Drug intelligence / Profile preview

BMS-955176 + dolutegravir + atazanavir

Development stage
Unknown
Lead developer
ViiV Healthcare
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **triple combination drug regimen** in development for the treatment of HIV-1 infection, composed of three agents: - **BMS-955176**: A second-generation small molecule HIV-1 maturation inhibitor that binds to the Gag protein of HIV-1, specifically inhibiting the final protease-mediated cleavage (CA/SP1 junction) required for the maturation of viral particles, thereby producing non-infectious virions[1][2][4][5][7]. - **Dolutegravir**: A small molecule integrase strand transfer inhibitor (INSTI) that blocks the integration of viral DNA into the host cell genome, inhibiting HIV replication. - **Atazanavir**: A small molecule protease inhibitor that prevents the cleavage of viral polyproteins necessary for the production of mature, infectious HIV particles. This combination was studied as a potential nucleoside-sparing regimen for treatment-experienced HIV-1-infected adults, including those with multidrug resistance or intolerance to current antiretroviral therapies. Development has focused on oral, once-daily administration, with or without a pharmacokinetic booster (ritonavir)[3][5][7]. The regimen is designed to provide potent antiviral activity, a distinct mechanism of action from current therapies, and the potential to address resistance, safety, and tolerability limitations of existing treatments[2][7]. BMS-955176 is developed by Bristol Myers Squibb, dolutegravir by ViiV Healthcare, and atazanavir by Bristol Myers Squibb.

02

Targets

Integrase allosteric pocket (HIV)Gag (HIV-1 Gag polyprotein)PR (Progesterone receptor)

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