Emestedastat
CAS 1346013-80-6
MF C19H19N5O2S MW381.5 g/mol
[(1R,3r,5S)-3-hydroxy-3-(pyrimidin-2-yl)-8-azabicyclo[3.2.1]octan-8-yl][5-(1H-pyrazol-4-yl)thiophen-3-yl]methanone
11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor, UE-2343, UE 2343, 106ELK29GH
Emestedastat (proposed brand name Xanamem; developmental code name UE-2343) is a steroidogenesis inhibitor which is under development for the treatment of major depressive disorder, Alzheimer’s disease, and fragile X syndrome.[1][2] It specifically acts as a centrally penetrant inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) and thereby inhibits the synthesis of the glucocorticoid steroid hormone cortisol.[1][3][4][2] As of August 2024, emestedastat is in phase 2 clinical trials for major depressive disorder and Alzheimer’s disease and is in the preclinical stage of development for fragile X syndrome.[1][2] Clinical effectiveness for Alzheimer’s disease has been mixed.[2] It was originated by the University of Edinburgh and is being developed by Actinogen Medical.[1]
- Phase I MAD, Fed-Fasted, CSF Study of UE2343 in Healthy SubjectsCTID: NCT02616445Phase: Phase 1Status: CompletedDate: 2025-01-22
- Effect of 10 mg Xanamem on Dementia Due to Alzheimer’s DiseaseCTID: NCT06125951Phase: Phase 2Status: Active, not recruitingDate: 2025-12-02
- A Phase I Study of Oral UE2343 in Healthy SubjectsCTID: NCT01770886Phase: Phase 1Status: CompletedDate: 2013-07-17
- Xanamem™ in Healthy Elderly SubjectsCTID: NCT03830762Phase: Phase 1Status: CompletedDate: 2025-01-22
- OriginatorUniversity of Edinburgh
- DeveloperActinogen Medical
- ClassAntidementias; Azabicyclo compounds; Ketones; Pyrazoles; Pyrimidines; Small molecules; Thiophenes
- Mechanism of Action11-beta-hydroxysteroid dehydrogenase type 1 inhibitors
- Phase II/IIIAlzheimer’s disease
- Phase IIMajor depressive disorder
- No development reportedFragile X syndrome
- 15 Sep 2025Meeting similar to that of Type C will be held for Alzheimer’s disease (AD) with European Medicines Agency and subsequently with the UK MHRA and other regulators in 2026
- 27 Aug 2025Pharmacokinetics data from a phase I pharmacokinetics trial in volunteers released by Actinogen
- 28 Jul 2025No recent reports of development identified for preclinical development in Fragile-X-syndrome in Australia (PO)
Syn
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2022094668&_cid=P20-MKKJLN-11715-1
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2021062472&_cid=P20-MKKJLN-11715-1
PAT
- medical cognitive therapyPublication Number: CN-114761005-APriority Date: 2019-09-30
- Medicinal cognitive treatmentsPublication Number: CA-3152902-A1Priority Date: 2019-09-30
- Therapeutic editingPublication Number: AU-2020395113-A1Priority Date: 2019-12-02
- Medicinal cognitive treatmentsPublication Number: EP-4037684-A1Priority Date: 2019-09-30
- Medicinal cognitive treatmentsPublication Number: US-2023000843-A1Priority Date: 2019-09-30
- Medicinal cognitive treatmentsPublication Number: WO-2021062472-A1Priority Date: 2019-09-30
- Cognitive pharmacological treatmentPublication Number: JP-2022550221-APriority Date: 2019-09-30
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References
- “UE 2343”. AdisInsight. 28 August 2024. Retrieved 9 October 2024.
- Seckl J (January 2024). “11β-Hydroxysteroid dehydrogenase and the brain: Not (yet) lost in translation”. Journal of Internal Medicine. 295 (1): 20–37. doi:10.1111/joim.13741. PMID 37941106.
- Bachurin SO, Gavrilova SI, Samsonova A, Barreto GE, Aliev G (March 2018). “Mild cognitive impairment due to Alzheimer disease: Contemporary approaches to diagnostics and pharmacological intervention”. Pharmacological Research. 129: 216–226. doi:10.1016/j.phrs.2017.11.021. PMID 29170097.
- Canet G, Hernandez C, Zussy C, Chevallier N, Desrumaux C, Givalois L (2019). “Is AD a Stress-Related Disorder? Focus on the HPA Axis and Its Promising Therapeutic Targets”. Frontiers in Aging Neuroscience. 11 269. doi:10.3389/fnagi.2019.00269. PMC 6776918. PMID 31611783.
///////////emestedastat, 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor, UE-2343, UE 2343, 106ELK29GH