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Avasimibe [CI 1011] is an ACAT inhibitor that was in development with Parke-Davis (Warner-Lambert) in the USA for the treatment of atherosclerosis and hyperlipidaemia.
This profile has been selected from R&D Insight™, a pharmaceutical intelligence database produced by Adis International Ltd.In June 2000, Warner-Lambert merged with Pfizer and the resulting company retained the Pfizer name. Parke-Davis was integrated into Pfizer Global Research and Development.
Pfizer is continuing development and avasimibe is in Phase III studies. Over 1300 patients have been treated for up to 1 year and initial results from these studies were expected mid-2001. However, they have not been reported. Table I
The pharmacokinetics of avasimibe were examined in two placebo-controlled Phase I trials. In a single-dose study, healthy volunteers received single oral doses of avasimibe (12.5–500mg) in fasted or fed states. At dose levels of 12.5–125mg, ava ...
- Vora J, Stern R, Lathia C. Clinical pharmacokinetics of CI-1011, an ACAT inhibitor. Pharm Res 14 (Suppl): 505, Nov 1997
- Post SM, Zoeteweij JP, Bos MHA, et al. Acyl-coenzyme A: cholesterol acyltransferase inhibitor, avasimibe, stimulates bile acid synthesis and cholesterol 7 alpha-hydroxylase in cultured rat hepatocytes and in vivo in the rat. Hepatology. 30: 491–500, Aug 1999 CrossRef
- Laitinen L, Nicolosi RJ, Krause BR. The ACAT inhibitor, CI-1011 is effective in the prevention and regression of atherogenesis in hamsters. FASEB J 10: 511, Mar 1996
- Wilcox LJ, Hugh P, Barrett R, et al. ApoB100 secretion from HepG2 cells is decreased by the ACAT inhibitor CI-1011: an effect associated with enhanced intracellular degradation of ApoB. Arterioscler Thromb Vasc Biol 19: 939–949, Apr 1999 CrossRef
- Dianne B, Delsing JM, Offerman EH, et al. The acyl-CoA:cholesterol acyltransferase-inhibitor avasimibe reduces atherosclerosis independently of its lipid-lowering effect in apoE3-Leiden mice. Circulation. 100 (Suppl): 613, 2 Nov 1999
Drugs in R & D
Volume 3, Issue 3 , pp 173-174
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