotyped CYP2A6, CYP2B6 and CYP3A4, which encode enzymes principally involved in EFV metabolism, from patients enrolled in the multinational SMART, FIRST and ESPRIT studies, for whom outcome data of treatment adherence was available. efavirenz 94-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 26288843-8 2015 FINDINGS: Patients with highest pharmacogenetic risk, as defined by cumulative SNPs in CYP2A6, CYP2B6 and CYP3A4, have an increased risk of discontinuation of EFV containing therapy compared to patients with lower genetic risk scores (adjusted HR 1.9, 95% CI 1.2, 3.1, P = 0.009). efavirenz 159-162 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 87-93 26288843-8 2015 FINDINGS: Patients with highest pharmacogenetic risk, as defined by cumulative SNPs in CYP2A6, CYP2B6 and CYP3A4, have an increased risk of discontinuation of EFV containing therapy compared to patients with lower genetic risk scores (adjusted HR 1.9, 95% CI 1.2, 3.1, P = 0.009). efavirenz 159-162 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 95-101 26288843-8 2015 FINDINGS: Patients with highest pharmacogenetic risk, as defined by cumulative SNPs in CYP2A6, CYP2B6 and CYP3A4, have an increased risk of discontinuation of EFV containing therapy compared to patients with lower genetic risk scores (adjusted HR 1.9, 95% CI 1.2, 3.1, P = 0.009). efavirenz 159-162 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-112 30222398-8 2015 In multivariate analysis, efavirenz-based regimens showed more likelihood of immunologic recovery, whether defined as a CD4 cell count of >200 cells/mm3 (hazard ratio [HR] = 1.31 [95% CI, 1.05-1.59]), >350 cells/mm3 (HR = 1.26 [95% CI, 1.08-1.47]), or >500 cells/mm3 (HR = 1.95 [95% CI, 1.57-2.41]). efavirenz 26-35 CD4 molecule Homo sapiens 120-123 25906774-2 2015 EFV, NVP, artemether and lumefantrine are substrates, inhibitors or inducers of CYP3A4 and CYP2B6, creating a potential for drug-drug interactions. efavirenz 0-3 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 91-97 25914645-11 2015 Absolute SLC22A1 IC50 values for efavirenz, darunavir, and prazosin were 21.8, 46.2, and 2.8 muM, respectively. efavirenz 33-42 solute carrier family 22 member 1 Homo sapiens 9-16 25914645-11 2015 Absolute SLC22A1 IC50 values for efavirenz, darunavir, and prazosin were 21.8, 46.2, and 2.8 muM, respectively. efavirenz 33-42 latexin Homo sapiens 93-96 25914645-12 2015 Efavirenz accumulation was higher in SLC22A1-expressing cells compared to mock-transfected cells (17% higher, p = 0.009) which was reversed using prazosin, whereas no difference was observed for darunavir (p = 0.86). efavirenz 0-9 solute carrier family 22 member 1 Homo sapiens 37-44 25096076-0 2014 Pharmacokinetic and pharmacogenomic modelling of the CYP3A activity marker 4beta-hydroxycholesterol during efavirenz treatment and efavirenz/rifampicin co-treatment. efavirenz 107-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-58 25914645-7 2015 SLC22A1 IC50 values for efavirenz, darunavir, and prazosin were determined. efavirenz 24-33 solute carrier family 22 member 1 Homo sapiens 0-7 25733917-4 2015 As a substrate of CYP 3A4, dolutegravir is affected by rifampin, efavirenz, tipranavir/ritonavir, fosamprenavir/ritonavir, and dose increase is required. efavirenz 65-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-25 25777186-9 2015 The mean changes from baseline in CD4 count were similar in both rilpivirine and efavirenz (RR = 1.05, 95% CI: 0.85-1.24). efavirenz 81-90 CD4 molecule Homo sapiens 34-37 25889207-8 2015 RESULTS: CYP2B6*6 and *18 variant alleles, weight and sex were the most significant covariates explaining 55% of inter-individual variability in EFV clearance. efavirenz 145-148 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 9-15 25321623-10 2015 In the EFV/FTC/TDF group, virus from 14 patients (4.0%; 14/352 treated patients; 4 during weeks 96-144) developed a resistance substitution to EFV (n=14; K103N: n=13), FTC (M184V/I: n=4) or TDF (K65R: n=3). efavirenz 7-10 sex