- Source: Icalcaprant
Icalcaprant (developmental code name CVL-354) is an opioid antagonist which is under development for the treatment of major depressive disorder and substance-related disorders. It is taken by mouth.
It acts as a selective antagonist of the κ-opioid receptor. The drug is also more weakly an antagonist of the μ-opioid receptor, with about 31-fold lower affinity and 27-fold lower inhibitory potency at the μ-opioid receptor relative to the κ-opioid receptor.
It was originated by Pfizer and is under development by Cerevel Therapeutics. As of September 2022, icalcaprant is in phase 1 clinical trials for major depressive disorder and is in the preclincal stage of development for substance-related disorders.
See also
κ-Opioid receptor § Antagonists
List of investigational antidepressants § κ-Opioid receptor antagonists
