Chey William D, Lembo Anthony J, Rosenbaum David P
Division of Gastroenterology, Department of Medicine, University of Michigan Health System, Ann Arbor, Michigan, USA.
Division of Gastroenterology, Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts, USA.
Am J Gastroenterol. 2017 May;112(5):763-774. doi: 10.1038/ajg.2017.41. Epub 2017 Feb 28.
Tenapanor is a first-in-class, small-molecule inhibitor of the gastrointestinal sodium/hydrogen exchanger NHE3. This study assessed the efficacy and safety of tenapanor in patients with constipation-predominant irritable bowel syndrome (IBS-C).
In this phase 2, double-blind study, patients with IBS-C (Rome III criteria) were randomized (1:1:1:1) to receive tenapanor 5 mg, 20 mg, or 50 mg b.i.d., or placebo b.i.d. for 12 weeks. The primary end point was the complete spontaneous bowel movement (CSBM) responder rate, defined as the proportion of patients reporting an increase from baseline of ≥1 CSBM/week for ≥6/12 treatment weeks. Secondary end points included abdominal symptom responder rates (≥30% score improvement from baseline for ≥6/12 weeks) and a composite responder rate (CSBM and abdominal pain response in the same week for ≥6/12 weeks).
Overall, 356 patients were randomized (mean age: 45.7 years; 86.8% women) and 304 completed the study. The CSBM responder rate was significantly higher in the tenapanor 50 mg b.i.d. group than in the placebo group (60.7 vs. 33.7%; P<0.001), as was the composite responder rate (50.0 vs. 23.6%; P<0.001). Responder rates for abdominal symptoms (pain, discomfort, bloating, cramping, and fullness) were significantly higher in the tenapanor 50 mg b.i.d. group than in the placebo group (all P<0.05). Diarrhea was the most frequent adverse event (tenapanor b.i.d.: 20 mg, 12.4%; 50 mg, 11.2%).
Tenapanor 50 mg b.i.d. significantly increased stool frequency and reduced abdominal symptoms in patients with IBS-C. Further research into tenapanor as a potential treatment for these patients is justified.
替那帕诺是一种一流的胃肠道钠/氢交换体NHE3小分子抑制剂。本研究评估了替那帕诺治疗以便秘为主的肠易激综合征(IBS-C)患者的疗效和安全性。
在这项2期双盲研究中,符合IBS-C(罗马III标准)的患者按1:1:1:1随机分组,接受替那帕诺5mg、20mg或50mg每日两次,或安慰剂每日两次,治疗12周。主要终点是完全自主排便(CSBM)应答率,定义为报告在≥6/12个治疗周内每周CSBM较基线增加≥1次的患者比例。次要终点包括腹部症状应答率(≥6/12周内较基线评分改善≥30%)和综合应答率(≥6/12周内同一周出现CSBM和腹痛反应)。
总体而言,356例患者被随机分组(平均年龄:45.7岁;86.8%为女性),304例完成研究。替那帕诺50mg每日两次组的CSBM应答率显著高于安慰剂组(60.7%对33.7%;P<0.001),综合应答率也是如此(50.0%对23.6%;P<0.001)。替那帕诺50mg每日两次组腹部症状(疼痛、不适、腹胀、绞痛和饱腹感)的应答率显著高于安慰剂组(所有P<0.05)。腹泻是最常见的不良事件(替那帕诺每日两次:20mg组为12.4%;50mg组为11.2%)。
替那帕诺50mg每日两次显著增加了IBS-C患者的排便频率并减轻了腹部症状。对替那帕诺作为这些患者潜在治疗方法进行进一步研究是合理的。