Magazine article Drug Topics

Lipid-Lowering Drug Marks First New Class in 15 Years

Magazine article Drug Topics

Lipid-Lowering Drug Marks First New Class in 15 Years

Article excerpt

Physicians and patients have a new weapon in the war against hypercholesterolemia. Last month, the Food & Drug Administration approved ezetimibe (Zetia, Merck/Schering-Plough) for the treatment of primary hypercholesterolemia. Ezetimibe is also indicated for the treatment of homozygous familial hypercholesterolemia and homozygous sitosterolemia. The drug can be administered either as monotherapy or in combination with a statin.

"Ezetimibe represents a new option to help physicians and their patients achieve the aggressive reduction in low-density lipoprotein (LDL) cholesterol levels recommended in recently published guidelines, such as those issued by the National Cholesterol Education Program Adult Treatment Panel III last year," said Christie Ballantyne, MD., director, Center for Cardiovascular Disease Prevention, Methodist-DeBakey Heart Center, Baylor College of Medicine, Houston. Ezetimibe was slated to hit the shelves the second week in November.

This is the first in a new class of lipid-lowering agents to receive FDA approval since the statins were introduced 15 years ago. Ezetimibe does not inhibit cholesterol synthesis in the liver or increase bile acid excretion. Instead, it appears to act at the brush border of the small intestine to inhibit the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This caus- es a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood.

The LDL-lowering effect of ezetimibe is additive to that of the statins, because their mechanisms of action are different, said Ballantyne. According to the manufacturer, the FDA based its approval of ezetmibe at least in part on the results of four coadmin- istration studies in which combination therapy consisting of ezetimibe and a statin was initiated in previously untreated patients with hypercholesterolemia. The coadministration study of ezetimibe 10 mg and simvastatin (Zocor, Merck) 20 mg resulted in a 46% reduction in LDL cholesterol - a reduction similar to that seen with simvastatin 80-mg monotherapy, Ballantyne reported. Merck and Schering-Plough are currently testing a single drug that combines both ezetimibe and simvastatin, he continued. There are plans to file for approval of the combination drug in late 2003, with an anticipated approval in 2004.

The recommended dose of ezetimibe is one 10-mg tablet daily, taken without regard to food or time of day. Ballantyne recommends that his patients take their medication when it is most convenient. Dosing of ezetimibe should occur more than two hours before or more than four hours after administration of a bile acid sequestrant. …

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