Icalcaprant

Icalcaprant
Clinical data
Other names	CVL-354
Routes of; administration	Oral
Drug class	κ-Opioid receptor antagonist
Identifiers
	IUPAC name 4-[4-{{(2S)-2-(3-methoxy-1-methylpyrazol-4-yl)pyrrolidin-1-yl]methyl]phenoxy]benzamide;
CAS Number	2227384-17-8;
PubChem CID	134540598;
UNII	GNR4JZG668;
KEGG	D13002;
ChEMBL	ChEMBL5314519;
Chemical and physical data
Formula	C23H26N4O3
Molar mass	406.486 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1C=C(C(=N1)OC)[C@@H]2CCCN2CC3=CC=C(C=C3)OC4=CC=C(C=C4)C(=O)N;
	InChI InChI=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; Key:OBDLEFCGVHQDFR-NRFANRHFSA-N;

Icalcaprant (developmental code name CVL-354) is a κ-opioid receptor (KOR) 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 KOR. The drug is also more weakly an antagonist of the μ-opioid receptor (MOR), with about 31-fold lower affinity and 27-fold lower inhibitory potency at the MOR relative to the KOR.

It was originated by Pfizer and is under development by Cerevel Therapeutics (a subsidiary of AbbVie). 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.