Apabetalone

A small molecule inhibitor of BET proteins

Apabetalone
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Apabetalone (also known as RVX-208) is a small molecule that acts as a selective inhibitor of the bromodomain and extra-terminal domain (BET) family of proteins. It is being investigated for its potential therapeutic effects in various cardiovascular and metabolic diseases.

Mechanism of Action

Apabetalone functions by inhibiting the activity of BET proteins, which are epigenetic "readers" that recognize acetylated lysine residues on histone tails. This interaction plays a crucial role in the regulation of gene expression. By inhibiting BET proteins, apabetalone modulates the expression of genes involved in inflammation, lipid metabolism, and vascular function.

Therapeutic Applications

Apabetalone is primarily being studied for its effects in cardiovascular disease, particularly in patients with atherosclerosis and chronic kidney disease. It has shown potential in reducing the risk of major adverse cardiovascular events (MACE) by modulating inflammatory pathways and improving lipid profiles.

Cardiovascular Disease

In clinical trials, apabetalone has demonstrated the ability to reduce levels of C-reactive protein (CRP), a marker of inflammation, and improve high-density lipoprotein (HDL) function. These effects are thought to contribute to its cardiovascular benefits.

Metabolic Disorders

Apabetalone is also being explored for its role in managing type 2 diabetes mellitus and related metabolic disorders. By influencing gene expression, it may improve insulin sensitivity and glucose metabolism.

Clinical Trials

Several clinical trials have been conducted to evaluate the efficacy and safety of apabetalone. These include studies focusing on its impact on cardiovascular outcomes, renal function, and metabolic parameters in high-risk patient populations.

Safety and Tolerability

Apabetalone has been generally well-tolerated in clinical studies, with a safety profile comparable to placebo. Common adverse effects include headache, nasopharyngitis, and gastrointestinal disturbances.

Related pages

• Bromodomain and extra-terminal domain family
• Epigenetics
• Cardiovascular disease
• Type 2 diabetes mellitus