Icalcaprant
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| Other names | CVL-354 |
| Routes of administration | Oral administration |
| Drug class | Opioid antagonist; κ-Opioid receptor antagonist |
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| Chemical and physical data | |
| Formula | C23H26N4O3 |
| Molar mass | 406.486 g·mol−1 |
| 3D model (JSmol) | |
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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
[edit]- κ-Opioid receptor § Antagonists
- List of investigational antidepressants § κ-Opioid receptor antagonists
References
[edit]- ^ "Icalcaprant (CVL-354)". AbbVie. Retrieved 2024-08-15.
- ^ a b c d e "CVL 354 – Cerevel therapeutics". Adis Insight. Springer Nature Switzerland AG.
- ^ 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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