Opioid receptors μOR, δOR, κOR and NOPR are all G protein-coupled receptors (GPCRs), which mainly function through G protein and β-arrestin. Recent studies have found that G protein mediates analgesia, while β-arrestin reduces analgesia and is related to the side effects of opioids. Oliceridine is the first biased μOR agonist approved for commerce. It mainly exerts analgesic effect by activating G protein. It has rapid onset of action and reliable analgesic effect. Due to its low activity on β-arrestin, the incidence of side effects is low, comparing to the classic opioid morphine. Oliceridine can be safely used in patients with liver or kidney insufficiency and its metabolite is inactive. This article summarizes the current progress of pharmacological research and clinical application of oliceridine, aiming to provide reference for the clinical practice of oliceridine.