Fostemsavir is an antiretroviral HIV-1 attachment inhibitor targeted against the gp120 subunit within the HIV-1 gp160 envelope glycoprotein. The discovery of gp120 as a potential target of interest in the treatment of HIV-1 infection is relatively recent, and was born out of a desire to find alternative target proteins (i.e. mechanistically orthogonal therapies)...
- Mechanism
- Curator reviewed · 5 references
The gp120 subunit within the gp160 envelope glycoprotein of HIV-1 is a new and novel target in the treatment of HIV-1 infection. These subunits are responsible for facilitating the first step in the viral life cycle, attachment, by mediating the interaction between the virus and host cell CD4 receptors. Following attachment, HIV-1 undergoes assembly, budding, and maturation within the host cell, after which mature viral particles are released to continue the viral life cycle.
Fostemsavir's active metabolite, temsavir, is an HIV-1 attachment inhibitor. It binds directly to the gp120 subunit to inhibit viral interaction with host CD4 receptors, thereby preventing the initial attachment required for viral replication. It has also been shown to inhibit other gp120-dependent post-attachment steps required for viral entry.
- Primary indication
- Fostemsavir is indicated, in combination with other antiretrovirals, for the treatment of multidrug-resistant HIV-1 infection in heavily treatment-experienced adults failing their current antiretroviral therapy due to resistance, intolerance, or safety concerns.Curator reviewed · 1 structured indication
- Formula / weight
- C25H26N7O8P · 583.498 g/mol (avg)
- First approval
- Canada, 2021 · United States, 2020 · European Union, 2021
- Code names
- BMS-663068
- Brand names
Resolves to
SWMDAPWAQQTBOG-UHFFFAOYSA-NSMILESCOC1=CN=C(N2C=NC(C)=N2)C2=C1C(=CN2COP(O)(O)=O)C(=O)C(=O)N1CCN(CC1)C(=O)C1=CC=CC=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Fostemsavir, and which of those have an active Phase 3 trial?
Create a free account or log in to explore the full data card.
Create Account