Drug intelligence / Profile preview

RVX000222 + atorvastatin

Development stage
Unknown
Lead developer
ResVerlogiX
Modality
Small Molecules
Administration
Oral
01

Overview

RVX000222 + atorvastatin is a **combination drug therapy** consisting of the small molecule BET inhibitor RVX000222 (apabetalone) and the HMG-CoA reductase inhibitor atorvastatin. RVX000222 selectively inhibits the second bromodomain (BD2) of BET proteins (BRD2, BRD3, BRD4), modulating gene expression linked to inflammation, atherosclerosis, lipid metabolism (increasing HDL and ApoA-I), and cardiovascular protection. Atorvastatin reduces cholesterol through competitive inhibition of HMG-CoA reductase, lowering LDL and providing anti-inflammatory and plaque stabilization effects. This combination has been studied primarily for reduction of major adverse cardiovascular events (MACE) in high-risk patients with type 2 diabetes and coronary artery disease, aiming to achieve greater cardiovascular benefit than statins alone. Developed by Resverlogix, the drug combination has progressed to phase III trials such as BETonMACE evaluating outcomes in conjunction with standard-of-care statin therapy[3][4][5].

Other names
apabetalone + atorvastatin
02

Targets

Bromodomain and Extra-Terminal domain family bromodomain 1BRD3 BD2 (Bromodomain-containing protein 3 (BRD3) bromodomain 2 (BD2))Bromodomain-containing protein 4, Bromodomain 2BRD3 BD1 (Bromodomain-containing protein 3, bromodomain 1)BRD2 BD2 (Bromodomain-containing protein 2, bromodomain 2)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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