Drug intelligence / Profile preview

BMS-986001 + efavirenz + lamivudine

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

Overview

This drug is a combination of three antiretroviral agents: BMS-986001 (also known as censavudine or festinavir), efavirenz, and lamivudine. It is used in investigational and clinical trial settings for the treatment of human immunodeficiency virus type 1 (HIV-1), and has also shown potent activity against HIV-2 in vitro[1][3][5]. - **BMS-986001** is a novel nucleoside reverse transcriptase inhibitor (NRTI) structurally related to stavudine but distinguished by an ethynyl group at the 4′-carbon. Its active form is incorporated into viral DNA by reverse transcriptase, causing termination of DNA synthesis[1][3][5]. - **Efavirenz** is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds allosterically to reverse transcriptase, inducing a conformational change and inhibiting enzyme activity[4][6]. - **Lamivudine** is a nucleoside reverse transcriptase inhibitor (NRTI) that is phosphorylated to its active triphosphate form and incorporated into viral DNA, also resulting in chain termination[6]. The combination acts by targeting HIV reverse transcriptase at multiple sites and has shown efficacy in suppressing HIV replication in clinical studies[1][3][4]. BMS-986001 is experimental, while efavirenz and lamivudine are widely used antiretrovirals.

02

Targets

Human immunodeficiency virus type 1 reverse transcriptasePOLG (Mitochondrial DNA polymerase gamma)HIV-2 reverse transcriptase

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