Temsavir

Temsavir (BMS-626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4⁺ T cells. IC50 & Target: HIV-1^[1] In Vitro: Temsavir has half-maximal effective concentration (EC₅₀) values of <10 nM against the vast majority of viral isolates. Temsavir exhibits an average EC₅₀ against LAI virus of 0.7±0.4 nM. Temsavir exhibits an EC₅₀ of 0.01 nM against the most susceptible virus and an EC₅₀ 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^[1]. 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^[2].