Emestedastat

Emestedastat
Clinical data
Other namesXanamem; UE-2343; UE2343
Drug class11β-Hydroxysteroid dehydrogenase type 1 inhibitor
Identifiers
  • [(1R,5S)-3-hydroxy-3-pyrimidin-2-yl-8-azabicyclo[3.2.1]octan-8-yl]-[5-(1H-pyrazol-4-yl)thiophen-3-yl]methanone
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC19H19N5O2S
Molar mass381.45 g·mol−1
3D model (JSmol)
  • C1C[C@H]2CC(C[C@@H]1N2C(=O)C3=CSC(=C3)C4=CNN=C4)(C5=NC=CC=N5)O
  • InChI=1S/C19H19N5O2S/c25-17(12-6-16(27-11-12)13-9-22-23-10-13)24-14-2-3-15(24)8-19(26,7-14)18-20-4-1-5-21-18/h1,4-6,9-11,14-15,26H,2-3,7-8H2,(H,22,23)/t14-,15+,19?
  • Key:MMZFGTAMARVHAF-RTHVDDQRSA-N

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]

References

  1. ^ a b c d "UE 2343". AdisInsight. 28 August 2024. Retrieved 9 October 2024.
  2. ^ a b c d 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.