Ezetimibe (Schering-Plough).
Ezetimibe (Sch-58235) is a cholesterol absorption inhibitor being developed by Schering-Plough for the potential treatment of atherosclerosis and hypercholesterolemia. By January 2000, it was in phase III trials in the US [353762], [363364]. Schering-Plough is studying ezetimibe as a monotherapy for lowering lipid levels and, by February 2000, it was also planning combination studies with commonly used statin (HMG-CoA reductase inhibitor) therapies. The company believes that ezetimibe will have additive effects with the statins, inhibiting the absorption of cholesterol in the intestine while the statins work by inhibiting the production of cholesterol in the liver [363364]. In May 2000, Merck signed an agreement with Schering-Plough to develop and market in the US a once-daily, fixed-combination tablet with simvastatin (Zocor) [368021]. This combination has been shown to improve LDL reduction to 52% as compared to 35% with Zocor alone [375966].
Meng
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CQ
AtheroGenics Inc, Alpharetta, GA 30004, USA. cmeng@atherogenics.com
D000818:Animals; D000924:Anticholesteremic Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D001161:Arteriosclerosis / Q000188:drug therapy; D001384:Azetidines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D001646:Bile / Q000378:metabolism; D002784:Cholesterol / Q000378:metabolism; D008078:Cholesterol, LDL / Q000096:biosynthesis; D017322:Clinical Trials, Phase II as Topic; D015536:Down-Regulation; D004338:Drug Combinations; D004353:Drug Evaluation, Preclinical; D004359:Drug Therapy, Combination; D015507:Drugs, Investigational; D000069438:Ezetimibe; D005544:Forecasting; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000008:administration & dosage / Q000627:therapeutic use; D006937:Hypercholesterolemia / Q000188:drug therapy; D007408:Intestinal Absorption / Q000187:drug effects; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000187:drug effects; D015394:Molecular Structure; D019821:Simvastatin / Q000008:administration & dosage / Q000627:therapeutic use
D000924:Anticholesteremic Agents; D001384:Azetidines; D008078:Cholesterol, LDL; D004338:Drug Combinations; D015507:Drugs, Investigational; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D002784:Cholesterol; D019821:Simvastatin; D000069438:Ezetimibe