Evaluation of the Safety, Acceptability, and Pharmacokinetic Profile of a Gel Formulation of OB-002 in Healthy Volunteers.

Abstract

OB-002 is an extremely potent CCR5 antagonist that has previously been shown to completely block transmission in a non-human primate model of HIV infection. The purpose of this study was to characterize the safety, acceptability, and pharmacokinetic profile of a gel formulation of OB-002 (OB-002H). The trial had two phases, an open label single dose exposure (vaginal and rectal) and a randomized placebo controlled multiple dose phase during which study participants received five vaginal daily doses of OB-002H gel or matched placebo in a 2:1 ratio. Serum OB-002 levels were quantified at multiple time points up to 24 hours after the first dose. A total of thirty female and male participants were enrolled in the study (12 in the single dose phase and 18 in the multiple dose phase). All adverse events were Grade 1 or Grade 2 and the majority were unrelated to study product. Only two product related transient Grade 2 events (both vulval dryness) occurred in the study, both in the OB-002H gel randomized multiple dose arm. All colposcopic and anoscopic assessments following product exposure were normal. There was no evidence of systemic absorption of OB-002. Overall, the product had a positive acceptability profile, and most study participants would consider using the product for protection against HIV or pregnancy. Future studies are needed to assess the extended safety and acceptability of OB-002H gel in sexually active participants.