ArticleDrug metabolism and pharmacokinetics2013
In vitro analysis and quantitative prediction of efavirenz inhibition of eight cytochrome P450 (CYP) enzymes: major effects on CYPs 2B6, 2C8, 2C9 and 2C19.
Article in Drug metabolism and pharmacokinetics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 54 citations in OpenAlex.
- A Population Pharmacokinetic Approach to Understand the Effect of Efavirenz on CYP3A Activity in Healthy Volunteers Using Midazolam as a Probe.CPT: pharmacometrics & systems pharmacology · 2025Trial
- CYP2B6 Genotype-Dependent Inhibition of CYP1A2 and Induction of CYP2A6 by the Antiretroviral Drug Efavirenz in Healthy Volunteers.Clinical and translational science · 2019Trial
- Predicting Efavirenz Concentrations in the Brain Tissue of HIV-Infected Individuals and Exploring their Relationship to Neurocognitive Impairment.Clinical and translational science · 2019Trial
- Effect of Antiretroviral Therapy on Plasma Concentrations of Chloroquine and Desethyl-chloroquine.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2018Trial
- Efavirenz and CYP2C9 Genetic Polymorphisms Reduce CYP2C9 Activity in Healthy Participants.Clinical and translational science · 2026Article
- A Physiologically-Based Pharmacokinetic Simulation to Evaluate Approaches to Mitigate Efavirenz-Induced Decrease in Levonorgestrel Exposure with a Contraceptive Implant.Pharmaceutics · 2024Article
- Antivirals for prevention of hepatitis B virus mother-to-child transmission in human immunodeficiency virus positive pregnant women co-infected with hepatitis B virus.The Cochrane database of systematic reviews · 2023Review
- Combined Oral Contraceptives As Victims of Drug Interactions.Drug metabolism and disposition: the biological fate of chemicals · 2023Review
- Article
- Clinically relevant enantiomer specific R- and S-praziquantel pharmacokinetic drug-drug interactions with efavirenz and ritonavir.Pharmacology research & perspectives · 2021Article
- HIV Associated Neurocognitive Disorders Subsidence Through Citalopram Addition in Anti-retroviral Therapy (HANDS-CARE): A Concept Note.Frontiers in neurology · 2021Article
- Physiologically Based Pharmacokinetic Modeling to Predict Drug-Drug Interactions with Efavirenz Involving Simultaneous Inducing and Inhibitory Effects on Cytochromes.Clinical pharmacokinetics · 2017Article
- Neurotoxicity in the Post-HAART Era: Caution for the Antiretroviral Therapeutics.Neurotoxicity research · 2016Review
- Insights into CYP2B6-mediated drug-drug interactions.Acta pharmaceutica Sinica. B · 2016Review
- Towards a Best Practice Approach in PBPK Modeling: Case Example of Developing a Unified Efavirenz Model Accounting for Induction of CYPs 3A4 and 2B6.CPT: pharmacometrics & systems pharmacology · 2016Article
- Kinetics of cytochrome P450 enzymes for metabolism of sodium tanshinone IIA sulfonate in vitro.Chinese medicine · 2016Article
- Human hepatocyte assessment of imatinib drug-drug interactions - complexities in clinical translation.British journal of clinical pharmacology · 2015Article
- PharmGKB summary: Efavirenz pathway, pharmacokinetics.Pharmacogenetics and genomics · 2015Review
- A pharmacist's guide to the 2012 update of the Canadian Cardiovascular Society Guidelines for the Use of Antiplatelet Therapy.Canadian pharmacists journal : CPJ = Revue des pharmaciens du Canada : RPC · 2015Article
- Managing drug interactions in HIV-infected adults with comorbid illness.CMAJ : Canadian Medical Association journal = journal de l'Association medicale canadienne · 2015Review
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
Abstract
In order to quantitatively predict drug interactions associated with efavirenz-based anti-HIV therapy, we evaluated reversible and time-dependent inhibitions of efavirenz on eight cytochrome P450 (CYP) enzymes in vitro. The present study showed that efavirenz was a potent competitive inhibitor of CYP2B6 (average K(i) = 1.68 µM in HLMs and K(i) = 1.38 µM in expressed CYP2B6) and CYP2C8 (K(i) = 4.78 µM in pooled HLMs and K(i) = 4.80 µM in HLMs with CYP2C8*3/*3 genotype). Efavirenz was a moderate inhibitor of CYP2C9 (K(i) = 19.46 µM) and CYP2C19 (K(i) = 21.31 µM); and a weak inhibitor of CYP3A (K(i) = 40.33 µM). No appreciable inhibition was observed on CYP1A2, CYP2A6 or CYP2D6. No time-dependent inhibition of the CYPs by efavirenz was observed in this study. Quantitative predictions showed that single dose of efavirenz may substantially slow the elimination of drugs predominantly cleared by CYP2B6, CYP2C19 or by both enzymes and may also lower the area under the plasma concentration time curve (AUC) of active metabolites of some pro-drugs (e.g., clopidogrel and proguanil) by up to 30%. Depending on substrates, chronic administration of efavirenz may increase the AUC of CYP2C8 and CYP2C9 substrates about 3.5-4.4-fold and 1.7-2.0-fold at steady state.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.