Evacetrapib

Evacetrapib

Evacetrapib is a cholesterylester transfer protein (CETP) inhibitor that was being developed for the treatment of cardiovascular disease. CETP inhibitors are a class of drugs that aim to increase levels of high-density lipoprotein (HDL) cholesterol while reducing levels of low-density lipoprotein (LDL) cholesterol.

Mechanism of Action

Evacetrapib works by inhibiting the activity of CETP, a protein that facilitates the transfer of cholesterol esters from HDL to other lipoproteins such as LDL and very-low-density lipoprotein (VLDL). By inhibiting CETP, evacetrapib increases HDL cholesterol levels and decreases LDL cholesterol levels, which is believed to reduce the risk of atherosclerosis and subsequent cardiovascular events.

Clinical Development

Evacetrapib was developed by Eli Lilly and Company. It underwent several phases of clinical trials to evaluate its efficacy and safety in patients with cardiovascular disease. Despite showing promising results in early trials, a large Phase III clinical trial known as ACCELERATE was terminated in October 2015. The trial was stopped because evacetrapib did not demonstrate a significant reduction in major adverse cardiovascular events compared to placebo, despite substantial increases in HDL cholesterol and reductions in LDL cholesterol.

Pharmacokinetics

The pharmacokinetics of evacetrapib involve its absorption, distribution, metabolism, and excretion. The drug is administered orally and has a half-life that supports once-daily dosing. It is metabolized primarily in the liver and excreted through both renal and fecal pathways.

Side Effects

Common side effects observed in clinical trials included hypertension, gastrointestinal disturbances, and nasopharyngitis. The safety profile of evacetrapib was considered acceptable, but its lack of efficacy in reducing cardiovascular events led to the discontinuation of its development.

Related Pages

• Cholesterylester transfer protein
• High-density lipoprotein
• Low-density lipoprotein
• Atherosclerosis
• Eli Lilly and Company
• Cardiovascular disease

See Also

• Anacetrapib
• Torcetrapib
• Dalcetrapib