介绍一种治疗慢性肾病相关性瘙痒的新药:Difelikefalin  

Introducing a new drug for the treatment of pruritus associated with chronic kidney disease:Difelikefalin

作　　者：张文竹[1] 赵艳[1] 初晓[1] ZHANG Wen-zhu;ZHAO Yan;CHU Xiao(Clinical Pharmacological Research Department,Qingdao Municipal Hospital,Qingdao 266011,Shandong Province,China)

机构地区：[1]青岛市市立医院药理基地,山东青岛266011

出　　处：《中国临床药理学杂志》2022年第12期1401-1404,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：Difelikefalin是2021年8月由美国食品药品监督管理局批准的首个用于成人血液透析患者中重度慢性肾病相关性瘙痒(CKD-aP)的治疗药物。Difelikefalin是一种外周选择性κ-阿片受体(KOR)激动药,通过激活外周神经元和免疫细胞上的KOR发挥止痒作用,其外周特异性限制了对中枢神经系统KOR的影响,从而避免了阿片类药物的副作用。本文从Difelikefalin作用机制、药物临床前药效学研究、临床前毒理学研究、药代动力学、临床研究及安全性等方面作一介绍。Difelikefalin was the first drug approved by the US Food and Drug Administration(FDA) in August 2021 for the treatment of moderate-to-severe pruritus associated with chronic kidney disease(CKD-aP) in adults undergoing hemodialysis. Difelikefalin is a peripherally restricted, selective kappa opioid receptor(KOR) agonist that exerts antipruritic effects by means of activation of KORs on peripheral neurons and immune cells. Its peripheral specificity limits the impact on KORs within the central nervous system, thereby avoiding the side effects of opioids. This paper reviews the mechanism preclinical pharmacodynamics, preclinical toxicology, pharmacokinetics, clinical research and safety of difelikefalin.

关 键 词：difelikefalin 慢性肾病相关性瘙痒 κ-阿片受体激动药 

分 类 号：R97[医药卫生—药品]