Trial reportJournal of cardiovascular electrophysiology2016
Efavirenz Inhibits the Human Ether-A-Go-Go Related Current (hERG) and Induces QT Interval Prolongation in CYP2B6*6*6 Allele Carriers.
Trial report in Journal of cardiovascular electrophysiology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers, 5 of them syntheses that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
23 citing papers in PubMed, 5 syntheses or guidelines pooled it, 47 citations in OpenAlex.
- The prevalence of adverse drug reactions to antiretroviral therapy and associated factors among pediatric patients living with HIV in sub-Saharan African countries: a systematic review and meta-analysis.BMC infectious diseases · 2025Pooled it
- Antiretroviral Postexposure Prophylaxis After Sexual, Injection Drug Use, or Other Nonoccupational Exposure to HIV - CDC Recommendations, United States, 2025.MMWR. Recommendations and reports : Morbidity and mortality weekly report. Recommendations and reports · 2025Guideline
- Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2B6 and Efavirenz-Containing Antiretroviral Therapy.Clinical pharmacology and therapeutics · 2019Guideline
- Pooled it
- Pharmacogenomic markers associated with drug-induced QT prolongation: a systematic review.PharmacogenomicsPooled it
- De novo electrocardiographic abnormalities in persons living with HIV.Scientific reports · 2021Trial
- Efavirenz Pharmacogenetics and Weight Gain Following Switch to Integrase Inhibitor-Containing Regimens.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2021Trial
- CYP2B6 Genotype-Dependent Inhibition of CYP1A2 and Induction of CYP2A6 by the Antiretroviral Drug Efavirenz in Healthy Volunteers.Clinical and translational science · 2019Trial
- Pharmacogenomics of antibacterial and antiviral therapies: Clinical actionability, evidence gaps, and future directions.Pharmacological reviews · 2026Review
- Combined antiretroviral therapy with low- or normal-protein, high-calorie diets appears to induce significant deleterious electrocardiographic changes in a rodent model.Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas · 2026Article
- Antiretroviral therapy and associated drug interactions with cardiovascular drugs: a critical review.Frontiers in pharmacology · 2025Review
- An update on drug-drug interactions in older adults living with human immunodeficiency virus (HIV).Expert review of clinical pharmacology · 2024Review
- An overview of genetic variants regarding efavirenz-related dysthymias in HIV-infected patients: Response to a letter to the editor.Clinical cardiology · 2022Article
- Frequency of CYP2B6 Alleles in Major Iranian Ethnicities, Affecting Response to Efavirenz.Genetics research · 2022Article
- Efavirenz, dysrhythmia and HIV.Clinical cardiology · 2021Article
- Association between exposure to Efavirenz and substrates of dysrhythmia in HIV-infected young adults.Clinical cardiology · 2021Article
- Nanoparticle delivery system, highly active antiretroviral therapy, and testicular morphology: The role of stereology.Pharmacology research & perspectives · 2021Review
- Prevalence of Cytochrome P450 2B6 Single Nucleotide Polymorphism in an HIV-Positive Cohort in Jos, Nigeria: Implication for HIV Therapy.Nigerian journal of clinical practice · 2020Article
- Safety implications of combined antiretroviral and anti-tuberculosis drugs.Expert opinion on drug safety · 2020Review
- Predictors of electrocardiographic QT interval prolongation in men with HIV.Heart (British Cardiac Society) · 2019Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundEfavirenz (EFV) has been associated with torsade de pointes despite marginal QT interval lengthening. 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.
objectiveThe primary objective of this study was to evaluate EFV-associated QT interval changes with regard to CYP2B6 genotype and to explore mechanisms of QT interval lengthening.
methodsEFV was administered to healthy volunteers (n = 57) as a single 600 mg dose followed by multiple doses to steady-state. Subjects were genotyped for known CYP2B6 alleles and ECGs and EFV plasma concentrations were obtained serially. Whole-cell, voltage-clamp experiments were performed on cells stably expressing hERG and exposed to EFV in the presence and absence of CYP2B6 expression.
resultsEFV demonstrated a gene-dose effect and exceeded the FDA criteria for QTcF interval prolongation in CYP2B6*6/*6 carriers. The largest mean time-matched differences ∆∆QTcF were observed at 6 hours (14 milliseconds; 95% CI [1; 27]), 12 hours (18 milliseconds; 95% CI [-4; 40]), and 18 hours (6 milliseconds; 95% CI [-1; 14]) in the CYP2B6*6/*6 genotype. EFV concentrations exceeding 0.4 μg/mL significantly inhibited outward hERG tail currents (P < 0.05).
conclusionsThis study demonstrates that homozygous carriers of CYP2B6*6 allele may be at increased risk for EFV-induced QTcF interval prolongation via inhibition of hERG.
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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.