RTI Health Solutions NC 27709, USA.
Expert Opin Investig Drugs. 2010 Oct;19(10):1257-64. doi: 10.1517/13543784.2010.515209.
Irritable bowel syndrome (IBS) represents one of the most common gastrointestinal disorders, with the diarrhea-predominant form (D-IBS) representing an area of high unmet medical need. One difficulty in identifying suitable treatments for IBS is that although there are animal models for the components of IBS, it is not clear whether animals are afflicted by the disease. In a recently completed Phase II study, the kappa-opioid agonist, asimadoline, was shown to be efficacious in a prospectively defined subgroup of D-IBS patients. This study confirmed a good safety profile for asimadoline.
The chemistry, pharmacology, pharmacokinetics, pharmacodynamics and clinical safety and efficacy of asimadoline in relationship to IBS is reviewed. Papers were searched over the past 20 years using the PubMed database and key words 'asimadoline', 'kappa-opioid agonist' and 'irritable bowel syndrome'. Abstracts were reviewed and appropriate full papers were then evaluated.
The reader will gain an appreciation of kappa-opioid agonists as IBS treatments.
In a prospectively defined, clinically relevant patient subgroup, asimadoline shows efficacy in the treatment of D-IBS.
肠易激综合征（IBS）是最常见的胃肠道疾病之一，以腹泻为主型（D-IBS）代表了一个高度未满足医疗需求的领域。确定 IBS 合适治疗方法的一个困难是，尽管有 IBS 的动物模型，但尚不清楚动物是否患有该疾病。在最近完成的 II 期研究中，κ-阿片受体激动剂阿西马朵林在 D-IBS 患者的一个预先确定的亚组中显示出疗效。这项研究证实了阿西马朵林具有良好的安全性。
本文综述了阿西马朵林在 IBS 方面的化学、药理学、药代动力学、药效学和临床安全性及疗效。在过去 20 年中，使用 PubMed 数据库和关键词“asimadoline”、“kappa-opioid agonist”和“irritable bowel syndrome”搜索了论文。对摘要进行了审查，然后评估了适当的全文。
读者将了解 κ-阿片受体激动剂作为 IBS 治疗药物。
在一个预先确定的、具有临床相关性的患者亚组中，阿西马朵林显示出对 D-IBS 的治疗效果。
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