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引用次数: 0
摘要
替吉利定(Tegileridine)是江苏恒瑞医药股份有限公司开发的一种小分子μ-阿片受体偏性激动剂,用于治疗术后疼痛。替格列净可选择性地激活 G 蛋白偶联通路,该通路介导强烈的中枢镇痛作用,而对与呼吸抑制和胃肠道功能障碍等不良反应有关的 β-阿司匹林-2通路的激活作用较弱。2024 年 1 月,替格列奈首次在中国获批用于治疗中重度腹部手术后疼痛。本文总结了替吉利定开发过程中的里程碑事件,这些事件促成了替吉利定首次获批用于治疗腹部手术后的中重度疼痛。
Tegileridine () is a small molecule μ-opioid receptor biased agonist developed by Jiangsu Hengrui Pharmaceuticals Co., Ltd for the treatment of postoperative pain. Tegileridine selectively activates the G-protein-coupled pathway, which mediates strong central analgesic effects and only weakly activates the β-arrestin-2 pathway implicated in adverse events like respiratory depression and gastrointestinal dysfunction. In January 2024, tegileridine received its first approval in China for the treatment of moderate to severe pain after abdominal surgery. This article summarizes the milestones in the development of tegileridine leading to this first approval for the treatment of moderate to severe pain after abdominal surgery.
期刊介绍:
Drugs is a journal that aims to enhance pharmacotherapy by publishing review and original research articles on key aspects of clinical pharmacology and therapeutics. The journal includes:
Leading/current opinion articles providing an overview of contentious or emerging issues.
Definitive reviews of drugs and drug classes, and their place in disease management.
Therapy in Practice articles including recommendations for specific clinical situations.
High-quality, well designed, original clinical research.
Adis Drug Evaluations reviewing the properties and place in therapy of both newer and established drugs.
AdisInsight Reports summarising development at first global approval.
Moreover, the journal offers additional digital features such as animated abstracts, video abstracts, instructional videos, and podcasts to increase visibility and educational value. Plain language summaries accompany articles to assist readers with some knowledge of the field in understanding important medical advances.