Fostemsavir: A Novel CD4 Attachment Inhibitor for Heavily Treated HIV-1 Patient

Abstract

Abstract: Despite the evident success of antiretroviral therapy in recent years, many patients undergoing intense treatment still struggle to find a cure for their disease due to drug resistance or treatment failure. To solve this problem, new antiretroviral drug alternatives are required. The HIV-1 antiretroviral drug fostemsavir (GSK3684394, previously BMS-663068) is a first-in-class HIV-1 attachment inhibitor with a novel mechanism. After oral administration, fostemsavir gets converted into temsavir in the gastrointestinal lumen, which then attaches to the glycoprotein 120 surface subunit on HIV-1 and produces a conformational change that prevents it from adhering to CD4+ T cells of the host immune system, thereby preventing the virus from infecting other cells. Fostemsavir is indicated in heavily treated (HTE) patients with an ideal antiretroviral (ARV) regimen. The drug has shown significant tolerability, and no hepatic or renal dose adjustments were required. Fostemsavir can be used as an effective alternative in salvage therapy because of its favourable adverse effect profile and few drug interactions.