Study in Healthy Volunteers of the Safety and Metabolism of Different Doses of the Anti-HIV Drug TMC278LA.

Summary

TMC278 (also called rilpivirine) is a new drug being developed to treat HIV. Usually TMC278 is taken as a tablet, by mouth, once a day, but a 'long acting' formulation has been developed so the drug stays in the bloodstream for a longer time - this allows the drug to be given by injection and less often. It is hoped that this injectable version of the drug may be used to help prevent HIV transmission in the future by giving it to people who are at risk of HIV. This is similar to the way travellers to areas with malaria may take antibiotics to prevent infection. The investigators aim to investigate the feasibility of using TMC278 as a preventative medication by performing this study. The purpose of this study is to investigate the levels of drug which can be measured in the blood, as well as the tissues and fluids of the rectum (the lowest part of the bowels just before the opening of the anus) as well as the safety of the drug and how well tolerated it is when given as a single dose. In this study, the investigators will not be investigating whether the drug prevents HIV so the investigators will recruit people who are HIV negative, and whose lifestyle does not put them at risk of becoming infected before or during the study. If the study shows the drug is well tolerated and produces appropriate levels of the drug (in the bloodstream and the rectal compartment) to suggest that it could be effective, it will help design future studies looking at preventing HIV.

Timeline

Start

2011-01

Primary completion

2012-06

Completion

2012-06

Publications

• Results Jackson AG, Else LJ, Mesquita PM, Egan D, Back DJ, Karolia Z, Ringner-Nackter L, Higgs CJ, Herold BC, Gazzard BG, Boffito M. A compartmental pharmacokinetic evaluation of long-acting rilpivirine in HIV-negative volunteers for pre-exposure prophylaxis. Clin Pharmacol Ther. 2014 Sep;96(3):314-23. doi: 10.1038/clpt.2014.118. Epub 2014 May 26.

Drugs

Indications