Chemistry:Icalcaprant
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 (a subsidiary of AbbVie).[2][4] 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
- κ-Opioid receptor § Antagonists
- List of investigational antidepressants § κ-Opioid receptor antagonists
References
- ↑ "Icalcaprant (CVL-354)". https://www.abbvie.com/science/pipeline.html#icalcaprant_(cvl-354).
- ↑ 2.0 2.1 2.2 2.3 2.4 "CVL 354 – Cerevel therapeutics". Adis Insight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800057691.
- ↑ 3.0 3.1 3.2 "ACNP 61st Annual Meeting: Poster Abstracts P271-P540". Neuropsychopharmacology 47 (Suppl 1): 220–370. December 2022. doi:10.1038/s41386-022-01485-0. PMID 36456694.
- ↑ "AbbVie Completes Acquisition of Cerevel Therapeutics" (in en). https://news.abbvie.com/2024-08-01-AbbVie-Completes-Acquisition-of-Cerevel-Therapeutics.
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