Ezetimibe

Authors: Darkes M.J.M.; Poole R.M.; Goa K.L.

Source: American Journal of Cardiovascular Drugs, Volume 3, Number 1, 2003 , pp. 67-76(10)

Publisher: Adis International

Abstract:

Ezetimibe, a synthetic 2-azetidinone, is the first of a new class of compounds that selectively inhibits the absorption of cholesterol and related plant sterols in the intestine. The drug, and its glucuronyl metabolite, are thought to inhibit a putative cholesterol transporter of enterocytes, located within the brush-border membrane of the small intestine.

In large, randomized, placebo-controlled, 12-week trials, ezetimibe reduced levels of low density lipoprotein-cholesterol (LDL-C) by approximately 18%; triglyceride levels were reduced by approximately 6% in one trial but not another. Ezetimibe produced a modest increase in levels of high density lipoprotein-cholesterol.

Moreover, reductions in LDL-C and triglyceride levels were greater in patients treated with ezetimibe coadministered with a statin (lovastatin, pravastatin, atorvastatin or simvastatin), than with either of those agents given alone. The coadministration of the lowest statin dose and ezetimibe produced similar LDL-C reductions to the administration of the highest statin dose alone.

Ezetimibe also provided beneficial effects on plasma lipid levels when administered to patients with hypercholesterolemia already receiving a statin.

Ezetimibe plus a statin reduced LDL-C levels more than the maximum statin dose alone in a trial in patients with homozygous familial hypercholesterolemia and was effective in a placebo-controlled trial in patients with homozygous sitosterolemia.

The drug was well tolerated in clinical studies conducted to date. In large, randomized, double-blind trials, ezetimibe had a similar tolerability profile to that of placebo. Coadministration of ezetimibe and a statin did not increase the incidence of adverse events related to statin monotherapy.

Keywords: Adis Drug Profiles; Antihyperlipidaemics, general; Ezetimibe, general; Hypercholesterolaemia, treatment; Research and development

Language: English

Document Type: Miscellaneous

Affiliations: 1: Adis International Inc., Langhorne, Pennsylvania, USA *

Publication date: 2003-01-01

• In this: publication
• By this: publisher
• In this Subject: Cardiovascular Medicine ,  Pharmacology
• By this author: Darkes M.J.M. ;  Poole R.M. ;  Goa K.L.

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