ArticleBiochemical pharmacology2013
Dissimilarities in the metabolism of antiretroviral drugs used in HIV pre-exposure prophylaxis in colon and vagina tissues.
Article in Biochemical pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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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.
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Who cites it
19 citing papers in PubMed, 31 citations in OpenAlex.
- Metabolism of Long-Acting Rilpivirine After Intramuscular Injection: HIV Prevention Trials Network Study 076 (HPTN 076).AIDS research and human retroviruses · 2021Trial
- Brief Report: Dapivirine Vaginal Ring Use Does Not Diminish the Effectiveness of Hormonal Contraception.Journal of acquired immune deficiency syndromes (1999) · 2017Trial
- Pharmacological evaluation of an ex vivo cervicovaginal HIV prevention model.The Journal of antimicrobial chemotherapy · 2026Article
- Lenacapavir: Playing the Long Game in the New Era of Antiretrovirals.Clinical pharmacology and therapeutics · 2025Review
- Investigating the Contribution of Drug-Metabolizing Enzymes in Drug-Drug Interactions of Dapivirine and Miconazole.Pharmaceutics · 2021Article
- Environmental Pollutants, Mucosal Barriers, and Pathogen Susceptibility; The Case for Aflatoxin BPathogens (Basel, Switzerland) · 2021Review
- Endogenous Hormones and Antiretroviral Exposure in Plasma, Cervicovaginal Fluid, and Upper-Layer Packed Cells of Malawian Women Living with HIV.AIDS research and human retroviruses · 2020Observational
- Rational Design of a Multipurpose Bioadhesive Vaginal Film for Co-Delivery of Dapivirine and Levonorgestrel.Pharmaceutics · 2019Article
- Pharmacology of Antiretrovirals in the Female Genital Tract for HIV Prevention.Journal of clinical pharmacology · 2018Review
- Physiologically-based pharmacokinetic model of vaginally administered dapivirine ring and film formulations.British journal of clinical pharmacology · 2018Article
- Rilpivirine Plasma and Cervicovaginal Concentrations in Women During Pregnancy and Postpartum.Journal of acquired immune deficiency syndromes (1999) · 2018Article
- Importance of Drug Pharmacokinetics at the Site of Action.Clinical and translational science · 2017Review
- Levonorgestrel in contraceptives and multipurpose prevention technologies: does this progestin increase HIV risk or interact with antiretrovirals?AIDS (London, England) · 2016Article
- Distinct Pharmacodynamic Activity of Rilpivirine in Ectocervical and Colonic Explant Tissue.Antimicrobial agents and chemotherapy · 2016Article
- Broadly Neutralizing Anti-HIV Antibodies Prevent HIV Infection of Mucosal Tissue Ex Vivo.Antimicrobial agents and chemotherapy · 2016Article
- Comparative Expression Analysis of Cytochrome P450 1A1, Cytochrome P450 1B1 and Nuclear Receptors in the Female Genital and Colorectal Tissues of Human and Pigtailed Macaque.BAOJ pharmaceutical sciences · 2016Article
- Pharmacodynamic Activity of Dapivirine and Maraviroc Single Entity and Combination Topical Gels for HIV-1 Prevention.Pharmaceutical research · 2015Article
- Article
- Pharmacokinetics and preliminary safety study of pod-intravaginal rings delivering antiretroviral combinations for HIV prophylaxis in a macaque model.Antimicrobial agents and chemotherapy · 2014Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
Abstract
Attempts to prevent HIV infection through pre-exposure prophylaxis (PrEP) include topical application of anti-HIV drugs to the mucosal sites of infection; however, a potential role for local drug metabolizing enzymes in modulating the exposure of the mucosal tissues to these drugs has yet to be explored. Here we present the first report that enzymes belonging to the cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) families of drug metabolizing enzymes are expressed and active in vaginal and colorectal tissue using biopsies collected from healthy volunteers. In doing so, we discovered that dapivirine and maraviroc, a non-nucleoside reverse transcriptase inhibitor and an entry inhibitor currently in development as microbicides for HIV PrEP, are differentially metabolized in colorectal tissue and vaginal tissue. Taken together, these data should help to guide the optimization of small molecules being developed for HIV PrEP.
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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.