PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 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 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 20201776-10 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 15496645-7 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 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 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 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 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 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 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 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 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 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 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 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 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 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 3 subfamily A member 4 Homo sapiens 106-112 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 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 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 25096076-10 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 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 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 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 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 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 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 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 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 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