Cabotegravir (GSK744; GSK1265744)

Description: Cabotegravir (also known as GSK744, GSK1265744) is a potent, orally bioavailable and long-acting inhibitor of HIV integrase used for the treatment and prevention of HIV infection. It has a broad spectrum of activity against different HIV subtypes. Cabotegravir inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. In resistance passage experiments, integrase enzyme assays, and cellular assays with site-directed molecular (SDM) HIV clones resistant to other classes of anti-HIV-1 agents and earlier integrase strand transfer inhibitors, Cabotegravir showed efficient inhibition of HIV replication through inhibiting HIV integrase. It is an investigational new drug under development for the treatment of HIV infection.

References: Antimicrob Agents Chemother. 2015 Jan; 59(1):397-406; Sci Transl Med. 2015 Jan 14; 7(270):270ra4.

GSK744; GSK-744; GSK 744; S/GSK1265744; S/GSK 1265744; S/GSK-1265744; Cabotegravir.

Chemical Name: (3S, 11aR)-N-(2, 4-difluorobenzyl)-6-hydroxy-3-methyl-5, 7-dioxo-2, 3, 5, 7, 11, 11a-hexahydrooxazolo[3, 2-a]pyrido[1, 2-d]pyrazine-8-carboxamide

Exact Mass: 405.1136