Experimental Cholesterol Drug Shows Promise

Evacetrapib found to lower bad cholesterol and increase good cholesterol

(RxWiki News) Eli Lily's experimental drug evacetrapib has been shown to raise good cholesterol levels while also decreasing bad cholesterol. It also successfully lowered triglyceride levels.

The drug did not cause elevated blood pressure similar to another drug in the same class under development, which was previously halted. Trials for torcetrapib were stopped following excessive deaths in a large clinical trial.

"Monitor your cholesterol regularly."

Evacetrapib was found to be effective alone and offered additional benefits when taking with traditional cholesterol-lowering statins. The drug belongs to a new class of medications capable of blocking the enzyme cholesteryl ester transfer protein, or CETP, to transfer cholesterol particles from HDL to LDL. When more active CETP is in the bloodstream, blood LDL levels are higher.

Dr. Stephen J. Nicholls, lead researcher and cardiovascular director of the Cleveland Clinic Coordinating Center for Clinical Research, said there has been considerable hope for CETP inhibitors as the next big thing in heart disease treatment, but researchers were forced back to square one after the failure of torcetrapib. He now believes he has a drug safe enough to test in large clinical trials to determine whether it is beneficial for patients.

During the trial's second phase, researchers enrolled 393 men and women with an average age of 59 years old at 57 medical centers throughout the United States and Europe. During the 12-week trial, participants took either 30, 100 or 500 milligrams a day of evacetrapib.

LDL cholesterol levels were found to have fallen by between 14 percent and 36 percent, while HDL levels increased by 54 percent to 129 percent as compared to taking a placebo. Triglycerides were also found to fall by 16 percent. At the highest dose, the experimental drug reduced LDL cholesterol by up to 170 percent.

Some patients took both 100 milligrams of evacetrapib as well as a cholesterol-lowering statin ― either 20 milligrams daily of atorvastatin (Lipitor), 10 milligrams a day of rosuvastatin (Crestor) or 40 milligrams a day of simvastatin (Zocor). In these patients, LDL levels fell and HDL levels rose more significantly than in patients taking only the statins.

When investigators analyzed the effects of evacetrapib in pre-specified subgroups of patients, they found it had a greater impact in those who were younger or started the trial with lower HDL or higher triglycerides.

Researchers also discovered that evacetrapib had a greater impact in younger patients or those who started the trial with lower HDL or higher triglycerides.

The study was presented today at the American Heart Association's annual meeting in Orlando, Fla., and also simultaneously published in the Journal of the American Medical Association. The research was funded by Eli Lily.

Review Date: 
November 15, 2011