Elcubragistat
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| Other names | ABX-1431; ABX1431; Lu-AG06466 |
| Routes of administration | Oral[1] |
| Drug class | Monoacylglycerol lipase (MAGL) inhibitor |
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| Formula | C20H22F9N3O2 |
| Molar mass | 507.401 g·mol−1 |
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Elcubragistat (INN; 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]
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
- ^ a b c d e f "Elcubragistat". AdisInsight. 28 December 2024. Retrieved 30 September 2025.
- ^ a b c d "Delving into the Latest Updates on ABX-1431 with Synapse". Synapse. 13 September 2025. Retrieved 30 September 2025.
- ^ a b c d e 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.
- ^ a b c 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.
- ^ 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. hdl:11370/272cf142-8d7c-420b-81b1-38fb2dce4e30. PMID 40494414.