brecanavir

Brecanavir is an orally active aspartic protease inhibitor developed for the treatment of HIV-1 infection. It was investigated by Vertex and GlaxoSmithKline. Brecanavir inhibits the HIV viral proteinase enzyme, preventing cleavage of the Gag-Pol polyprotein and resulting in noninfectious, immature viral particles. In vitro studies demonstrated that brecanavir has potent activity against both wild-type and protease inhibitor-resistant strains of HIV-1 at concentrations much lower than most existing protease inhibitors. It showed synergistic or additive effects when combined with other antiretroviral agents such as nucleoside reverse transcriptase inhibitors and non-nucleoside reverse transcriptase inhibitors. Despite promising preclinical results, development was discontinued in December 2006 due to insurmountable formulation issues[1][2][3][4][7].

Other names

brecanavir