ArticleJournal of clinical pharmacology2014
Expression of six drug transporters in vaginal, cervical, and colorectal tissues: Implications for drug disposition in HIV prevention.
Article in Journal of clinical pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT02983110 (Does Sex Hormone Therapy Decrease Nucleos), which is not on this map. Cited by 42 papers.
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.
Does Sex Hormone Therapy Decrease Nucleos(t)Ide Reverse Transcriptase Inhibitors (NRTI) Active Metabolite Formation in Mucosal Tissues?
Who cites it
42 citing papers in PubMed, 53 citations in OpenAlex.
- Phase 1 Pharmacokinetic Trial of 2 Intravaginal Rings Containing Different Dose Strengths of Vicriviroc (MK-4176) and MK-2048.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2019Trial
- Phase 2a Safety, Pharmacokinetics, and Acceptability of Dapivirine Vaginal Rings in US Postmenopausal Women.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2019Trial
- Single-dose pharmacokinetics of tenofovir alafenamide and its active metabolite in the mucosal tissues.The Journal of antimicrobial chemotherapy · 2017Trial
- Analytical Advances in the Ex Vivo Challenge Efficacy Assay.AIDS research and human retroviruses · 2017Trial
- Trial
- Effect of HIV infection and menopause status on raltegravir pharmacokinetics in the blood and genital tract.Antiviral therapy · 2015Trial
- Expanding the Gene Expression Profiling of Drug Transporters and Drug-Metabolizing Enzymes to Include the Upper Female Reproductive Tract.Pharmaceutics · 2026Article
- Tenofovir, Interferon Pathways, and Mucosal Immunity: Implications for People Living With HIV.American journal of reproductive immunology (New York, N.Y. : 1989) · 2026Review
- Pharmacological evaluation of an ex vivo cervicovaginal HIV prevention model.The Journal of antimicrobial chemotherapy · 2026Article
- Female Reproductive Tract Organ-on-Chips: Modeling Barrier Function and Drug Transport.Pharmaceutics · 2026Review
- Heterogeneous Antiretroviral Drug Exposure in Male and Female Genital Tract Tissues.The Journal of infectious diseases · 2025Article
- Drug transporter mRNA expression and genital inflammation in South African women on oral pre-exposure prophylaxis (PrEP).AIDS research and therapy · 2025Article
- Female Genital Tract Host Factors and Tenofovir and Lamivudine Active Metabolites.The Journal of infectious diseases · 2024Article
- Translational Models to Predict Target Concentrations for Pre-Exposure Prophylaxis in Women.AIDS research and human retroviruses · 2022Review
- Transport and Permeation Properties of Dapivirine: Understanding Potential Drug-Drug Interactions.Pharmaceutics · 2022Article
- Comprehensive Study of Antiretroviral Drug Permeability at the Cervicovaginal MucosaPharmaceutics · 2022Article
- Pharmacogenomics of drug transporters for antiretroviral long-acting pre-exposure prophylaxis for HIV.Frontiers in genetics · 2022Review
- Antiretroviral Penetration and Drug Transporter Concentrations in the Spleens of Three Preclinical Animal Models and Humans.Antimicrobial agents and chemotherapy · 2020Article
- 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
- Changes in the Serum Metabolome of Patients Treated With Broad-Spectrum Antibiotics.Pathogens & immunity · 2020Article
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 3 institutions in 1 country.
Funding
Abstract
Effective antiretroviral (ARV)-based HIV prevention strategies require optimizing drug exposure in mucosal tissues; yet factors influencing mucosal tissue disposition remain unknown. We hypothesized drug transporter expression in vaginal, cervical, and colorectal tissues is a contributing factor and selected 3 efflux (ABCB1/MDR1, ABCC2/MRP2, ABCC4/MRP4) and 3 uptake (SLC22A6/OAT1, SLC22A8/OAT3, SLCO1B1/OATP1B1) transporters to further investigate based on their affinity for 2 ARVs central to prevention (tenofovir, maraviroc). Tissue was collected from 98 donors. mRNA and protein expression were quantified using qPCR and immunohistochemistry (IHC). Hundred percent of tissues expressed efflux transporter mRNA. IHC localized them to the epithelium and/or submucosa. Multivariable analysis adjusted for age, smoking, and co-medications revealed significant (P < 0.05) differences in efflux transporter mRNA between tissue types (vaginal ABCB1 3.9-fold > colorectal; vaginal ABCC2 2.9-fold > colorectal; colorectal ABCC4 2.0-fold > cervical). In contrast, uptake transporter mRNA was expressed in <25% of tissues. OAT1 protein was detected in 0% of female genital tissues and in 100% of colorectal tissues, but only in rare epithelial cells. These data support clinical findings of higher maraviroc and tenofovir concentrations in rectal tissue compared to vaginal or cervical tissue after oral dosing. Quantifying mucosal transporter expression and localization can facilitate ARV selection to target these tissues.
Indexed as
Identifiers
What OpenQuestion holds
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.