新型抑酸药物钾离子竞争型酸阻滞剂研发进展

Research and development progress of the novel acid suppression drugs potassium-competitive acid blockers

质子泵抑制剂(proton pump inhibitors,PPIs)的问世是酸相关性疾病治疗史上一个重要的里程碑。然而,此类药物存在着一些药动学与药效学上的缺陷。钾离子竞争型酸阻滞剂(potassium-competitive acid blockers,P-CABs)以钾离子竞争性的方式、可逆性地结合于质子泵从而达到抑制胃酸分泌的作用并且具有多种优势。本文回顾了该类药物的研发经历、药理学特点及临床研究,并着重介绍了已上市的瑞伐拉赞和沃诺拉赞,以期为酸相关性疾病的药物治疗提供新的参考。

The advent of proton pump inhibitors represents an important milestone in the treatment of acid related diseases. However,these drugs have some deficiencies in pharmacokinetics and pharmacodynamics. Potassium-competitive acid blockers reversibly bind to proton pumps in a competitive manner with potassium ions,thereby inhibiting gastric acid secretion and having multiple advantages. In order to provide a new reference for the treatment of acid related diseases,the research and development experience and pharmacological characteristics and clinical research of these drugs are reviewed,and the focuses are on the already listed revaprazan and vonoprazan.