Meng C Q
AtheroGenics Inc, Alpharetta, GA 30004, USA.
Curr Opin Investig Drugs. 2001 Mar;2(3):389-92.
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].
依泽替米贝（Sch-58235）是先灵葆雅公司正在研发的一种胆固醇吸收抑制剂，用于潜在治疗动脉粥样硬化和高胆固醇血症。到2000年1月，它在美国处于III期试验阶段[353762]，[363364]。先灵葆雅公司正在研究依泽替米贝作为降低血脂水平的单一疗法，到2000年2月，它还计划与常用的他汀类药物（HMG-CoA还原酶抑制剂）疗法进行联合研究。该公司认为依泽替米贝与他汀类药物会有相加作用，在他汀类药物通过抑制肝脏中胆固醇的产生起作用时，依泽替米贝抑制肠道中胆固醇的吸收[363364]。2000年5月，默克公司与先灵葆雅公司签署协议，在美国研发和销售一种与辛伐他汀（舒降之）的每日一次固定复方片剂[368021]。与单独使用舒降之相比，这种复方制剂已显示可将低密度脂蛋白降低幅度提高到52%，而单独使用舒降之的降低幅度为35%[375966]。
