Overview and Prospects of the Clinical Application of Oliceridine

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.