determining region Y Homo sapiens 190-193 26699137-8 2015 RESULTS: A 48 hours exposure of human erythrocytes to efavirenz (>= 2 microg/ml) significantly increased the percentage of annexin-V-binding cells, significantly decreased forward scatter (2 microg/ml), significantly increased Fluo3-fluorescence (>= 2 microg/ml), but did not significantly modify DCFDA fluorescence or ceramide abundance. efavirenz 54-63 annexin A5 Homo sapiens 126-135 26699137-9 2015 The effect of efavirenz on annexin-V-binding was significantly blunted, but not abolished by removal of extracellular Ca2+. efavirenz 14-23 annexin A5 Homo sapiens 27-36 26699137-10 2015 The effect of efavirenz on annexin-V-binding was further significantly blunted by p38 kinase inhibitor SB203580 (2 microM) and casein kinase 1alpha inhibitor D4476 (10 microM), but not by cyclooxygenase inhibitor aspirin (50 microM). efavirenz 14-23 annexin A5 Homo sapiens 27-36 25625582-7 2015 Furthermore, EFV resulted in increased formation of peroxynitrite and oxidation of mitochondrial protein thiols, including cyclophilin D (CypD). efavirenz 13-16 peptidylprolyl isomerase F (cyclophilin F) Mus musculus 123-136 25625582-7 2015 Furthermore, EFV resulted in increased formation of peroxynitrite and oxidation of mitochondrial protein thiols, including cyclophilin D (CypD). efavirenz 13-16 peptidylprolyl isomerase F (cyclophilin F) Mus musculus 138-142 25625582-10 2015 Finally, EFV increased the NADH/NAD(+) ratio, inhibited Sirt3 activity, and led to hyperacetylated lysine residues, including those in CypD. efavirenz 9-12 sirtuin 3 Mus musculus 56-61 25625582-10 2015 Finally, EFV increased the NADH/NAD(+) ratio, inhibited Sirt3 activity, and led to hyperacetylated lysine residues, including those in CypD. efavirenz 9-12 peptidylprolyl isomerase F (cyclophilin F) Mus musculus 135-139 25625582-11 2015 However, hepatocytes isolated from Sirt3-null mice were protected against 40microM EFV as compared to their wild-type controls. efavirenz 83-86 sirtuin 3 Mus musculus 35-40 25096076-7 2014 Efavirenz treatment in arm 1 resulted in 1.74 (relative standard error = 15%), 3.3 (relative standard error = 33.1%) and 4.0 (relative standard error = 37.1%) average fold induction of CYP3A for extensive (CYP2B6*1/*1), intermediate (CYP2B6*1/*6) and slow (CYP2B6*6/*6) efavirenz metabolizers, respectively. efavirenz 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 185-190 25096076-7 2014 Efavirenz treatment in arm 1 resulted in 1.74 (relative standard error = 15%), 3.3 (relative standard error = 33.1%) and 4.0 (relative standard error = 37.1%) average fold induction of CYP3A for extensive (CYP2B6*1/*1), intermediate (CYP2B6*1/*6) and slow (CYP2B6*6/*6) efavirenz metabolizers, respectively. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 206-212 25096076-7 2014 Efavirenz treatment in arm 1 resulted in 1.74 (relative standard error = 15%), 3.3 (relative standard error = 33.1%) and 4.0 (relative standard error = 37.1%) average fold induction of CYP3A for extensive (CYP2B6*1/*1), intermediate (CYP2B6*1/*6) and slow (CYP2B6*6/*6) efavirenz metabolizers, respectively. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 234-240 25096076-7 2014 Efavirenz treatment in arm 1 resulted in 1.74 (relative standard error = 15%), 3.3 (relative standard error = 33.1%) and 4.0 (relative standard error = 37.1%) average fold induction of CYP3A for extensive (CYP2B6*1/*1), intermediate (CYP2B6*1/*6) and slow (CYP2B6*6/*6) efavirenz metabolizers, respectively. