Syed Yahiya Y
Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.
Drugs. 2025 Jan;85(1):103-109. doi: 10.1007/s40265-024-02126-0. Epub 2024 Dec 24.
Xanomeline/trospium chloride (COBENFY™), formerly KarXT, is a first-in-class, oral, fixed-dose muscarinic agonist/antagonist combination being developed for use in schizophrenia and Alzheimer's disease psychosis. Xanomeline is thought to confer efficacy by acting as an agonist at M and M muscarinic acetylcholine receptors in the brain, and trospium chloride reduces the peripheral cholinergic adverse events associated with xanomeline. Xanomeline/trospium chloride received its first approval on 26 September 2024 in the USA for the treatment of schizophrenia in adults. This article summarizes the milestones in the development of xanomeline/trospium chloride leading to this first approval for schizophrenia.
昔奈美林/氯化曲司氯铵（COBENFY™，原称KarXT）是首个口服固定剂量的毒蕈碱激动剂/拮抗剂组合药物，正被开发用于治疗精神分裂症和阿尔茨海默病所致精神病。昔奈美林被认为通过作用于大脑中的M1和M4毒蕈碱型乙酰胆碱受体发挥疗效，而氯化曲司氯铵可减少与昔奈美林相关的外周胆碱能不良事件。昔奈美林/氯化曲司氯铵于2024年9月26日在美国首次获批用于治疗成人精神分裂症。本文总结了昔奈美林/氯化曲司氯铵在其首个精神分裂症适应症获批前的研发历程中的重要节点。
