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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 (1997) Clinical pharmacokinetics of CI-1011, an ACAT inhibitor. Pharm Res 14: pp. 505
- Post, SM, Zoeteweij, JP, Bos, MHA (1999) 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: pp. 491-500 CrossRef
- Laitinen, L, Nicolosi, RJ, Krause, BR (1996) The ACAT inhibitor, CI-1011 is effective in the prevention and regression of atherogenesis in hamsters. FASEB J 10: pp. 511
- Wilcox, LJ, Hugh, P, Barrett, R (1999) 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: pp. 939-949 CrossRef
- Dianne, B, Delsing, JM, Offerman, EH (1999) The acyl-CoA:cholesterol acyltransferase-inhibitor avasimibe reduces atherosclerosis independently of its lipid-lowering effect in apoE3-Leiden mice. Circulation 100: pp. 613
Drugs in R & D
Volume 3, Issue 3 , pp 173-174
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