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 234-240 25096076-10 2014 CONCLUSIONS: Our results indicate that efavirenz induction of CYP3A is influenced by CYP2B6 genetic polymorphisms and that efavirenz/rifampicin co-treatment results in higher induction than efavirenz alone. efavirenz 39-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-67 25096076-10 2014 CONCLUSIONS: Our results indicate that efavirenz induction of CYP3A is influenced by CYP2B6 genetic polymorphisms and that efavirenz/rifampicin co-treatment results in higher induction than efavirenz alone. efavirenz 39-48 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 85-91 25355844-4 2014 Patients received 600 mg efavirenz daily with the possibility of a dose increase in case of PSA progression. efavirenz 25-34 kallikrein related peptidase 3 Homo sapiens 92-95 25355844-7 2014 The exploratory analysis revealed that for the 7 patients in whom optimal plasma concentration of efavirenz was achieved, PSA progression was observed in only 28.6% compared with 81.8% of patients with suboptimal plasma concentrations of efavirenz. efavirenz 98-107 kallikrein related peptidase 3 Homo sapiens 122-125 25394049-8 2014 Whilst CSF efavirenz concentration was significantly associated with plasma concentration (P<0.001) and CYP2B6 genotype (CSF efavirenz GG to GT/TT GM ratio 0.56, 90% CI 0.42-0.74), CSF 8OH-efavirenz concentration was not (P=0.242 for association with plasma concentration and CSF 8OH-efavirenz GG to GT/TT GM ratio 1.52, 90% CI 0.97-2.36). efavirenz 11-20 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 107-113 25433665-9 2014 The mean changes from baseline in CD4 count were similar in both rilpivirine and efavirenz (RR, 1.05; 95% CI, 0.85-1.24). efavirenz 81-90 CD4 molecule Homo sapiens 34-37 24820076-0 2014 Isoniazid mediates the CYP2B6*6 genotype-dependent interaction between efavirenz and antituberculosis drug therapy through mechanism-based inactivation of CYP2A6. efavirenz 71-80 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 23-29 25309681-1 2014 Cytochrome P450 2B6 (CYP2B6) is primarily responsible for the metabolism of the anti-HIV drug efavirenz (EFV). efavirenz 105-108 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-19 25309681-1 2014 Cytochrome P450 2B6 (CYP2B6) is primarily responsible for the metabolism of the anti-HIV drug efavirenz (EFV). efavirenz 105-108 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 21-27 25309681-2 2014 We set out to explore the molecular basis for CYP2B6 activity toward EFV by examining the metabolism of eight EFV analogues. efavirenz 69-72 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 25309681-4 2014 Subsequent substrate depletion analysis of EFV and EFV analogues found to be CYP2B6 substrates revealed further differences between these CYP2B6 substrates. efavirenz 43-46 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 77-83 25309681-4 2014 Subsequent substrate depletion analysis of EFV and EFV analogues found to be CYP2B6 substrates revealed further differences between these CYP2B6 substrates. efavirenz 43-46 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 138-144 25309681-4 2014 Subsequent substrate depletion analysis of EFV and EFV analogues found to be CYP2B6 substrates revealed further differences between these CYP2B6 substrates. efavirenz 51-54 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 77-83 25309681-4 2014 Subsequent substrate depletion analysis of EFV and EFV analogues found to be CYP2B6 substrates revealed further differences between these CYP2B6 substrates. efavirenz 51-54 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 138-144 24820106-7 2014 MtDNA and cytochrome oxidase subunit II did not change, and cytochrome b increased significantly in EFV-treated patients. efavirenz 100-103 mitochondrially encoded cytochrome b Homo sapiens 60-72 24729492-9 2014 Fewer (P < .001) RPV-treated patients than EFV-treated patients had TC, LDL-C, and triglyceride levels above National Cholesterol Education Program cutoffs. efavirenz 46-49 component of oligomeric golgi complex 2 Homo sapiens 75-80 24846165-3 2014 Treatments of HIV patients with CML are with HAART drugs, ritonavir and efavirenz, may cause complex drug interactions through CYP3A inhibition or induction. efavirenz 72-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-132 24820076-0 2014 Isoniazid mediates the CYP2B6*6 genotype-dependent interaction between efavirenz and antituberculosis drug therapy through mechanism-based