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Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor. It was originally developed as an antilepic drug, and was shown to significantly reduce plasma total triglyceride and VLDL-cholesterol, but later clinical trials were disappointing. ACAT has also been investigated as a potential therapeutic target for Alzheimer′s disease. Recent studies have looked at the effects of avasimibe in reducing amyloid pathology by limiting generation and increasing clearance of diffusible amyloid-beta (Abeta).
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Keywords: Anti-inflammatory agents, Cardiovascular, Chemical vapor deposition, Clinical, Diabetes, Inflammation, Oxidations, Pharmaceutical, Transcription
The acyl-coenzyme A: cholesterol acyltransferase inhibitor CI-1011 reverses diffuse brain amyloid pathology in aged amyloid precursor protein transgenic mice. Huttunen HJ, Havas D, Peach C, et al. J. Neuropathol. Exp. Neurol. 69(8), 777-88, (2010)
Statin therapy alone and in combination with an acyl-CoA:cholesterol O-acyltransferase inhibitor on experimental atherosclerosis. Worthley SG, Helft G, Corti R, et al. Pathophysiol. Haemost. Thromb. 36(1), 9-17, (2007)
Comparison of intravascular ultrasound and quantitative coronary angiography for the assessment of coronary artery disease progression. Berry C, L'Allier PL, Grégoire J, et al. Circulation 115(14), 1851-7, (2007)
Effect of atherosclerotic regression on total luminal size of coronary arteries as determined by intravascular ultrasound. Tardif JC, Grégoire J, L'Allier PL, et al. Am. J. Cardiol. 98(1), 23-7, (2006)
The ACAT inhibitor avasimibe increases the fractional clearance rate of postprandial triglyceride-rich lipoproteins in miniature pigs. Burnett JR, Telford DE, Barrett PH, et al. Biochim. Biophys. Acta 1738(1-3), 10-8, (2005)
The effect of inhibition of acyl coenzyme A-cholesterol acyltransferase (ACAT) on exercise performance in patients with peripheral arterial disease. Hiatt WR, Klepack E, Nehler M, et al. Vasc. Med. 9(4), 271-7, (2004)
Avasimibe, an ACAT inhibitor, enhances the lipid lowering effect of atorvastatin in subjects with homozygous familial hypercholesterolemia. Raal FJ, Marais AD, Klepack E, et al. Atherosclerosis 171(2), 273-9, (2003)
Avasimibe induces CYP3A4 and multiple drug resistance protein 1 gene expression through activation of the pregnane X receptor. Sahi J, Milad MA, Zheng X, et al. J. Pharmacol. Exp. Ther. 306(3), 1027-34, (2003)
Design features of the Avasimibe and Progression of coronary Lesions assessed by intravascular UltraSound (A-PLUS) clinical trial. Tardif JC, Grégoire J, Lespérance J, et al. Am. Heart J. 144(4), 589-96, (2002)
Anti-atherogenic effects of the acyl-CoA:cholesterol acyltransferase inhibitor, avasimibe (CI-1011), in cultured primary human macrophages. Rodriguez A and Usher DC Atherosclerosis 161(1), 45-54, (2002)
Intracellular mechanisms mediating the inhibition of apoB-containing lipoprotein synthesis and secretion in HepG2 cells by avasimibe (CI-1011), a novel acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor. Taghibiglou C, Van Iderstine SC, Kulinski A, et al. Biochem. Pharmacol. 63(3), 349-60, (2002)
Inhibition of acyl-coenzyme A: cholesterol acyl transferase modulates amyloid precursor protein trafficking in the early secretory pathway. Huttunen HJ, Peach C, Bhattacharyya R, Barren C, Pettingell W, Hutter-Paier B, et al. FASEB J. 11, 3819-28, (2009)
Acyl-coenzyme A: cholesterol acyltransferase inhibitor Avasimibe affect survival and proliferation of glioma tumor cell lines. Bemlih S, Poirier MD, El Andaloussi A. Cancer Biol. Ther. 12, 1025-32, (2010)
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