Fostemsavir Tris

Fostemsavir Tris is the prodrug of BMS-626529, is a oral, safe and effective inhibitor of HIV-1 attachment. It inhibits human immunodeficiency virus type 1 (HIV-1) infection by binding to gp120 and interfering with the attachment of virus to CD4+ T-cells.BMS-663068 is the phosphonooxymethyl prodrug of BMS-626529, a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 (+) T cells.The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120. BMS-626529 had half-maximal effective concentration (EC (50) ) values of 6 log (10), with half-maximal effective concentration values in the low pM range against the most susceptible viruses. The in vitro antiviral activity of BMS-626529 was generally not associated with either tropism or subtype, with few exceptions. Measurement of the binding affinity of BMS-626529 for purified gp120 suggests that a contributory factor to its inhibitory potency may be a relatively long dissociative half-life. (In Vivo) :Fostemsavir Tris has good antiviral activity in subjects infected with virus shown to be susceptible (IC50, <100 nM) to the agent.