ArticleThe Journal of antimicrobial chemotherapy2013
Pharmacokinetics and efficacy of a vaginally administered maraviroc gel in rhesus macaques.
Article in The Journal of antimicrobial chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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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.
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Who cites it
32 citing papers in PubMed.
- Review
- TheiScience · 2022Article
- In vitro inhibitory effect of maraviroc on the association of the simian immunodeficiency virus envelope glycoprotein with CCR5.Virus genes · 2021Article
- In situ-forming and pH-responsive hydrogel based on chitosan for vaginal delivery of therapeutic agents.Journal of materials science. Materials in medicine · 2018Article
- Transcutaneously refillable nanofluidic implant achieves sustained level of tenofovir diphosphate for HIV pre-exposure prophylaxis.Journal of controlled release : official journal of the Controlled Release Society · 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
- CD4-mimetic sulfopeptide conjugates display sub-nanomolar anti-HIV-1 activity and protect macaques against a SHIV162P3 vaginal challenge.Scientific reports · 2016Article
- Simultaneous measurement of etravirine, maraviroc and raltegravir in pigtail macaque plasma, vaginal secretions and vaginal tissue using a LC-MS/MS assay.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences · 2016Article
- Coaxially electrospun fiber-based microbicides facilitate broadly tunable release of maraviroc.Materials science & engineering. C, Materials for biological applications · 2016Article
- Biophysical characterization of small molecule antiviral-loaded nanolipogels for HIV-1 chemoprophylaxis and topical mucosal application.Acta biomaterialia · 2016Article
- Short Communication: Limited Anti-HIV-1 Activity of Maraviroc in Mucosal Tissues.AIDS research and human retroviruses · 2016Article
- C5A Protects Macaques from Vaginal Simian-Human Immunodeficiency Virus Challenge.Antimicrobial agents and chemotherapy · 2016Article
- Current strategies for sustaining drug release from electrospun nanofibers.Journal of controlled release : official journal of the Controlled Release Society · 2015Review
- Protection Against Rectal Chimeric Simian/Human Immunodeficiency Virus Transmission in Macaques by Rectal-Specific Gel Formulations of Maraviroc and Tenofovir.The Journal of infectious diseases · 2015Article
- Pharmacokinetic and Pharmacodynamic Evaluation following Vaginal Application of IQB3002, a Dual-Chamber Microbicide Gel Containing the Nonnucleoside Reverse Transcriptase Inhibitor IQP-0528 in Rhesus Macaques.Antimicrobial agents and chemotherapy · 2015Article
- Pharmacodynamic Activity of Dapivirine and Maraviroc Single Entity and Combination Topical Gels for HIV-1 Prevention.Pharmaceutical research · 2015Article
- Maraviroc: a review of its use in HIV infection and beyond.Drug design, development and therapy · 2015Review
- Animal and human mucosal tissue models to study HIV biomedical interventions: can we predict success?Journal of the International AIDS Society · 2015Review
- Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
objectivesTo investigate the pharmacokinetics (PK) of maraviroc, a CCR5-targeted HIV-1 entry inhibitor, in rhesus macaques following vaginal administration of various maraviroc-loaded aqueous hydroxyethylcellulose (HEC) gels, and to correlate the PK data with efficacy in a single high-dose vaginal SHIV-162P3 challenge model.
methodsMaraviroc concentrations in vaginal fluid (Weck-Cel(®) sponge), vaginal tissue (punch biopsy) and plasma were assessed over 72 h following single-dose vaginal application of various maraviroc-loaded HEC gels. The range of maraviroc gel concentrations was sufficiently broad (0.003%-3.3% w/w) that test gels included both fully solubilized and predominantly dispersed formulations. The efficacy of the HEC gels against a single high-dose vaginal SHIV-162P3 challenge was also measured, and correlated with the PK concentrations.
resultsMaraviroc concentrations in vaginal fluid (range 10(4)-10(7) ng/mL), vaginal tissue (100-1200 ng/g) and plasma (<10(2) ng/mL) were highly dependent on maraviroc gel loading, irrespective of the form of the maraviroc component within the gel (solubilized versus dispersed). Fluid and plasma concentrations were generally highest 0.5 or 2 h after gel application, before declining steadily through to 72 h. Maraviroc concentrations in the various biological compartments correlated strongly with the extent of protection against vaginal SHIV-162P3 challenge. Complete protection was achieved with a 3.3% w/w maraviroc gel.
conclusionsA high degree of correlation between PK and efficacy was observed. Based on the data obtained with the 3.3% w/w maraviroc gel, maintenance of vaginal fluid and tissue levels in the order of 10(7) ng/mL and 10(3) ng/g, respectively, are required for complete protection with this compound.
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