temsavir

Temsavir is a small molecule HIV-1 attachment inhibitor and the active metabolite of fostemsavir. It works by binding directly to the gp120 subunit of the HIV-1 envelope glycoprotein, adjacent to the CD4 binding site, thereby preventing the conformational change required for viral attachment and entry into host CD4+ T cells. This mechanism blocks the first step in the HIV-1 lifecycle—viral entry—making it effective against multidrug-resistant strains of HIV-1. Temsavir is administered as its prodrug fostemsavir (marketed as Rukobia), which is rapidly converted to temsavir after oral administration[1][2][6]. The drug was developed primarily for use in combination with other antiretrovirals in heavily treatment-experienced patients with multidrug-resistant HIV-1 infection who are failing their current therapy[1][6].

Other names

temsavir