Opioids are the cornerstone in the treatment of moderate to severe pain but their clinical application is limited by opioid related adverse events. Oliceridine, a new G protein biased µ-opioid receptor agonist can reduce the incidence of ORAE due to its unique pharmacological properties. This review summarizes the pharmacological properties of oliceridine and the clinical studies on its efficacy and safety in the treatment of moderate to severe acute pain, focusing on the clinical studies on the safety of oliceridine in reducing opioid induced respiratory depression and gastrointestinal adverse reactions, and introduces its clinical application value in postoperative analgesia, painless endoscopy and non perioperative pain management such as burn and chronic pain, that it is expected to provide a new option for clinical pain management.