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]

Other namesBMS-986368; CC-97489

Routes of
administrationOral^[1][2]

Drug classFatty acid amide hydrolase (FAAH) inhibitor; Monoacylglycerol lipase (MAGL) inhibitor; Indirect cannabinoid

CAS Number

• 2244136-58-9

Quick facts Clinical data, Other names ...

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
IUPAC name (5-carbamoyl-3-pyridinyl) (2R)-2-methyl-4-[[3-(trifluoromethoxy)phenyl]methyl]piperazine-1-carboxylate
CAS Number	2244136-58-9
PubChem CID	139318505
ChemSpider	129623866
UNII	X3Q33L6UL2
KEGG	D13114
ChEMBL	ChEMBL5917190
Chemical and physical data
Formula	C20H21F3N4O4
Molar mass	438.407 g·mol−1
3D model (JSmol)	Interactive image
SMILES C[C@@H]1CN(CCN1C(=O)OC2=CN=CC(=C2)C(=O)N)CC3=CC(=CC=C3)OC(F)(F)F
InChI 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

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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]