Oliceridine, a G protein-selective ligand at the μ-opioid receptor, for the management of moderate to severe acute pain.

Oliceridine is a next-generation investigational intravenous opioid that is a G protein-selective agonist at the μ-opioid receptor. The G protein selectivity of this compound results in potent analgesia with substantially reduced recruitment of β-arrestin, a signaling pathway associated with opioid-related adverse events. In randomized, placebo- and active-controlled clinical studies, use of oliceridine for the management of moderate to severe acute pain provided potent analgesic effect superior to that observed with placebo, with lower incidence of adverse events, including respiratory events and gastrointestinal events of nausea and vomiting, compared with morphine. Here, we provide a review of the preclinical and clinical data of intravenous oliceridine, a selective agonist, which has the potential to offer a wider therapeutic window than conventional opioids.