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Canosimibe (AVE5530) is a small molecule cholesterol absorption inhibitor developed as a derivative of ezetimibe. It is designed to be non-soluble and act locally at the luminal surface of the gastrointestinal tract to inhibit cholesterol absorption. Its primary mechanism of action is inhibition of acyl-CoA cholesterol acyltransferase (ACAT), which plays a key role in intestinal cholesterol uptake. Canosimibe was investigated primarily for the treatment of primary hypercholesterolemia, both as monotherapy and in combination with statins such as atorvastatin. Clinical trials reached Phase 3 but were terminated or completed without approval[1][3][4].
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