Synthetic Studies of Vonoprazan Fumarate, a Novel Potassium-Competitive Acid Blocker (P-CAB)

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  • 新規カリウムイオン競合型アシッドブロッカー（P-CAB）ボノプラザンフマル酸塩の合成研究
  • シンキ カリウムイオン キョウゴウガタ アシッドブロッカー(P-CAB)ボノプラザンフマル サンエン ノ ゴウセイ ケンキュウ

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<p>The major target in the pharmacological treatment for acid related diseases is the gastric proton pump enzyme H+,K+-ATPase which is responsible for acid secretion. Potassium-competitive acid blocker (P-CAB), a new class of acid suppressant, inhibits gastric H+,K+-ATPase activity by reversible and K+-competitive binding to the enzyme whereas proton pump inhibitor (PPI) does by forming a covalent bond. In the pursuit of developing a novel P-CAB, a pyrrole derivative was found as a hit compound from high through-put screening (HTS), and its pharmacophore for potent inhibitory activity was identified. Following optimization by focusing on compounds with high ligand-lipophilicity efficiency (LLE) lead to discovery of Vonoprazan Fumarate (Takecab®). This article describes the successful medicinal chemistry activity from a HTS hit compound to the launched drug that will give hope for the patients suffering from acid related diseases not only in Japan but in worldwide.</p>

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