The Pharmaceutical Journal
Vol 270 No 7246 p563
26 April 2003

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Merck (www.merck.com)

Cholesterol inhibitor launched as additional treatment to statins

Ezetimibe (Ezetrol), a cholesterol absorption inhibitor, has been launched this week by Merck Sharpe & Dohme and Schering Plough (see p569). Its main use will be as an add-on therapy for patients with primary hypercholesterolaemia not controlled by a statin alone.

MSD and Schering Plough, co-developers of the new drug, say that adding ezetimibe to the lowest dose of any statin provides lipid lowering efficacy equivalent to the highest dose of that statin.

The molecular mechanism of action of ezetimibe is not fully understood. However, the summary of product characteristics for ezetimibe says that the drug localises at the brush border of the small intestine where it inhibits absorption of cholesterol leading to a decrease in the delivery of intestinal cholesterol to the liver. By contrast, statins reduce cholesterol synthesis in the liver. "Together these distinct mechanisms provide complementary cholesterol reduction," it states.

Katrina Simister, assistant director, new medicines scheme, National Prescribing Centre, said she sees ezetimibe as an add-on therapy. However, she said: "Longer term data are required to confirm its effectiveness in terms of both coronary heart disease impact and potential adverse events, particularly in comparison to the use of statins, including rosuvastatin."

Recent trial results also show that adding ezetimibe to low-dose simvastatin (Zocor) gives an additional reduction in C-reactive protein, a marker for cardiovascular events and atherosclerosis (PJ, 12 April, p506).