Overview and Prospects of the Clinical Application of Oliceridine.

IF 4.7 2区医学 Q1 CHEMISTRY, MEDICINAL

Drug Design, Development and Therapy Pub Date : 2025-06-26 eCollection Date: 2025-01-01 DOI:10.2147/DDDT.S525471

Kun Yi, Wenjie Sun, Wen Yu, Shibiao Chen

引用次数: 0

Abstract

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.

查看原文本刊更多论文

橄榄碱的临床应用综述与展望。

阿片类药物可以有效缓解疼痛，但有成瘾和不良反应的风险。胆碱是一种G蛋白偏倚μ-阿片受体（MOR）激动剂，已成为一种有希望的更安全的替代品。Olinvyk通过优先激活靶向μ-阿片受体的g蛋白偏向激动剂，同时下调β-arrestin2的募集，实现强效镇痛，降低阿片相关不良反应的发生率。在强有力的临床前数据支持下，奥利胆啶已显示出显著的临床潜力，促使全球临床试验确定其最佳适应症和治疗方案。这篇综述综合了目前关于橄榄碱在不同手术环境下的有效性、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了对比。此外，我们讨论了未来的研究重点，包括剂量优化，扩展到慢性疼痛管理和长期安全性评估。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Drug Design, Development and Therapy CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY

CiteScore

9.00

自引率

0.00%

发文量

382

审稿时长

>12 weeks

期刊介绍： Drug Design, Development and Therapy is an international, peer-reviewed, open access journal that spans the spectrum of drug design, discovery and development through to clinical applications. The journal is characterized by the rapid reporting of high-quality original research, reviews, expert opinions, commentary and clinical studies in all therapeutic areas. Specific topics covered by the journal include: Drug target identification and validation Phenotypic screening and target deconvolution Biochemical analyses of drug targets and their pathways New methods or relevant applications in molecular/drug design and computer-aided drug discovery* Design, synthesis, and biological evaluation of novel biologically active compounds (including diagnostics or chemical probes) Structural or molecular biological studies elucidating molecular recognition processes Fragment-based drug discovery Pharmaceutical/red biotechnology Isolation, structural characterization, (bio)synthesis, bioengineering and pharmacological evaluation of natural products** Distribution, pharmacokinetics and metabolic transformations of drugs or biologically active compounds in drug development Drug delivery and formulation (design and characterization of dosage forms, release mechanisms and in vivo testing) Preclinical development studies Translational animal models Mechanisms of action and signalling pathways Toxicology Gene therapy, cell therapy and immunotherapy Personalized medicine and pharmacogenomics Clinical drug evaluation Patient safety and sustained use of medicines.