Efavirenz and the CNS: what we already know and questions that need to be answered

N Apostolova, HA Funes, A Blas-Garcia… - Journal of …, 2015 - academic.oup.com
The NNRTI efavirenz has long been one of the most frequently employed antiretroviral drugs
in the multidrug regimens used to treat HIV infection, in accordance with its well …

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 …

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 …

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 …

CYP2B6, CYP2A6 and UGT2B7 genetic polymorphisms are predictors of efavirenz mid-dose concentration in HIV-infected patients

A Kwara, M Lartey, KWC Sagoe, E Kenu - Aids, 2009 - journals.lww.com
Objective: UDP-glucuronosyltransferase (UGT) 2B7 was recently identified as the main
enzyme mediating efavirenz N-glucuronidation. In this study, we determined whether …

Cytochrome P450 2B6 (CYP2B6) and constitutive androstane receptor (CAR) polymorphisms are associated with early discontinuation of efavirenz-containing …

C Wyen, H Hendra, M Siccardi, M Platten… - Journal of …, 2011 - academic.oup.com
Abstract Objectives Cytochrome P450 2B6 (CYP2B6) is responsible for the metabolic
clearance of efavirenz and single nucleotide polymorphisms (SNPs) in the CYP2B6 gene …

CYP2A6: genetics, structure, regulation, and function

H Raunio, M Rahnasto-Rilla - Drug metabolism and drug …, 2012 - degruyter.com
The human CYP2A gene subfamily consists of three members, CYP2A6, CYP2A7, and
CYP2A13. The CYP2A6 gene is highly polymorphic with approximately 40 annotated allelic …

Pharmacokinetic and pharmacodynamic comparison of once‐daily efavirenz (400 mg vs. 600 mg) in treatment‐naive HIV‐infected patients: results of the ENCORE1 …

L Dickinson, J Amin, L Else, M Boffito… - Clinical …, 2015 - Wiley Online Library
Daily efavirenz 400 mg (EFV400) was virologically noninferior to 600 mg (EFV600) at 48
weeks in treatment‐naïve patients. We evaluated EFV400 and EFV600 pharmacokinetics …

Liver autophagy in anorexia nervosa and acute liver injury

M Kheloufi, CM Boulanger, F Durand… - BioMed research …, 2014 - Wiley Online Library
Autophagy, a lysosomal catabolic pathway for long‐lived proteins and damaged organelles,
is crucial for cell homeostasis, and survival under stressful conditions. During starvation …

[PDF][PDF] Compromising mitochondrial function with the antiretroviral drug efavirenz induces cell survival‐promoting autophagy

N Apostolova, LJ Gomez‐Sucerquia, A Gortat… - …, 2011 - Wiley Online Library
Hepatotoxicity is a very common side effect associated with the pharmacological treatment
of human immunodeficiency virus (HIV) infection and its pathogenesis is poorly understood …