Discovery of the First in Class Drug for Intractable Itch, Nalfurafine Hydrochloride

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  • 新規メカニズムに基づく難治性そう痒症治療薬ナルフラフィン塩酸塩の創出
  • シンキ メカニズム ニ モトズク ナンチセイソウ ヨウショウ チリョウヤク ナルフラフィン エンサンエン ノ ソウシュツ

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Abstract

Nalfurafine hydrochloride (1) was launched on March of 2009 in Japan as the first in class non-narcotic opioid drug for intractable itch caused by haemodialysis. Rational medicinal chemistry effort led us to obtain the morphinan derivative, which is a new chemical class of opioid κ-agonist without the [N-C-C-N(sp2)] pharmacophore sequence of the typical U-50488H derivatives. The applicability of “Message-Address Concept” and “Accessory Site Hypothesis” in the development of the opioid κ-agonist could also be proven. Nalfurafine hydrochloride (1) showed significant opioid κ-agonist activity and induced neither aversion nor preference in rats on the CPP (Conditioned Place Preference) test. No dependence sign was observed in monkey on the self-administration test. This compound was approved without legal narcotic nor psychotropic drug control after a clinical evaluation on human. Details on design rationale and medicinal chemistry of this novel drug will be discussed.

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