Drug intelligence / Profile preview

bms-663068 + rosuvastatin

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

Overview

**BMS-663068 + rosuvastatin** is a combination of two pharmaceutical drugs: - **BMS-663068** is a prodrug that is metabolized to BMS-626529, a first-in-class HIV-1 attachment inhibitor. Its mechanism of action is binding directly to the HIV-1 gp120 protein, preventing initial viral attachment and entry into host CD4+ T cells. Unlike CCR5 antagonists, BMS-626529 binds the virus, not the host cell[1][2][3][6]. - **Rosuvastatin** is a statin (a cholesterol-lowering agent), used as a substrate probe for OATP and BCRP transporters, and is commonly prescribed to reduce LDL cholesterol[1][5]. This combination has been studied primarily to assess potential drug-drug interactions and pharmacokinetic changes, specifically in healthy subjects to determine the impact of BMS-663068 on the systemic exposure of rosuvastatin. Coadministration leads to increased rosuvastatin exposure (Cmax and AUCINF increased by 78% and 69%, respectively), and is generally well-tolerated. BMS-663068 is under development for HIV-1 infection, while rosuvastatin's main use is hypercholesterolemia[1][2][3][4][6].

02

Targets

Env (HIV-1 envelope glycoprotein)CAR/RXRα (Constitutive androstane receptor (CAR)/Retinoid X receptor alpha (RXRα) heterodimer)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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