Development of Epalrestat (Kinedak): Aldose Reductase Inhibitor.

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  • KAWAMURA Masanori
    Ono Pharmaceutical Co., Ltd. Fukui Research Institute, Chemical Process Research Laboratories
  • HAMANAKA Nobuyuki
    Ono Pharmaceutical Co., Ltd. Minase Research Institute, Medicinal Chemistry Laboratories

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  • 糖尿病合併症の治療薬，アルドース還元酸素阻害エパルレスタット（キネダック）の開発とその企業化
  • トウニョウビョウ ガッペイショウ ノ チリョウヤク アルドース カンゲン コウ

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It is believed that the aldose reductase (AR, EC 1.1.21), the initial enzyme of sorbitol pathway, plays a significant role in the initiation of diabetic complications. In a search for AR inhibitors, a series of 4-oxo-2-thioxothiazolidine-3-acetic acid derivatives was synthesized and showed the inhibitory activity against AR. (Z, E) -5- (2-Methyl-3-phenyl-2-propenylidene) -4-oxo-2-thioxothiazolidine-3-acetic acid (epalrestat) prevented the accumulation of sorbitol in rat sciatic nerve and rat blood cell, and improved motor nerve conduction velocity of diabetic rats. In clinical studies, epalrestat has shown the improvements in nerve function and subjective symptoms. In Japan, epalrestat was introduced on the market in January, 1992.

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