Cebranopadol effects on ventilatory drive, central nervous system, and pain

Background

Respiratory depression is a possible life-threatening complication following opioid administration, mediated via Mu-opioid receptor (MOP) activation.

Cebranopadol is a first-in-class dual nociceptin/orphanin FQ (NOP) and MOP receptor agonist (dual-NMR agonist) attenuating MOP related side effects.

Cebranopadol administration leads to substantial antinociceptive effects with significantly less MOP-related abuse potential, dependence, and respiratory
depression.

Clinical trials suggest a ceiling for respiratory depression.