inactivation of CYP2A6. efavirenz 71-80 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 155-161 24164392-7 2014 Patients receiving efavirenz had higher levels of L-FABP/creatinine in comparison to healthy controls (p=0.0039). efavirenz 19-28 fatty acid binding protein 1 Homo sapiens 50-56 24956253-2 2014 The aim of this study was to evaluate the clinical and economic impact of efavirenz (EFV) dose adjustment by monitoring plasma concentrations and pharmacogenetic analysis of the 516G>T CYP2B6 polymorphism. efavirenz 74-83 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 188-194 24956253-2 2014 The aim of this study was to evaluate the clinical and economic impact of efavirenz (EFV) dose adjustment by monitoring plasma concentrations and pharmacogenetic analysis of the 516G>T CYP2B6 polymorphism. efavirenz 85-88 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 188-194 24474568-12 2014 Efavirenz, a potent inducer of CYP3A4, resulted in increased exposure of N-desethyl sunitinib, whereas ritonavir caused decreased exposure of the metabolite. efavirenz 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 24488374-15 2014 The CYP3A4 inducers efavirenz and dexamethasone did not have a significant effect on docetaxel exposure (AUC). efavirenz 20-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-10 24352658-3 2014 We found that four pharmaceuticals (efavirenz (EFV), acetaminophen, mirtazapine, and galantamine) prescribed for indications unrelated to cholesterol maintenance increased CYP46A1 activity in vitro. efavirenz 36-45 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 172-179 24390631-6 2014 Ethnic differences and the associated prevalence of CYP2B6 polymorphisms result in significant differences in the PKPD associated with a standard 600 mg per day dose of EFV, warranting dosage reduction in carriers of specific CYP2B6 polymorphisms. efavirenz 169-172 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 52-58 24390631-6 2014 Ethnic differences and the associated prevalence of CYP2B6 polymorphisms result in significant differences in the PKPD associated with a standard 600 mg per day dose of EFV, warranting dosage reduction in carriers of specific CYP2B6 polymorphisms. efavirenz 169-172 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 226-232 24275118-0 2014 Efavirenz induces interactions between leucocytes and endothelium through the activation of Mac-1 and gp150,95. efavirenz 0-9 integrin subunit alpha M Homo sapiens 92-97 24275118-0 2014 Efavirenz induces interactions between leucocytes and endothelium through the activation of Mac-1 and gp150,95. efavirenz 0-9 integrin subunit beta 4 Homo sapiens 102-110 24275118-7 2014 Efavirenz, but not nevirapine, augmented the levels of CD11b, CD11c and CD18 in neutrophils and monocytes. efavirenz 0-9 integrin subunit alpha M Homo sapiens 55-60 24275118-7 2014 Efavirenz, but not nevirapine, augmented the levels of CD11b, CD11c and CD18 in neutrophils and monocytes. efavirenz 0-9 integrin subunit alpha X Homo sapiens 62-67 24275118-7 2014 Efavirenz, but not nevirapine, augmented the levels of CD11b, CD11c and CD18 in neutrophils and monocytes. efavirenz 0-9 integrin subunit beta 2 Homo sapiens 72-76 24759994-3 2014 Treatment with EFV or the EFV containing regimen generated significantly increased soluble amyloid beta (Abeta), and promoted increased beta-secretase-1 (BACE-1) expression while 3TC, AZT, or, vehicle control did not significantly alter these endpoints. efavirenz 15-18 beta-site APP cleaving enzyme 1 Mus musculus 136-152 24759994-3 2014 Treatment with EFV or the EFV containing regimen generated significantly increased soluble amyloid beta (Abeta), and promoted increased beta-secretase-1 (BACE-1) expression while 3TC, AZT, or, vehicle control did not significantly alter these endpoints. efavirenz 15-18 beta-site APP cleaving enzyme 1 Mus musculus 154-160 24759994-3 2014 Treatment with EFV or the EFV containing regimen generated significantly increased soluble amyloid beta (Abeta), and promoted increased beta-secretase-1 (BACE-1) expression while 3TC, AZT, or, vehicle control did not significantly alter these endpoints. efavirenz 26-29 beta-site APP cleaving enzyme 1 Mus musculus 136-152 24759994-3 2014 Treatment with EFV or the EFV containing regimen generated significantly increased soluble amyloid beta (Abeta), and promoted increased beta-secretase-1 (BACE-1) expression while 3TC, AZT, or, vehicle control did not significantly alter these endpoints. efavirenz 26-29 beta-site APP cleaving enzyme 1 Mus musculus 154-160 24759994-6 2014 EFV or the EFV containing regimen promoted significantly more BACE-1 expression and soluble Abeta generation while 3TC, AZT, or vehicle control did not. efavirenz 0-3 beta-site APP cleaving enzyme 1 Mus musculus 62-68 24759994-6 2014 EFV or the EFV containing regimen promoted significantly more BACE-1 expression and soluble Abeta generation while 3TC, AZT, or vehicle control did not. efavirenz 11-14 beta-site APP cleaving enzyme 1 Mus musculus 62-68 23629159-0 2014 Efavirenz-mediated induction of omeprazole metabolism is CYP2C19 genotype dependent. efavirenz 0-9 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 57-64 23629159-2 2014 We hypothesized that CYP2C19 and CYP2B6 genetic polymorphisms influence the extent of induction of omeprazole metabolism by efavirenz. efavirenz 124-133 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 21-28 23629159-2 2014 We hypothesized that CYP2C19 and CYP2B6 genetic polymorphisms influence the extent of induction of omeprazole metabolism by efavirenz. efavirenz 124-133 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 33-39 24589015-11 2014 IP-10 and MIG levels declined significantly less strongly with ATV/r than with EFV (IP-10Delta -57%, p = 0.011; MIGDelta -136%, p = 0.007), while no difference was noted between LPV/r and EFV. efavirenz 79-82 C-X-C motif chemokine ligand 10 Homo sapiens 0-5 24589015-11 2014 IP-10 and MIG levels declined significantly less strongly with ATV/r than with EFV (IP-10Delta -57%, p = 0.011; MIGDelta -136%, p = 0.007), while no difference was noted between LPV/r and EFV. efavirenz 79-82 C-X-C motif chemokine ligand 9 Homo sapiens 10-13 24352658-3 2014 We found that four pharmaceuticals (efavirenz (EFV), acetaminophen, mirtazapine, and galantamine) prescribed for indications unrelated to cholesterol maintenance increased CYP46A1 activity in vitro. efavirenz 47-50 cytochrome P450, family 46, subfamily a, polypeptide 1 Mus musculus 172-179 24316028-1 2014 Efavirenz (EFV) exhibits interindividual pharmacokinetic variability caused by differences in cytochrome P450 (CYP) expression. efavirenz 0-9 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 94-109 24316028-1 2014 Efavirenz (EFV) exhibits interindividual pharmacokinetic variability caused by differences in cytochrome P450 (CYP) expression. efavirenz 0-9 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 111-114 24316028-3 2014 We investigated in patients co-infected with human immunodeficiency virus (HIV) and TB recruited in Rwanda the effects of 10 SNPs in five drug-metabolizing enzymes on EFV plasma levels and treatment response when patients are treated with EFV-containing therapy alone (n=28) and when combined with rifampicin-based TB treatment (n=62), and the validity of genotyping for CYP2B6 single nucleotide polymorphisms in predicting supra-therapeutic EFV levels. efavirenz 239-242 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 371-377 24316028-3 2014 We investigated in patients co-infected with human immunodeficiency virus (HIV) and TB recruited in Rwanda the effects of 10 SNPs in five drug-metabolizing enzymes on EFV plasma levels and treatment response when patients are treated with EFV-containing therapy alone (n=28) and when combined with rifampicin-based TB treatment (n=62), and the validity of genotyping for CYP2B6 single nucleotide polymorphisms in predicting supra-therapeutic EFV levels. efavirenz 239-242 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 