Icalcaprant[1] (developmental code name CVL-354) is an opioid antagonist which is under development for the treatment of major depressive disorder and substance-related disorders.[2][3] It is taken by mouth.[2]

It acts as a selective antagonist of the κ-opioid receptor.[2][3] 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.[3]

It was originated by Pfizer and is under development by Cerevel Therapeutics.[2] 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.[2]

See also

References

  1. ^ "Icalcaprant (CVL-354)". AbbVie. Retrieved 2024-08-15.
  2. ^ a b c d e "CVL 354 – Cerevel therapeutics". Adis Insight. Springer Nature Switzerland AG.
  3. ^ a b c "ACNP 61st Annual Meeting: Poster Abstracts P271-P540". Neuropsychopharmacology. 47 (Suppl 1): 220–370. December 2022. doi:10.1038/s41386-022-01485-0. eISSN 1740-634X. PMC 9714399. PMID 36456694.


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