Elcubragistat

Last updated

Elcubragistat
Elcubragistat.svg
Clinical data
Other namesABX-1431; ABX1431; Lu-AG06466
Routes of
administration 		Oral [1]
Drug class Monoacylglycerol lipase (MAGL) inhibitor
ATC code
  • None
Identifiers
  • 1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[2-pyrrolidin-1-yl-4-(trifluoromethyl)phenyl]methyl]piperazine-1-carboxylate
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C20H22F9N3O2
Molar mass 507.401 g·mol−1
3D model (JSmol)
  • C1CCN(C1)C2=C(C=CC(=C2)C(F)(F)F)CN3CCN(CC3)C(=O)OC(C(F)(F)F)C(F)(F)F
  • InChI=1S/C20H22F9N3O2/c21-18(22,23)14-4-3-13(15(11-14)31-5-1-2-6-31)12-30-7-9-32(10-8-30)17(33)34-16(19(24,25)26)20(27,28)29/h3-4,11,16H,1-2,5-10,12H2
  • Key:SQZJGTOZFRNWCX-UHFFFAOYSA-N

Elcubragistat (INN Tooltip International Nonproprietary Name; developmental code names ABX-1431, Lu-AG06466) is a monoacylglycerol lipase (MAGL) inhibitor which is or was under development for a variety of indications but has not completed development or been marketed as of 2025. [1] [2] [3] [4] It is taken orally. [1]

Contents

Pharmacology

The drug acts as a highly potent and selective MAGL inhibitor and hence increases brain levels of the endocannabinoid 2-arachidonoylglycerol (2-AG) without affecting levels of anandamide. [3] [4] [5] It produces analgesic and other effects in animals. [3] [4]

Development

Elcubragistat is or was under development by Abide Therapeutics, Lundbeck, and the University of Oxford. [1] [2] [3] As of December 2024, no recent development for fibromyalgia, muscle spasticity, neurological disorders, neuropathic pain, non-ulcer dyspepsia, pain, partial epilepsies, post-traumatic stress disorder (PTSD), and an unspecified indication has been reported, whereas development for Tourette's syndrome has been discontinued. [1] [2] [3] The highest developmental stage that the drug has reached is phase 2 clinical trials. [1] [2]

References

  1. 1 2 3 4 5 6 "Elcubragistat". AdisInsight. 28 December 2024. Retrieved 30 September 2025.
  2. 1 2 3 4 "Delving into the Latest Updates on ABX-1431 with Synapse". Synapse. 13 September 2025. Retrieved 30 September 2025.
  3. 1 2 3 4 5 van Egmond N, Straub VM, van der Stelt M (January 2021). "Targeting Endocannabinoid Signaling: FAAH and MAG Lipase Inhibitors". Annu Rev Pharmacol Toxicol. 61: 441–463. doi:10.1146/annurev-pharmtox-030220-112741. hdl:1887/3158663. PMID   32867595.
  4. 1 2 3 Cisar JS, Weber OD, Clapper JR, Blankman JL, Henry CL, Simon GM, et al. (October 2018). "Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders". J Med Chem. 61 (20): 9062–9084. doi:10.1021/acs.jmedchem.8b00951. PMID   30067909.
  5. ↑ Heins MS, Ferger MD, Voehringer P, Cremers TI, Ferger B (September 2025). "Neurochemical in vivo microdialysis and postmortem tissue analysis of amygdala endocannabinoid levels after MAGL- and FAAH-inhibition in rodents". Neurochem Int. 188 106006. doi:10.1016/j.neuint.2025.106006. PMID   40494414.


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