Irafamdastat
| Clinical data | |
|---|---|
| Other names | BMS-986368; CC-97489 |
| Routes of administration | Oral [1] [2] |
| Drug class | Fatty acid amide hydrolase (FAAH) inhibitor; Monoacylglycerol lipase (MAGL) inhibitor; Indirect cannabinoid |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C20H21F3N4O4 |
| Molar mass | 438.407g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Irafamdastat (INN Tooltip International Nonproprietary Name, USAN Tooltip 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]
The drug is an irreversible inhibitor of both FAAH and MAGL, with IC50 Tooltip half-maximal inhibitory concentration values of 32nM and 480nM, 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
[edit ]References
[edit ]- 1 2 3 4 5 "Celgene Corporation". AdisInsight. 27 May 2026. Retrieved 8 June 2026.
- 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.
- 1 2 3 "Delving into the Latest Updates on Irafamdastat with Synapse". Synapse. 25 May 2026. Retrieved 8 June 2026.
- 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.
{{cite journal}}: CS1 maint: unflagged free DOI (link) - 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年02月15日5.