Emerging Field of Biased Opioid Agonists

Abstract

Advances in opioid pharmacology promise to bring a "better opioid." Biased opioid agonists, designed to recruit G protein over β-arrestin signaling, may provide analgesia without adverse effects of traditional opioids. Oliceridine, the first biased opioid agonist, was approved in 2020. In vitro and in vivo data present a complicated picture, with decreased gastrointestinal and respiratory adverse effects but similar abuse potential. Advances in pharmacology will result in new opioids brought to market. However, lessons learned from the past implore appropriate safeguards to patient safety and critical evaluation of the data and science behind new drugs.

Keywords: Agonists; G-protein coupled receptors; Opioids; Perioperative medicine; Pharmacology.