Anacetrapib is a CETP inhibitor

CETP inhibitor

A CETP inhibitor is a member of a class of drugs that inhibit cholesterylester transfer protein . They are intended to reduce the risk of atherosclerosis by improving blood lipid levels.Examples include:...

 being developed to treat hypercholesterolemia

Hypercholesterolemia

Hypercholesterolemia is the presence of high levels of cholesterol in the blood. It is not a disease but a metabolic derangement that can be caused by many diseases, notably cardiovascular disease...

 (elevated cholesterol levels) and prevent cardiovascular disease

Cardiovascular disease

Heart disease or cardiovascular disease are the class of diseases that involve the heart or blood vessels . While the term technically refers to any disease that affects the cardiovascular system , it is usually used to refer to those related to atherosclerosis...

.

Clinical trials

At the 16th International Symposium on Drugs Affecting Lipid Metabolism (New York, Oct 4-7, 2007), Merck reported on a Phase IIb study. The eight week study reported dosage correlated reduction in LDL-C and increases in HDL-C levels with no corresponding increases in blood pressure in any cohort. The increase in HDL was particularly significant, averaging 44 percent, 86 percent, 139 percent and 133 percent at doses of 10 mg, 40 mg, 150 mg and 300 mg.

Merck performed a dose-ranging study of anacetrapib, with the results presented in 2009

Phase III trial (DEFINE)

Merck started a Phase III trial to assess the drug's effects on LDL, HDL, clinically measurable cardiovascular events, and safety; It was code-named DEFINE (Determining the Efficacy and Tolerability of CETP Inhibition with Anacetrapib), and was described as a medium sized safety and efficacy trial.

Early results from the DEFINE trial were presented on November 17 at AHA2010, a meeting of the American Heart Association

American Heart Association

The American Heart Association is a non-profit organization in the United States that fosters appropriate cardiac care in an effort to reduce disability and deaths caused by cardiovascular disease and stroke. It is headquartered in Dallas, Texas...

. At 100 mg dosage, LDL decreased by 36% while HDL increased by 138%. Systolic blood pressure showed no increase, and there was no association with increased CVD death or events.
Cardiologist Steve Nissen

Steven Nissen

Steven E. Nissen , is a cardiologist, researcher and patient advocate. He is chairman of cardiovascular medicine at the Cleveland Clinic, in Cleveland, Ohio....

 described DEFINE as a medium-sized safety trial intended to find out "whether anacetrapib would show the same increase in adverse cardiovascular events that was seen with torcetrapib." Fortunately, anacetrapib did not. In his opinion the DEFINE study was too small to show a clear benefit, but the trends in the major adverse cardiovascular events were going in the right direction.

Two year follow up due to complete by December 2012.

See also

• Torcetrapib
  Torcetrapib
  Torcetrapib was a drug being developed to treat hypercholesterolemia and prevent cardiovascular disease...
  
  , another CETP inhibitor, which was developed by Pfizer
  Pfizer
  Pfizer, Inc. is an American multinational pharmaceutical corporation. The company is based in New York City, New York with its research headquarters in Groton, Connecticut, United States...
  
  but caused unacceptable increases in blood pressure and had net cardiovascular detriment.