Irafamdastat

Irafamdastat
Clinical data
Other namesBMS-986368; CC-97489
Routes of
administration		Oral
Drug classFatty acid amide hydrolase (FAAH) inhibitor; Monoacylglycerol lipase (MAGL) inhibitor; Indirect cannabinoid
Identifiers
  • (5-carbamoyl-3-pyridinyl) (2R)-2-methyl-4-[[3-(trifluoromethoxy)phenyl]methyl]piperazine-1-carboxylate
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC20H21F3N4O4
Molar mass438.407 g·mol−1
3D model (JSmol)
  • C[C@@H]1CN(CCN1C(=O)OC2=CN=CC(=C2)C(=O)N)CC3=CC(=CC=C3)OC(F)(F)F
  • InChI=1S/C20H21F3N4O4/c1-13-11-26(12-14-3-2-4-16(7-14)31-20(21,22)23)5-6-27(13)19(29)30-17-8-15(18(24)28)9-25-10-17/h2-4,7-10,13H,5-6,11-12H2,1H3,(H2,24,28)/t13-/m1/s1
  • Key:XXDVCULQMDDOAX-CYBMUJFWSA-N

Irafamdastat (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code names BMS-986368 and CC-97489) is a centrally penetrant dual fatty acid amide hydrolase (FAAH) inhibitor and monoacylglycerol lipase (MAGL) inhibitor which is under development for the treatment of agitation, muscle spasticity, and neurological disorders. It is taken orally.

The drug is an irreversible inhibitor of both FAAH and MAGL, with IC50Tooltip half-maximal inhibitory concentration values of 32 nM and 480 nM, respectively. By inhibiting these enzymes, irafamdastat is thought to increase levels of the endocannabinoids anandamide (AEA) and 2-arachidonoylglycerol (2-AG), and thereby to indirectly activate the cannabinoid CB1 and CB2 receptors. It produces anticonvulsant effects in animals. The drug is described as a potential first-in-class medication.

Irafamdastat is under development by Bristol Myers Squibb (via acquisition of Celgene Corporation). As of May 2026, it is in phase 2 clinical trials for agitation and muscle spasticity and is in phase 1 trials for neurological disorders.

See also

References

  1. 1 2 3 4 5 "Celgene Corporation". AdisInsight. 27 May 2026. Retrieved 8 June 2026.
  2. 1 2 3 4 5 6 7 Dines K, Paget K, Steinberg M, Yan Y, Ruiz I, Lopez C, et al. (May 2026). "A Comprehensive Preclinical Characterization of BMS-986368, a First-in-Class, Oral, Dual Inhibitor of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase". Multiple Sclerosis Journal. 32 (2): 227–228. doi:10.1177/13524585261430792.
  3. 1 2 3 "Delving into the Latest Updates on Irafamdastat with Synapse". Synapse. 25 May 2026. Retrieved 8 June 2026.
  4. 1 2 3 4 Couttas TA, Hoffmann AE, Jieu B, Golla FR, Shepherd CE, Leweke FM, et al. (May 2026). "Enhancing anandamide signalling through fatty acid amide hydrolase inhibition: An update on the pharmacological strategy for treating psychiatric disorders". Translational Psychiatry. 16 (1) 288. doi:10.1038/s41398-026-04120-4. PMC 13219800. PMID 42209468.
  5. 1 2 3 4 5 Bethoux F, Coffey M, Carramusa B, Heine W, Miceli R, Gao G, et al. (2026). "Design of a Phase 2, Randomized, Double-blind, Placebo-controlled Trial of BMS-986368, a Fatty Acid Amide Hydrolase/monoacylglycerol Lipase Inhibitor, for Spasticity Treatment in Multiple Sclerosis". Archives of Physical Medicine and Rehabilitation. 107 (5): e62–e63. doi:10.1016/j.apmr.2026.02.155.