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

1.  “UE 2343”. AdisInsight. 28 August 2024. Retrieved 9 October 2024.
2.  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.
3.  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.
4.  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