Chemistry:Elcubragistat
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
- ↑ 1.0 1.1 1.2 1.3 1.4 "Elcubragistat". 28 December 2024. https://adisinsight.springer.com/drugs/800042817.
- ↑ 2.0 2.1 2.2 2.3 "Delving into the Latest Updates on ABX-1431 with Synapse". 13 September 2025. https://synapse.patsnap.com/drug/a75228c00f0e4f579a951d3d4e8862c5.
- ↑ 3.0 3.1 3.2 3.3 3.4 "Targeting Endocannabinoid Signaling: FAAH and MAG Lipase Inhibitors". Annu Rev Pharmacol Toxicol 61: 441–463. January 2021. doi:10.1146/annurev-pharmtox-030220-112741. PMID 32867595.
- ↑ 4.0 4.1 4.2 "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. October 2018. doi:10.1021/acs.jmedchem.8b00951. PMID 30067909.
- ↑ "Neurochemical in vivo microdialysis and postmortem tissue analysis of amygdala endocannabinoid levels after MAGL- and FAAH-inhibition in rodents". Neurochem Int 188. September 2025. doi:10.1016/j.neuint.2025.106006. PMID 40494414.
 |  |
