| Routes Of Administration: | Oral administration |
| Class: | Opioid antagonist |
| Cas Number: | 2227384-17-8 |
| Pubchem: | 134540598 |
| Unii: | GNR4JZG668 |
| Chembl: | 5314519 |
| Synonyms: | CVL-354 |
| Iupac Name: | 4-[4-{{((}}(2''S'')-2-(3-methoxy-1-methylpyrazol-4-yl)pyrrolidin-1-yl]methyl]phenoxy]benzamide |
| C: | 23 |
| H: | 26 |
| N: | 4 |
| O: | 3 |
| Smiles: | CN1C=C(C(=N1)OC)[C@@H]2CCCN2CC3=CC=C(C=C3)OC4=CC=C(C=C4)C(=O)N |
| Stdinchi: | 1S/C23H26N4O3/c1-26-15-20(23(25-26)29-2)21-4-3-13-27(21)14-16-5-9-18(10-6-16)30-19-11-7-17(8-12-19)22(24)28/h5-12,15,21H,3-4,13-14H2,1-2H3,(H2,24,28)/t21-/m0/s1 |
| Stdinchikey: | OBDLEFCGVHQDFR-NRFANRHFSA-N |
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.
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.