Wikipedia

Irafamdastat

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.[1][3][4][2][5] It is taken orally.[1][2]

Irafamdastat
Clinical data
Other namesBMS-986368; CC-97489
Routes of
administration		Oral[1][2]
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

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.[4][2][5] 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.[4][2][5] It produces anticonvulsant effects in animals.[2] The drug is described as a potential first-in-class medication.[2][5]

Irafamdastat is under development by Bristol Myers Squibb (via acquisition of Celgene Corporation).[1][3][4] 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.[1][3][5]

See also

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References

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  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.
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