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Vytorin (exetimibe/simvastatin) Dual Inhibition of the Two Sources of Cholestero

Jul 27, 2004

Loweres LDL cholesterol by 52 percent. VYTORIN(TM) lowered LDL cholesterol by 52 percent at the recommended starting dose (10/20 mg) and 60 percent at the maximum dose (10/80 mg). Merck/Schering-Plough Pharmaceuticals announced today that the U.S. Food and Drug Administration has approved VYTORIN(TM) (ezetimibe/simvastatin) for the treatment of high LDL cholesterol (LDL-C) in patients with primary hypercholesterolemia or mixed hyperlipidemia as adjunctive therapy to diet when diet alone is not enough.
VYTORIN is the first and only product approved to treat the two sources of cholesterol by inhibiting the production of cholesterol in the liver and blocking the absorption of cholesterol in the intestine, including cholesterol from food. The active ingredients in VYTORIN are ezetimibe and simvastatin. The recommended starting dose of VYTORIN is 10/20 mg (10 mg ezetimibe/20 mg simvastatin).

"Many patients who continue to have high cholesterol despite diet and other lifestyle modifications may require powerful LDL cholesterol lowering-agents and to do this we frequently look to highly efficacious medicines to provide the reduction they need," said Christie Ballantyne, M.D., director of the Center for Cardiovascular Disease Prevention, Methodist DeBakey Heart Center, Houston, TX.

In head-to-head trials, VYTORIN provided greater reductions in LDL cholesterol than atorvastatin (Lipitor) and simvastatin (Zocor) across the dosing range

"The dual inhibition of cholesterol provided by VYTORIN delivers impressive LDL cholesterol reductions across the dosing range and offers physicians a unique and powerful new option in the evolving treatment of hyperlipidemia, especially in people who need more aggressive treatment to reach goal," said Margo Denke, M.D., clinical professor, University of Texas Health Science Center, San Antonio, TX.

In a 24-week, multi-center, randomized, double-blind, active-controlled, forced titration study of 788 patients, VYTORIN (doses ranging from 10/10 mg to 10/80 mg) was compared to atorvastatin monotherapy (doses ranging from 10 mg to 80 mg). The average LDL cholesterol levels at baseline across treatment groups ranged from 179 mg/dL to 181 mg/dL. At the recommended usual starting doses, VYTORIN 10/20 mg lowered LDL cholesterol by 50 percent vs. 37 percent for atorvastatin 10 mg and 44 percent for atorvastatin 20 mg. The impact on clinical outcomes of these differences in lipid altering effects is unknown.

Cholesterol in the blood is derived from two sources – production by the body and absorption from the small intestine. The most widely prescribed cholesterol-lowering medications, called statins, work in the liver to reduce cholesterol production and increase clearance of cholesterol from the bloodstream. VYTORIN inhibits absorption of cholesterol in the small intestine, while also reducing cholesterol synthesis in the liver, leading to clearance of cholesterol from the bloodstream.

Muscle pain, tenderness or weakness in people taking VYTORIN should be reported to a doctor promptly because these could be signs of a serious side effect. VYTORIN should be discontinued if myopathy is diagnosed or suspected. People taking VYTORIN 10/80 mg should receive an additional liver function test prior to and three months after titration and periodically during the first year.

VYTORIN has been approved for use in patients at the following doses: 10/10 mg, 10/20 mg, 10/40 mg and 10/80 mg. Across the dosing range, the ezetimibe component of VYTORIN is held constant at 10 mg, while the simvastatin component ranges from 10 mg to 80 mg. The recommended starting dose for VYTORIN is 10/20 mg. Patients requiring LDL cholesterol reductions greater than 55 percent can be started on 10/40 mg. Patients requiring less aggressive LDL cholesterol reductions may be started at 10/10 mg. The price of VYTORIN will be $2.34 at all doses.