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Anacetrapib significantly raises HDL cholesterol, cuts LDL cholesterol nearly in half

An investigational drug, Anacetrapib, has raised HDL cholesterol by 138% and decreased LDL cholesterol by 40% without raising blood pressure.

DEFINE ( Determining the EFficacy and Tolerability of CETP INhibition with AnacEtrapib ) is a randomized, double-blind trial of 1,623 patients who took either 100 milligrams of the cholesterylester transfer protein ( CETP ) inhibitor Anacetrapib, or a placebo for 18 months at 153 centers in 20 countries. The patients were already being treated with a statin and/or other lipid-lowering medicine and had achieved their goal level of LDL cholesterol.

Anacetrapib reduced LDL by 40 percent ( from 81 mg/dL to 49 mg/dL ). It also more than doubled the level of HDL ( from 40 mg/dL to 101 mg/dL ).

The experimental drug is one of a new class that blocks the ability of the CETP enzyme to transfer cholesterol particles from HDL to LDL.

Elevated LDL and low levels of HDL are both risk factors for cardiovascular disease. Statins reduce LDL and lessen cardiovascular risk.
High natural levels of HDL are associated with lower cardiovascular risk.

Patients in DEFINE were 62.5 years old on average; 23 percent were women; 17 percent were Asian, black or multiracial and 15 percent were Hispanic. The study included interim safety analyses at six and 12 months, and researchers found no change in blood pressure or electrolytes among participants.

Levels of aldosterone, a hormone produced in the adrenal gland that affects kidney function and blood pressure, didn’t change. The researchers also found no increase in muscle problems or liver function abnormalities between groups, a side effect occasionally associated with statins.

Although the study was not designed or powered to assess the effects of Anacetrapib on cardiovascular events, fewer cardiovascular events occurred in the Anacetrapib group than in the statin-only group. The full efficacy and safety of Anacetrapib will be evaluated in a larger Phase III trial.

Source: American Heart Association’s Scientific Sessions, 2010

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