治疗腹泻型肠易激综合征新药艾沙度林

Eluxadoline,a new drug for treating diarrhea-predominant irritable bowel syndrome

肠易激综合征(IBS)是常见的功能性胃肠道失调疾病,其中以腹泻型肠易激综合征(IBS-D)居多。但是,目前治疗的手段并不能满足临床需求,特效治疗药物仍然急缺。艾沙度林机制特殊,作用于3个靶点:分别为mu阿片受体激动剂、delta阿片受体拮抗剂、kappa受体激动剂,目前是该类机制中第一个也是唯一一个获批的药物,具有止泻和治疗腹痛的效果,且同时不产生便秘的不良反应。艾沙度林于2015年5月27日在FDA获得批准。本文对其药理作用、药动学、临床研究及不良反应方面做简要综述。

Irritable bowel syndrome（ IBS） is the most common functional gastrointestinal disorder,in which patients with diarrhea-predominant IBS（ IBS-D） comprise a substantial proportion of the overall IBS population.However,many patients have persistent symptoms without effective therapies at present,so the unmet need for special treatment still exists. Eluxadoline is the first and only approved mu-opioid receptor agonist / delta opioid receptor antagonist / kappa-receptor agonist for IBS-D. It has properties of anti diarrheal and abdominal painrelieving without constipation,which may be explained by its mechanism. Eluxadoline is approved by FDA in May27 th 2015. In this paper,we briefly reviewed the pharmacology,pharmacokinetics,clinical studies and adverse events of eluxadoline.