ArticleAntimicrobial agents and chemotherapy2012
Sustained release of the CCR5 inhibitors CMPD167 and maraviroc from vaginal rings in rhesus macaques.
Article in Antimicrobial agents and chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 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
33 citing papers in PubMed, 58 citations in OpenAlex.
- Pediatric NIH Workshop: Session I: Nonhuman Primate Models in HIV Prevention Research-A Historical and Comparative Perspective.Journal of medical primatology · 2026Review
- Ex Vivo Evaluation of Mucosal Responses to Vaccination with ALVAC and AIDSVAX of Non-Human Primates.Vaccines · 2022Article
- Prevalence of CCR5delta32 in Northeastern Iran.BMC medical genetics · 2019Article
- Relating Advanced Electrospun Fiber Architectures to the Temporal Release of Active Agents to Meet the Needs of Next-Generation Intravaginal Delivery Applications.Pharmaceutics · 2019Review
- Griffithsin carrageenan fast dissolving inserts prevent SHIV HSV-2 and HPV infections in vivo.Nature communications · 2018Article
- Vaginal drug delivery for the localised treatment of cervical cancer.Drug delivery and translational research · 2017Review
- Historical development of vaginal microbicides to prevent sexual transmission of HIV in women: from past failures to future hopes.Drug design, development and therapy · 2017Review
- Sustained release of the candidate antiretroviral peptides T-1249 and JNJ54310516-AFP from a rod insert vaginal ring.Drug delivery and translational research · 2016Article
- Drug transporters in tissues and cells relevant to sexual transmission of HIV: Implications for drug delivery.Journal of controlled release : official journal of the Controlled Release Society · 2015Review
- ADS-J1 inhibits semen-derived amyloid fibril formation and blocks fibril-mediated enhancement of HIV-1 infection.Antimicrobial agents and chemotherapy · 2015Article
- Lack of in vitro-in vivo correlation for a UC781-releasing vaginal ring in macaques.Drug delivery and translational research · 2015Article
- A long-acting integrase inhibitor protects female macaques from repeated high-dose intravaginal SHIV challenge.Science translational medicine · 2015Article
- Article
- Short communication: a repeated simian human immunodeficiency virus reverse transcriptase/herpes simplex virus type 2 cochallenge macaque model for the evaluation of microbicides.AIDS research and human retroviruses · 2014Article
- Pharmacokinetic evaluation of tenofovir disoproxil fumarate released from an intravaginal ring in pigtailed macaques after 6 months of continuous use.Journal of medical primatology · 2014Article
- Pharmacokinetics and preliminary safety study of pod-intravaginal rings delivering antiretroviral combinations for HIV prophylaxis in a macaque model.Antimicrobial agents and chemotherapy · 2014Article
- Electrospun solid dispersions of Maraviroc for rapid intravaginal preexposure prophylaxis of HIV.Antimicrobial agents and chemotherapy · 2014Article
- Pharmacokinetics of antiretrovirals in genital secretions and anatomic sites of HIV transmission: implications for HIV prevention.Clinical pharmacokinetics · 2014Review
- Modified silicone elastomer vaginal gels for sustained release of antiretroviral HIV microbicides.Journal of pharmaceutical sciences · 2014Article
- Pharmacokinetics of a CCR5 inhibitor in rhesus macaques following vaginal, rectal and oral application.The Journal of antimicrobial chemotherapy · 2014Article
Corrections and comments
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Authors and funding
15 authors at 4 institutions in 2 countries.
Funding
Abstract
Antiretroviral entry inhibitors are now being considered as vaginally administered microbicide candidates for the prevention of the sexual transmission of human immunodeficiency virus. Previous studies testing the entry inhibitors maraviroc and CMPD167 in aqueous gel formulations showed efficacy in the macaque challenge model, although protection was highly dependent on the time period between initial gel application and subsequent challenge. In this paper, we describe the sustained release of maraviroc and CMPD167 from matrix-type silicone elastomer vaginal rings both in vitro and in vivo. Both inhibitors were released continuously during 28 days from rings in vitro at rates of 100 to 2,500 μg/day. In 28-day pharmacokinetic studies in rhesus macaques, the compounds were measured in the vaginal fluid and vaginal tissue; steady-state fluid concentrations were ~10(6)-fold greater than the 50% inhibitory concentrations (IC(50)s) for simian human immunodeficiency virus 162P3 inhibition in macaque lymphocytes in vitro. Plasma concentrations for both compounds were very low. The pretreatment of macaques with Depo-Provera (DP), which is commonly used in macaque challenge studies, was shown to significantly modify the biodistribution of the inhibitors but not the overall amount released. Vaginal fluid and tissue concentrations were significantly decreased while plasma levels increased with DP pretreatment. These observations have implications for designing macaque challenge experiments and also for ring performance during the human female menstrual cycle.
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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.