Discovery of Evocalcet for the Treatment of Secondary Hyperparathyroidism

DOI
  • Miyazaki Hiroshi
    Research Unit/Immunology & Inflammation, Sohyaku. Innovative Research Division, Mitsubishi Tanabe Pharma Corporation
  • Kawata Takehisa
    Medical Affairs, Kyowa Kirin Co., Ltd.
  • Hisada Yutaka
    Research Unit/Immunology & Inflammation, Research Unit/Immunology & Inflammation, Sohyaku. Innovative Research Division, Mitsubishi Tanabe Pharma Corporation
  • Moritani Yasunori
    Human Resources Department, Mitsubishi Tanabe Pharma Corporation
  • Sakurai Osamu
    Global Quality Assurance Department, Mitsubishi Tanabe Pharma Corporation

Bibliographic Information

Other Title
  • 二次性副甲状腺機能亢進症治療薬エボカルセトの創製

Search this article

Description

<p>Cinacalcet hydrochloride is well-used for the treatment of secondary hyperparathyroidism as a CaSR agonist in dialysis patients. However, it is also known that cinacalcet has several issues such as adverse effects on the gastrointestinal tract (e.g., nausea and vomiting) and drug-drug interactions from strong CYP2D6 inhibition. We started the drug discovery efforts targeting CaSR agonists without the defects of cinacalcet, and it leaded the discovery of evocalcet. It shows excellent BA and does not inhibit CYPs such as 2D6. Evocalcet was approved for marketing as Orkedia® that contributes to the achievement of management targets for patients with secondary hyperparathyroidism by taking it once a day and reduces their adverse effects on upper gastrointestinal tracts. This research is an extraordinary drug discovery program where PAM (Positive Allosteric Modulator) of GPCR was succeeded to reach the market.</p>

Journal

  • MEDCHEM NEWS

    MEDCHEM NEWS 30 (2), 78-83, 2020-05-01

    The Pharmaceutical Society of Japan

Keywords

Details 詳細情報について

Report a problem

Back to top