Drug intelligence / Profile preview

RVX000222 + rosuvastatin

Development stage
Phase 3
Lead developer
ResVerlogiX
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of **apabetalone (RVX000222, also known as RVX-208)**, a first-in-class, orally active, small-molecule BET (bromodomain and extraterminal domain) inhibitor, with **rosuvastatin**, a widely used statin. Apabetalone is developed to modulate gene expression by inhibiting BET proteins, which affect a variety of pathways including inflammation, lipid metabolism, and atherogenesis. It upregulates apolipoprotein AI and thereby increases HDL cholesterol, aiming to reduce cardiovascular risk and events. Rosuvastatin inhibits HMG-CoA reductase to lower LDL cholesterol and has anti-inflammatory and plaque-stabilizing effects. The combination is investigated for potential additive or synergistic lipid-lowering and cardioprotective benefits, especially in dyslipidemia and cardiovascular disease.

02

Targets

BET (BET family proteins)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)BRD (Bromodomain-containing protein family)

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