Chemistry:Irafamdastat
Irafamdastat (INN, USAN; 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][2][3][4][5] It is taken orally.[1][4]
The drug is an irreversible inhibitor of both FAAH and MAGL, with IC50 values of 32 nM and 480 nM, respectively.[3][4][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.[3][4][5] It produces anticonvulsant effects in animals.[4] The drug is described as a potential first-in-class medication.[4][5]
Irafamdastat is under development by Bristol Myers Squibb (via acquisition of Celgene Corporation).[1][2][3] 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][2][5]
See also
- List of investigational agitation drugs
References
- ↑ 1.0 1.1 1.2 1.3 "Celgene Corporation". 27 May 2026. https://adisinsight.springer.com/drugs/800060072.
- ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on Irafamdastat with Synapse". 25 May 2026. https://synapse.patsnap.com/drug/94858edfed8a4cec8a48804d92551051.
- ↑ 3.0 3.1 3.2 3.3 "Enhancing anandamide signalling through fatty acid amide hydrolase inhibition: An update on the pharmacological strategy for treating psychiatric disorders". Translational Psychiatry 16 (1). May 2026. doi:10.1038/s41398-026-04120-4. PMID 42209468.
- ↑ 4.0 4.1 4.2 4.3 4.4 4.5 "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. May 2026. doi:10.1177/13524585261430792. https://journals.sagepub.com/doi/pdf/10.1177/13524585261430792#page=208.
- ↑ 5.0 5.1 5.2 5.3 5.4 "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. 2026. doi:10.1016/j.apmr.2026.02.155.
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