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Tegilicine (also known as HSK21542) is a novel, highly selective, peripherally acting kappa opioid receptor (KOR) agonist developed by Sichuan Haisco Pharmaceutical. It is designed to provide potent analgesia and anti-pruritic effects while minimizing the central nervous system (CNS) side effects typically associated with traditional mu-opioid agonists, such as respiratory depression and addiction, as well as the dysphoria and sedation linked to centrally acting KOR agonists. Tegilicine acts primarily on peripheral sensory neurons to modulate pain and itch signaling, avoiding significant penetration of the blood-brain barrier. It is primarily being developed for the management of postoperative pain and chronic kidney disease-associated pruritus (CKD-aP).
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