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替那帕诺用于以便秘为主的肠易激综合征。

Tenapanor for constipation-predominant irritable bowel syndrome.

作者信息

Siddiqui S, Cash B D

机构信息

University of Texas Health Science Center at Houston, Division of Gastroenterology, Houston, Texas, USA.

出版信息

Drugs Today (Barc). 2020 Mar;56(3):203-210. doi: 10.1358/dot.2020.56.3.3115214.

Abstract

Irritable bowel syndrome (IBS) is among the most common gastrointestinal disorders encountered in primary and secondary care and is associated with impaired quality of life, increased healthcare utilization, and significant costs to patients and society. There are three primary phenotypes of IBS, categorized according to stool pattern: IBS with diarrhea (IBS-D), IBS with constipation (IBS-C) and IBS with a mixed bowel pattern (IBS-M). The treatment approach to all forms of IBS is typically hierarchal, with initial therapies consisting of dietary and lifestyle modifications. When these interventions are impractical or ineffective, pharmacotherapy with over-the-counter and prescription therapies is often employed. Tenapanor is a locally acting, minimally absorbed, selective small-molecule inhibitor of the intestinal sodium/hydrogen exchanger 3 (NHE3) that was approved in September 2019 by the U.S. Food and Drug Administration (FDA) for IBS-C. This agent works by increasing the sodium level in the intestinal lumen and promoting the efflux of fluid into the gut lumen to maintain osmotic balance in addition to having an antinociceptive effect. Tenapanor has been shown to improve bowel movement frequency/form and abdominal pain in patients with IBS-C. This article will elaborate on the clinical development program for tenapanor for this indication.

摘要

肠易激综合征(IBS)是初级和二级医疗保健中最常见的胃肠道疾病之一,与生活质量受损、医疗保健利用率增加以及患者和社会的巨大成本相关。IBS有三种主要表型,根据粪便模式分类:腹泻型肠易激综合征(IBS-D)、便秘型肠易激综合征(IBS-C)和混合型肠易激综合征(IBS-M)。所有形式的IBS的治疗方法通常是分层的,初始治疗包括饮食和生活方式的改变。当这些干预措施不切实际或无效时,通常会采用非处方和处方药物治疗。替那帕诺是一种局部作用、极少吸收的肠道钠/氢交换蛋白3(NHE3)选择性小分子抑制剂,于2019年9月被美国食品药品监督管理局(FDA)批准用于治疗IBS-C。该药物通过增加肠腔内的钠水平并促进液体流入肠腔以维持渗透平衡,此外还具有抗伤害感受作用。已证明替那帕诺可改善IBS-C患者的排便频率/形式和腹痛。本文将详细阐述替那帕诺针对该适应症的临床开发计划。

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