Discovery of Levodopa Prodrug ONO-2160

DOI
  • Kokubo Masaya
    Ono Pharmaceutical Co., Ltd., Group VI, Division I, Medicinal Chemistry Research Laboratories
  • Kinoshita Atsushi
    ONO Pharmaceutical Co., Ltd., Group IV Division II, Medicinal Chemistry Research Labolatories
  • Kodera Yasuyo
    ONO Pharmaceutical Co., Ltd., Group II Division I, Medicinal Chemistry Research Labolatories
  • Koyanagi Takashi
    ONO Pharmaceutical Co., Ltd., Biomarker Strategy Translational Research Laboratories
  • Maruyama Toru
    ONO Pharmaceutical Co., Ltd., Division I, Medicinal Chemistry Research Labolatories

Bibliographic Information

Other Title
  • レボドパプロドラッグ（ONO-2160）の創製

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Description

<p>Levodopa known as prodrug of dopamine is one of the most powerful agent for treating Parkinson’s disease (PD). However, pharmacokinetic (PK) profile of Levodopa has issue of its metabolism in peripheral caused short duration. To address this PK issue, we inspired to make Levodopa prodrug to improve Levodopa duration in plasma. We synthesized more than 700 compounds and evaluated dog PK study to find ONO-2160 that had good PK profile in animals. ONO-2160 and dopa decarboxylase inhibitor (DCI) combination showed long duration in both dogs and rodents. ONO-2160 and DCI combination also showed good PK profiles in healthy volunteers and PD patients in Phase I study.</p>

Journal

  • MEDCHEM NEWS

    MEDCHEM NEWS 30 (3), 126-132, 2020-08-01

    The Pharmaceutical Society of Japan

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