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Tegilerdin fumarate (HSK21542) is a peripherally acting, highly selective kappa opioid receptor (KOR) agonist developed by Sichuan Haisco Pharmaceutical. By targeting KORs located on peripheral sensory nerve endings, tegilerdin provides analgesic and anti-pruritic effects while avoiding the central nervous system-mediated side effects, such as respiratory depression, addiction, and dysphoria, commonly associated with mu-opioid agonists or centrally acting KOR agonists. The drug was approved by the China National Medical Products Administration (NMPA) in June 2024 for the treatment of postoperative pain and is also undergoing clinical evaluation for the management of chronic kidney disease-associated pruritus (CKD-aP) in patients on hemodialysis.
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