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Abstract

CHEMISTRY OF FOUR MEMBERED HETEROCYLIC EZETIMIBE AS LIPID LOWERING AGENT

Ezetimibe is a drug that lowers cholesterol. It acts by decreasing cholesterol absorption in the intestine. It may be used alone (marketed as Zetia or Ezetrol), when other cholesterol-lowering medications are not tolerated, or together with statins (e.g., ezetimibe/simvastatin, marketed as Vytorin and Inegy) when statins alone do not control cholesterol. Even though ezetimibe decreases cholesterol levels, the results of two major, high-quality clinical trials (in 2008 and 2009) showed that it did not improve clinically significant outcomes, such as major coronary events, and actually made some outcomes, such as artery wall thickness, worse. Indeed, a panel of experts concluded in 2008 that it should "only be used as a last resort". In one of those studies, a head-to-head trial in 2009, a much less expensive medication (extended-release niacin) was found to be superior. Ezetimibe actually increased the thickness of artery walls (a measurement of atherosclerosis) and caused more major cardiovascular events. However, in combination with simvastatin a 2010 trial has shown it to be better than atorvastatin and rosuvastatin at lowering lipid levels. A significantly more positive view of the benefits of Ezetimibe is offered by Britain's NICE.


Author(s): Kiran M. Patel, Divyang H. Shah, Jignesh B. Patel, Jimit S. Patel, Charoo S. Garg and Prof. Dr. Dhrubo Jyoti Sen

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