HIV-1 envelope glycoprotein gp41 (targeted by albuvirtide) (gp41)

Albuvirtide is a chemically modified peptide HIV-1 fusion inhibitor, approved in China, that targets the gp41 subunit of the HIV-1 envelope glycoprotein[2][4][7]. By binding to the HR1 region of gp41, it prohibits the formation of the six-helix bundle critical for viral fusion and entry into host CD4+ T cells[1][2][4]. Albuvirtide distinguishes itself from earlier fusion inhibitors through the addition of a 3-maleimimidopropionic acid group, allowing irreversible binding to serum albumin, which greatly prolongs its half-life (to approximately 11–12 days) and enables once-weekly intravenous dosing[1][3][9]. It shows potent antiviral activity against a broad spectrum of HIV-1 subtypes, including strains resistant to other fusion inhibitors like enfuvirtide. Albuvirtide is primarily indicated for treatment-experienced people living with HIV, particularly those with multidrug-resistant virus or those challenged by daily medication adherence, and is typically administered in combination with other antiretroviral agents[2][5]. The drug has demonstrated a favorable safety profile, with no major organ toxicity observed in clinical trials and no significant infusion site reactions, though the potential for resistance development remains a consideration[5][2][4].

Other names

LabuvirtideAlbuvirtide (ABT)MG9PC54E431417179-66-8

Prevents the formation of the six-helix bundle in HIV-1 gp41 by binding to the hydrophobic groove of the N-terminal heptad repeat (HR1) region, thereby blocking the fusion of the viral membrane with host CD4+ T cell membranes and preventing viral entry[1][2][4].