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Remarks
TAP311 is a novel, piperidine-based inhibitor of cholesteryl ester transfer protein (CETP). It has a core structure distinct from other reported CETP inhibitors. CETP inhibitors have therapeutic potential against coronary heart disease as they mediate chemical exchange involving cholesterol. TAP311 has a limited lipophilicity, improving pharmacological profile. It is under clinical trials.
References
1: Yamada K, Brousseau M, Honma W, Iimura A, Imase H, Iwaki Y, Kawanami T, LaSala D, Liang G, Mitani H, Nonomura K, Ohmori O, Pan M, Rigel DF, Umemura I, Yasoshima K, Zhu G, Mogi M. Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma. J Med Chem. 2017 Oct 16. doi: 10.1021/acs.jmedchem.7b00900. [Epub ahead of print] PubMed PMID: 29035537.