Discovery of TA-8995 (obicetrapib) as a CETP Inhibitor

DOI
  • Hayashi Norimitsu
    Research Unit/Neuroscience, Sohyaku. Innovative Research Division, Mitsubishi Tanabe Pharma Corporation
  • Kubota Hitoshi
    Mitsubishi Tanabe Pharma Corporation
  • Nakamura Yoshinori
    Mitsubishi Tanabe Pharma Corporation
  • Yamamoto Yasuo
    Research Unit/Frontier, Sohyaku. Innovative Research Division, Mitsubishi Tanabe Pharma Corporation
  • Oka Kozo
    Research Unit/Frontier, Sohyaku. Innovative Research Division, Mitsubishi Tanabe Pharma Corporation

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Other Title
  • 世界最強の作用を有するCETP阻害剤TA-8995（obicetrapib）の創製

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Description

<p>Cholesteryl Ester Transfer Protein (CETP) inhibitors are expected to have anti-atherosclerotic effects by inducing favorable changes in lipoprotein profiles, such as increased HDL-C and decreased LDL-C. In the course of our exploration of structure-activity-relationship based on torcetrapib, “in vivo method that focused on drug development in conventional formulations” and “in vitro method that reflected the effects of in vivo experiments so well” were conducted. As a result, it was found that the carboxylic acid derivatives possessed promising pharmacological effects. After further optimization of carboxylic acid, we successfully discovered highly potent compound TA-8995 (obicetrapib) as a clinical candidate. In the recent clinical studies, TA-8995 showed the strongest LDL-C lowering and HDL-C raising effects in the class of CETP inhibitors.</p>

Journal

  • MEDCHEM NEWS

    MEDCHEM NEWS 29 (3), 128-132, 2019-08-01

    The Pharmaceutical Society of Japan

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