PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 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 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 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 34945777-11 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 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 181-190 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 30-36 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 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 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 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 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 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 14-20 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 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 35235559-1 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 32829410-10 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 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 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 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 32451120-9 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 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 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 31628422-6 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 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 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 31324697-0 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 B member 6 Homo sapiens 30-36 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 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 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 2 subfamily B member 6 Homo sapiens 85-91 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 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 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 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 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 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 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 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 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 24316028-6 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 102-105 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 157-163 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 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 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 16267764-9 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 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 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 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 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 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 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