Rocavorexant

Rocavorexant
Clinical data
Other names	C4X-3256; C4X3256; INDV-2000; INDV2000
Routes of; administration	Oral
Drug class	Orexin OX1 receptor antagonist
Identifiers
	IUPAC name N,6-dimethyl-3-(triazol-2-yl)-N-[(2S)-1-[[5-(trifluoromethyl)pyrazin-2-yl]amino]propan-2-yl]pyridine-2-carboxamide;
CAS Number	2115665-09-1;
PubChem CID	130295635;
ChemSpider	133325612;
UNII	8RJN30TJM6;
Chemical and physical data
Formula	C18H19F3N8O
Molar mass	420.400 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=NC(=C(C=C1)N2N=CC=N2)C(=O)N(C)[C@@H](C)CNC3=NC=C(N=C3)C(F)(F)F;
	InChI InChI=1S/C18H19F3N8O/c1-11-4-5-13(29-25-6-7-26-29)16(27-11)17(30)28(3)12(2)8-23-15-10-22-14(9-24-15)18(19,20)21/h4-7,9-10,12H,8H2,1-3H3,(H,23,24)/t12-/m0/s1; Key:KYPYNXQQCRWPBB-LBPRGKRZSA-N;

Rocavorexant (INNTooltip International Nonproprietary Name; developmental code names C4X-3256 and INDV-2000) is an orexin OX₁ receptor antagonist which is under development for the treatment of opioid-related disorders and other substance-related disorders.^[1]^[2]^[3]^[4] It is taken orally.^[1] The drug is under development by C4X Discovery and/or Indivior.^[1]^[2] As of May 2026, development for all indications has been suspended.^[1] The drug has reached phase 2 clinical trials for opioid-related disorders and phase 1 trials for substance-related disorders.^[1]^[2]^[4]

References

^ ^a ^b ^c ^d ^e ^f "Rocavorexant". AdisInsight. 12 May 2026. Retrieved 5 June 2026.
^ ^a ^b ^c "Delving into the Latest Updates on Rocavorexant with Synapse". Synapse. 9 May 2026. Retrieved 5 June 2026.
^ Raymond JS, Vareed RD, Peters J, James MH (October 2025). "Found in translation: orexin receptor antagonism for the treatment of opioid use disorder". Translational Psychiatry. 15 (1) 432. doi:10.1038/s41398-025-03571-5. PMC 12552597. PMID 41136352.
^ ^a ^b Lorente JS, Sokolov AV, Ferguson G, Schiöth HB, Hauser AS, Gloriam DE (June 2025). "GPCR drug discovery: new agents, targets and indications". Nature Reviews. Drug Discovery. 24 (6): 458–479. doi:10.1038/s41573-025-01139-y. PMID 40033110.