Safety, tolerability and pharmacokinetics of rilpivirine following administration of a long‐acting formulation in healthy volunteers

• Published in: HIV medicine 2015-09, Vol.16 (8), p.477-484
• Main Authors: Verloes, R, Deleu, S, Niemeijer, N, Crauwels, H, Meyvisch, P, Williams, P
• Format: Article
• Language: English
• Subjects: Adult; Anti-HIV Agents - administration & dosage; Anti-HIV Agents - adverse effects; Anti-HIV Agents - pharmacokinetics; Area Under Curve; Delayed-Action Preparations; Double-Blind Method; Female; Healthy Volunteers; HIV; HIV Infections - drug therapy; Humans; long‐acting formulation; Male; Middle Aged; nonnucleoside reverse transcriptase inhibitor; pharmacokinetics; Reverse Transcriptase Inhibitors - administration & dosage; Reverse Transcriptase Inhibitors - adverse effects; Reverse Transcriptase Inhibitors - pharmacokinetics; rilpivirine; Rilpivirine - administration & dosage; Rilpivirine - adverse effects; Rilpivirine - pharmacokinetics; Young Adult
• ISSN: 1464-2662; 1468-1293
• DOI: 10.1111/hiv.12247

Objectives This phase I healthy volunteer study (NCT01031589) was carried out to investigate the safety/tolerability and pharmacokinetics of a rilpivirine (RPV; TMC278) long‐acting (LA) formulation after single and multiple intramuscular (IM) injections. Methods In the first part of the study, which had an open‐label design, a single RPV LA IM injection (300 mg/mL) of 300 (n = 6) or 600 (n = 5) mg was given to the volunteers. In the second part of the study, which had a double‐blind, randomized, placebo‐controlled design, three RPV LA IM injections (one every 4 weeks) at 1200/600/600 mg (n = 6) or placebo (n = 2) were given. Safety and local tolerability were monitored. RPV plasma concentrations were analysed up to 28 days after injection or until they were