钾离子竞争性酸阻滞剂的药学特征研究进展

Progress on pharmaceutical characteristics of potassium-competitive acid blocker

钾离子竞争性酸阻滞剂(P-CAB)是一类新型抑酸药,通过与H^(+),K^(+)-ATP酶的K^(+)结合位点附近可逆结合,抑制其构象转变而无法完成H^(+)、K^(+)交换,以K^(+)竞争性的方式抑制胃酸分泌。P-CAB独特的结构与新颖的作用机制赋予其优于其他质子泵抑制剂(PPI)的药学特征,使其成为了酸相关性疾病(ARDs)的新选择。就P-CAB的药学特征展开综述。

As a new class of acid inhibitors,potassium-competitive acid blocker(P-CAB)inhibits the conformational transition of H^(+),K^(+)-ATPase with subsequent suppression of H^(+),K^(+)exchanging by binding reversibly near the K^(+)binding site of H^(+),K^(+)-ATPase,which results in the inhibition of gastric acid secretion in a K^(+)-competitive manner.The unique structure and novel mechanism of P-CAB contribute to the pharmaceutical characteristics superior to other PPIs,making it a new alternative for acidrelated diseases(ARDs).Progress on pharmaceutical characteristics of P-CAB were reviewed in this paper.