BMS626529

Temsavir, also known as BMS-626529, is a potent HIV-1 attachment inhibitor. BMS-663068 is also the phosphonooxymethyl prodrug of BMS-626529 that targets HIV-1 gp120 and prevents its binding to CD4 (+) T cells. 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. (In Vitro) :Temsavir has half-maximal effective concentration (EC50) values of 2,000 nM against the least susceptible virus. The cytotoxicity profile of Temsavir is examined in several cell types from different human tissues. CC50 values of >200 μM are observed in MT-2 (T lymphocytes), HEK293 (kidney), HEp-2 (larynx), HepG2 (liver), HeLa (cervix), HCT116 (colorectal), MCF-7 (breast), SK-N-MC (neuroepithelium), HOS (bone), H292 (lung), and MDBK (bovine kidney) cells measured after 3 or 6 days in culture. CC50 values of 105 and 192 μM are obtained in the T-cell line PM1 and in PBMCs, respectively, following 6 days in culture. These results show that Temsavir exhibits low cytotoxicity in cell culture. Temsavir exhibits a broad spectrum of antiviral activity against a panel of clinical isolates, with a 50% inhibitory concentration (IC50) ranging from subnanomolar levels to >0.1 μM.