Sharma Amol, Herekar Anam Asif, Bhagatwala Jigar, Rao Satish Sc
Division of Gastroenterology and Hepatology, Department of Medicine, Medical College of Georgia, Augusta University, Augusta, GA, USA,
Clin Exp Gastroenterol. 2019 Jan 22;12:31-36. doi: 10.2147/CEG.S145668. eCollection 2019.
Constipation is a multifactorial disorder that can cause significant psychological distress to patients and economic burden on the health care system. Many patients are not satisfied with their current established treatment, highlighting the need for new and improved therapeutic options. Guanylate cyclase-C (GC-C)/cyclic guanosine monophosphate agonists have emerged as a safe and efficacious class of drugs for the treatment of chronic idiopathic constipation (CIC). Plecanatide, a second-in-class, US FDA-approved, synthetic GC-C agonist, has recently been approved in the US for the treatment of irritable bowel syndrome with constipation at doses of 3 and 6 mg and CIC at the 3 mg dosage. In this study, we summarize the design of this novel 16-amino acid uroguanylin analog, drug development through Phase I, II, and III clinical studies, and its role in the treatment of CIC.
便秘是一种多因素疾病，会给患者带来严重的心理困扰，并给医疗保健系统造成经济负担。许多患者对当前已确立的治疗方法不满意，这凸显了对新的、改良的治疗选择的需求。鸟苷酸环化酶-C（GC-C）/环磷酸鸟苷激动剂已成为一类安全有效的治疗慢性特发性便秘（CIC）的药物。普卡那肽是该类中的第二种、经美国食品药品监督管理局（FDA）批准的合成GC-C激动剂，最近在美国已获批用于治疗便秘型肠易激综合征，剂量为3毫克和6毫克，以及用于治疗剂量为3毫克的CIC。在本研究中，我们总结了这种新型16氨基酸尿鸟苷素类似物的设计、通过I期、II期和III期临床研究进行的药物研发，以及它在治疗CIC中的作用。
