Drug intelligence / Profile preview

bms-663068 + maraviroc

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination of two antiretroviral agents** used in the treatment of HIV-1: - **BMS-663068** (also known as fostemsavir) is a prodrug of BMS-626529 and acts as an attachment inhibitor by binding to the HIV-1 gp120 protein, blocking the virus from attaching to and entering CD4+ T-cells. This mechanism is active regardless of whether the virus uses CCR5 or CXCR4 co-receptors, and provides a novel resistance profile, remaining effective against virus strains resistant to other antiretrovirals[1][3][5][7]. - **Maraviroc** is a CCR5 antagonist that blocks the CCR5 co-receptor on the surface of CD4+ cells, thereby preventing HIV from entering these cells. It is effective in patients with CCR5-tropic HIV and is known for a favorable safety and efficacy profile[4][6]. - This combination targets two distinct steps in the HIV entry process, potentially providing synergistic antiviral activity for heavily treatment-experienced patients or those with multidrug-resistant HIV-1[1][5]. - BMS-663068 (fostemsavir) was developed by Bristol Myers Squibb; maraviroc was originally developed by Pfizer and is marketed as Celsentri (internationally) or Selzentry (in the USA).

Brand names
CelsentriSelzentry
Other names
fostemsavirmaraviroc
02

Targets

gp120 (HIV-1 envelope glycoprotein (gp120/gp41) epitopes)CCR5 (C-C chemokine receptor type 5)

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