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Drugs. 2021 Nov;81(16):1937-1944. doi: 10.1007/s40265-021-01619-6.
Difelikefalin (Korsuva) is a synthetic peptide agonist of the kappa opioid receptor being developed by Cara Therapeutics for the treatment of pruritus. In August 2021, intravenous difelikefalin was approved in the USA for the treatment of moderate-to-severe pruritus associated with chronic kidney disease (CKD) in adults undergoing haemodialysis. Intravenous difelikefalin has also been evaluated for CKD-associated pruritus in patients undergoing haemodialysis in various other countries, with Marketing Authorization Application under regulatory review in the EU and a phase III trial ongoing in Japan. Clinical studies of an oral formulation of difelikefalin have also been completed or are underway in pruritus indications, including pruritus associated with atopic dermatitis, notalgia paraesthetica or primary biliary cholangitis. This article summarizes the milestones in the development of difelikefalin leading to this first approval for CKD-associated pruritus in adults undergoing haemodialysis.
地氟来辛（Korsuva）是一种合成的κ阿片受体激动剂，由 Cara Therapeutics 公司研发，用于治疗瘙痒症。2021 年 8 月，地氟来辛静脉制剂在美国获批，用于治疗接受血液透析的成人慢性肾脏病（CKD）相关的中重度瘙痒。地氟来辛静脉制剂也在接受血液透析的其他国家的 CKD 相关瘙痒症患者中进行了评估，其在欧盟的上市许可申请正在监管审查中，在日本也正在开展 III 期临床试验。地氟来辛口服制剂在瘙痒症适应证中的临床研究也已完成或正在进行，包括特应性皮炎相关瘙痒、感觉异常性股痛或原发性胆汁性胆管炎。本文总结了地氟来辛开发过程中的重要里程碑，最终该药在接受血液透析的成人 CKD 相关瘙痒症中获得批准。