371-377 24316028-4 2014 There was a significant difference between CYP1A2 -739T/G and T/T genotypes when patients were treated with EFV-containing therapy combined with rifampicin-based TB treatment, but not when EFV-containing therapy was alone. efavirenz 108-111 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 43-49 24316028-6 2014 Predictive factors of EFV plasma levels in the presence of rifampicin-based TB treatment were CYP2A6 1093G>A, CYP2B6 516G>T, and CYP2B6 983T>C accounting for 27%, 43%, and 29% of the total variance in EFV levels, respectively. efavirenz 22-25 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 94-100 24316028-6 2014 Predictive factors of EFV plasma levels in the presence of rifampicin-based TB treatment were CYP2A6 1093G>A, CYP2B6 516G>T, and CYP2B6 983T>C accounting for 27%, 43%, and 29% of the total variance in EFV levels, respectively. efavirenz 22-25 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 113-119 24316028-6 2014 Predictive factors of EFV plasma levels in the presence of rifampicin-based TB treatment were CYP2A6 1093G>A, CYP2B6 516G>T, and CYP2B6 983T>C accounting for 27%, 43%, and 29% of the total variance in EFV levels, respectively. efavirenz 22-25 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 135-141 24316028-7 2014 There was a high positive predictive value (PPV) (100%) for CYP2B6 516T/T and 983T/T genotypes in predicting EFV plasma levels above the therapeutic range, but this PPV decreased in the presence of rifampicin-based TB treatment. efavirenz 109-112 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 60-66 23990572-0 2014 Dependence of efavirenz- and rifampicin-isoniazid-based antituberculosis treatment drug-drug interaction on CYP2B6 and NAT2 genetic polymorphisms: ANRS 12154 study in Cambodia. efavirenz 14-23 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 108-114 23990572-0 2014 Dependence of efavirenz- and rifampicin-isoniazid-based antituberculosis treatment drug-drug interaction on CYP2B6 and NAT2 genetic polymorphisms: ANRS 12154 study in Cambodia. efavirenz 14-23 N-acetyltransferase 2 Homo sapiens 119-123 24497997-8 2014 RESULTS: EFV apparent clearance (CL/F) was 2.2 and 1.74 fold higher in CYP2B6*6 (*1/*1) and CYP2B6*6 (*1/*6) compared CYP2B6*6 (*6/*6) carriers, while a 22% increase in F1 was observed for carriers of ABCB1 c.4046A>G variant allele. efavirenz 9-12 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 71-77 24497997-8 2014 RESULTS: EFV apparent clearance (CL/F) was 2.2 and 1.74 fold higher in CYP2B6*6 (*1/*1) and CYP2B6*6 (*1/*6) compared CYP2B6*6 (*6/*6) carriers, while a 22% increase in F1 was observed for carriers of ABCB1 c.4046A>G variant allele. efavirenz 9-12 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 92-98 24497997-8 2014 RESULTS: EFV apparent clearance (CL/F) was 2.2 and 1.74 fold higher in CYP2B6*6 (*1/*1) and CYP2B6*6 (*1/*6) compared CYP2B6*6 (*6/*6) carriers, while a 22% increase in F1 was observed for carriers of ABCB1 c.4046A>G variant allele. efavirenz 9-12 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 92-98 24497997-8 2014 RESULTS: EFV apparent clearance (CL/F) was 2.2 and 1.74 fold higher in CYP2B6*6 (*1/*1) and CYP2B6*6 (*1/*6) compared CYP2B6*6 (*6/*6) carriers, while a 22% increase in F1 was observed for carriers of ABCB1 c.4046A>G variant allele. efavirenz 9-12 ATP binding cassette subfamily B member 1 Homo sapiens 201-206 24268674-2 2014 Efavirenz, neviparine, darunavir and atazanavir increased nitric oxide (NO) production in microglial cells activated with Gp120CN54 and interferon-gamma. efavirenz 0-9 interferon gamma Rattus norvegicus 136-152 24142869-8 2014 The final model included only CYP2B6 genotype as a covariate that predicts EFV clearance through the formation of 8-OH EFV that represented 65% to 80% of EFV clearance. efavirenz 75-78 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 30-36 24142869-8 2014 The final model included only CYP2B6 genotype as a covariate that predicts EFV