治疗便秘型肠易激综合征新药替那帕诺

Tenapanor: a new drug for the treatment of irritable bowel syndrome with constipation

替那帕诺是Ardelyx公司研发的一种Na+/H+交换蛋白-3(NHE3)抑制剂。它通过抑制肠道NHE3减少肠道对钠离子的吸收,从而增加肠腔水分,软化粪便并缩短肠道转运时间。该药于2019年9月被美国FDA批准上市,用于治疗便秘型肠易激综合征。本文结合近年来国内外相关文献,概述临床试验中替那帕诺的作用机制、药物代谢动力学、临床疗效、安全性等。

Tenapanor is a novel potent inhibitor of the sodium/hydrogen exchanger 3(NHE3) developed by Ardelyx Company. By inhibiting NHE3 on the apical surface of the enterocytes, tenapanor reduces absorption of sodium from the small intestine and colon, resulting in an increase in water secretion into the intestinal lumen, which accelerates intestinal transit time and results in a softer stool consistency. It was approved by FDA in September 2019 for the treatment of irritable bowel syndrome with constipation(IBS-C). In this artical, we summarize its available information, including mechanism of action, pharmacodynamics, pharmacokinetics, clinical efficacy and safety.