Yi Kun, Sun Wenjie, Yu Wen, Chen Shibiao
Department of Anesthesiology, The First Affiliated Hospital, Jiangxi Medical College, Nanchang University, Nanchang, Jiangxi Province, People's Republic of China.
Drug Des Devel Ther. 2025 Jun 26;19:5415-5430. doi: 10.2147/DDDT.S525471. eCollection 2025.
Opioids can effectively relieve pain but carry risks of addiction and adverse effects. Oliceridine, a G protein-biased μ-Opioid receptor (MOR) agonist, has emerged as a promising safer alternative. By preferentially activating G-protein-biased agonist targeting the μ-opioid receptor while downregulating β-arrestin2 recruitment, oliceridine (Olinvyk) achieves potent analgesia with reduced incidence of opioid-related adverse effects. Supported by robust preclinical data, oliceridine has demonstrated significant clinical potential, prompting global clinical trials to define its optimal indications and therapeutic scenarios. This review synthesizes current evidence on oliceridine's efficacy, safety, and mechanistic specificity across diverse surgical settings, contrasting its profile with conventional opioids. Additionally, we discuss future research priorities, including dose optimization, expansion into chronic pain management, and long-term safety evaluation.
阿片类药物能有效缓解疼痛，但存在成瘾和不良反应风险。奥利替丁是一种G蛋白偏向性μ-阿片受体（MOR）激动剂，已成为一种有前景的更安全替代药物。通过优先激活靶向μ-阿片受体的G蛋白偏向性激动剂，同时下调β-抑制蛋白2的募集，奥利替丁（Olinvyk）实现了强效镇痛，且阿片类药物相关不良反应的发生率降低。在强有力的临床前数据支持下，奥利替丁已展现出显著的临床潜力，促使全球开展临床试验以确定其最佳适应症和治疗方案。本综述综合了当前关于奥利替丁在不同手术场景下的疗效、安全性和机制特异性的证据，并将其与传统阿片类药物进行对比。此外，我们还讨论了未来的研究重点，包括剂量优化、拓展至慢性疼痛管理以及长期安全性评估。