clearance through the formation of 8-OH EFV that represented 65% to 80% of EFV clearance. efavirenz 119-122 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 30-36 24142869-9 2014 The total clearance of EFV in CYP2B6*6/*6 genotype was ~30% lower than CYP2B6*1/*1 or CYP2B6*1/*6 alleles (P < .001). efavirenz 23-26 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 30-36 24091996-5 2013 In contrast, the primary metabolite of efavirenz, 8-hydroxy-efavirenz, stimulated the glycolytic flux in viable astrocytes in a time- and concentration-dependent manner with half-maximal and maximal effects at concentrations of 5 and 10 muM, respectively. efavirenz 39-48 latexin Homo sapiens 237-240 23836171-8 2013 Amprenavir, atazanavir, darunavir, efavirenz, ritonavir, and lopinavir were found to activate hPXR, whereas abacavir, efavirenz, and nevirapine were found to activate hCAR. efavirenz 35-44 nuclear receptor subfamily 1 group I member 2 Homo sapiens 94-98 23836171-8 2013 Amprenavir, atazanavir, darunavir, efavirenz, ritonavir, and lopinavir were found to activate hPXR, whereas abacavir, efavirenz, and nevirapine were found to activate hCAR. efavirenz 35-44 CXADR Ig-like cell adhesion molecule Homo sapiens 167-171 23836171-8 2013 Amprenavir, atazanavir, darunavir, efavirenz, ritonavir, and lopinavir were found to activate hPXR, whereas abacavir, efavirenz, and nevirapine were found to activate hCAR. efavirenz 118-127 CXADR Ig-like cell adhesion molecule Homo sapiens 167-171 24372550-5 2014 KEY RESULTS: Direct LBD interactions with LXRalpha and/or LXRbeta were predicted in silico and confirmed in vitro for darunavir, efavirenz, flavopiridol, maraviroc and tipranavir. efavirenz 129-138 nuclear receptor subfamily 1 group H member 3 Homo sapiens 42-50 24372550-5 2014 KEY RESULTS: Direct LBD interactions with LXRalpha and/or LXRbeta were predicted in silico and confirmed in vitro for darunavir, efavirenz, flavopiridol, maraviroc and tipranavir. efavirenz 129-138 nuclear receptor subfamily 1 group H member 2 Homo sapiens 58-65 23846872-3 2013 Efavirenz clearance was predictable using in vitro data for carriers of the CYP2B6*1/*1 genotype, but the prediction in carriers of the CYP2B6*6 allele was poor. efavirenz 0-9 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 76-82 24521642-9 2013 Logistic regression analysis showed CYP2B6 516G>T polymorphism significantly associated with virologic outcome in patients receiving EFV-based regimen. efavirenz 136-139 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 36-42 24334181-1 2013 BACKGROUND: ACTG A5202 randomized treatment-naive individuals to tenofovir-emtricitabine (TDF/FTC) or abacavir-lamivudine (ABC/3TC) combined with efavirenz (EFV) or atazanavir/ritonavir (ATV/r). efavirenz 146-155 actin gamma 1 Homo sapiens 12-16 24334181-1 2013 BACKGROUND: ACTG A5202 randomized treatment-naive individuals to tenofovir-emtricitabine (TDF/FTC) or abacavir-lamivudine (ABC/3TC) combined with efavirenz (EFV) or atazanavir/ritonavir (ATV/r). efavirenz 157-160 actin gamma 1 Homo sapiens 12-16 23937548-1 2013 The fixed-dose combination efavirenz, emtricitabine, and tenofovir (EFV/FTC/TDF) is a first-line agent for the treatment of HIV. efavirenz 27-36 sex determining region Y Homo sapiens 76-79 23612009-8 2013 Furthermore, the effect of EFV on the phosphorylation state of the growth factors Erk, Akt and the tumour suppressor protein p53 was tested. efavirenz 27-30 mitogen-activated protein kinase 1 Homo sapiens 82-85 23612009-14 2013 Furthermore, EFV led to an activating phosphorylation of the tumour suppressor protein p53 going in line with earlier reports that EFV may be antitumourigenic and a potential cytostatic drug. efavirenz 13-16 tumor protein p53 Homo sapiens 87-90 23612009-14 2013 Furthermore, EFV led to an activating phosphorylation of the tumour suppressor protein p53 going in line with earlier reports that EFV may be antitumourigenic and a potential cytostatic drug. efavirenz 131-134 tumor protein p53 Homo sapiens 87-90