fostemsavir

Fostemsavir is an antiretroviral drug used in combination with other medications to treat human immunodeficiency virus type 1 (HIV-1) infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 who are failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations[1][2][7]. It is a first-in-class HIV attachment inhibitor and acts as a prodrug of temsavir. Temsavir binds directly to the Envelope glycoprotein gp120 subunit of the HIV-1 envelope glycoprotein near the CD4 binding site, locking gp120 into a closed conformation and preventing its interaction with host CD4+ T cells. This blocks the initial step of viral entry into immune cells[3][6][8]. Fostemsavir was developed by ViiV Healthcare/GlaxoSmithKline and received FDA approval in July 2020 for use in patients with limited treatment options due to resistance or intolerance to other therapies[5][7].

Brand names

Rukobia

Other names

fostemsavir tromethamineFTRtemsavir (active metabolite)