[HTML][HTML] Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation
UM Zanger, M Schwab - Pharmacology & therapeutics, 2013 - Elsevier
Cytochromes P450 (CYP) are a major source of variability in drug pharmacokinetics and
response. Of 57 putatively functional human CYPs only about a dozen enzymes, belonging …
response. Of 57 putatively functional human CYPs only about a dozen enzymes, belonging …
[HTML][HTML] HIV-1 and human genetic variation
PJ McLaren, J Fellay - Nature Reviews Genetics, 2021 - nature.com
Over the past four decades, research on the natural history of HIV infection has described
how HIV wreaks havoc on human immunity and causes AIDS. HIV host genomic research …
how HIV wreaks havoc on human immunity and causes AIDS. HIV host genomic research …
Cohort profile: the Swiss HIV Cohort study
Swiss HIV Cohort Study… - International journal …, 2010 - academic.oup.com
The Swiss HIV Cohort study (SHCS) was established in 1988. It is an ongoing multicentre,
prospective observational study for interdisciplinary human immunodeficiency virus (HIV) …
prospective observational study for interdisciplinary human immunodeficiency virus (HIV) …
[HTML][HTML] Efavirenz: history, development and future
B Costa, N Vale - Biomolecules, 2022 - mdpi.com
Efavirenz (Sustiva®) is a first-generation non-nucleoside reverse transcriptase inhibitor
(NNRTI) used to treat human immunodeficiency virus (HIV) type 1 infection or to prevent the …
(NNRTI) used to treat human immunodeficiency virus (HIV) type 1 infection or to prevent the …
Genome-wide association study of plasma efavirenz pharmacokinetics in AIDS Clinical Trials Group protocols implicates several CYP2B6 variants
ER Holzinger, B Grady, MD Ritchie… - Pharmacogenetics …, 2012 - journals.lww.com
Objectives Prior candidate gene studies have associated CYP2B6 516G→ T [rs3745274]
and 983T→ C [rs28399499] with increased plasma efavirenz exposure. We sought to …
and 983T→ C [rs28399499] with increased plasma efavirenz exposure. We sought to …
Efavirenz in the therapy of HIV infection
NY Rakhmanina, JN Van den Anker - Expert opinion on drug …, 2010 - Taylor & Francis
Importance of the field: The use of the first generation non-nucleoside reverse transcriptase
inhibitor efavirenz (EFV) as a component of first-line antiretroviral therapy has been …
inhibitor efavirenz (EFV) as a component of first-line antiretroviral therapy has been …
Efavirenz primary and secondary metabolism in vitro and in vivo: identification of novel metabolic pathways and cytochrome P450 2A6 as the principal catalyst of …
ET Ogburn, DR Jones, AR Masters, C Xu, Y Guo… - Drug Metabolism and …, 2010 - ASPET
Efavirenz primary and secondary metabolism was investigated in vitro and in vivo. In human
liver microsome (HLM) samples, 7-and 8-hydroxyefavirenz accounted for 22.5 and 77.5% of …
liver microsome (HLM) samples, 7-and 8-hydroxyefavirenz accounted for 22.5 and 77.5% of …
In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function
J di Iulio, A Fayet, M Arab-Alameddine… - Pharmacogenetics …, 2009 - journals.lww.com
Methods This study characterized CYP2A6 variation (14 alleles) in individuals (N= 169)
previously characterized for functional variants in CYP2B6 (18 alleles). Plasma …
previously characterized for functional variants in CYP2B6 (18 alleles). Plasma …
Glucuronidation of the antiretroviral drug efavirenz by UGT2B7 and an in vitro investigation of drug-drug interaction with zidovudine
AS Bélanger, P Caron, M Harvey, PA Zimmerman… - Drug Metabolism and …, 2009 - ASPET
The non-nucleoside reverse transcriptase inhibitor efavirenz (EFV) is directly conjugated by
the UDP-glucuronosyltransferase (UGT) pathway to form EFV-N-glucuronide (EFV-G), but …
the UDP-glucuronosyltransferase (UGT) pathway to form EFV-N-glucuronide (EFV-G), but …
CYP2B6, CYP2A6 and UGT2B7 genetic polymorphisms are predictors of efavirenz mid-dose concentration in HIV-infected patients
Objective: UDP-glucuronosyltransferase (UGT) 2B7 was recently identified as the main
enzyme mediating efavirenz N-glucuronidation. In this study, we determined whether …
enzyme mediating efavirenz N-glucuronidation. In this study, we determined whether …