Chemistry:Foliglurax

From HandWiki
Short description: Chemical compound
Foliglurax
Foliglurax tautomer skeletal.svg
Clinical data
Other namesDT2331; PXT-002331; PXT-2331
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC23H23N3O3S
Molar mass421.52 g·mol−1
3D model (JSmol)

Foliglurax (developmental code names PXT-002331, DT2331) is a positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4),[1] which is under development by Prexton Therapeutics for the treatment of Parkinson's disease.[2][3][4] It reached phase II clinical trials,[2] but while it was found to be safe and showed some signs of clinical improvement, it failed to sufficiently distinguish itself from placebo to meet the study endpoints.[5][6]

The other tautomeric form of foliglurax.

References

  1. "Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4". Journal of Medicinal Chemistry 60 (20): 8515–8537. October 2017. doi:10.1021/acs.jmedchem.7b00991. PMID 28902994. 
  2. 2.0 2.1 "Foliglurax - Lundbeck". Adis Insight. Springer Nature Switzerland AG. http://adisinsight.springer.com/drugs/800044176. 
  3. "Current approaches to the treatment of Parkinson's disease". Neuropsychiatric Disease and Treatment 4 (4): 743–57. August 2008. doi:10.1016/j.bmcl.2017.07.075. PMID 19043519. 
  4. "Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4". Expert Opinion on Drug Discovery 13 (5): 411–423. May 2018. doi:10.1080/17460441.2018.1443076. PMID 29486616. 
  5. "Non-Dopaminergic Treatments for Motor Control in Parkinson's Disease: An Update". CNS Drugs 34 (10): 1025–1044. October 2020. doi:10.1007/s40263-020-00754-0. PMID 32785890. 
  6. "A Randomized, Double-Blind, Controlled Phase II Study of Foliglurax in Parkinson's Disease". Movement Disorders 37 (5): 1088–1093. February 2022. doi:10.1002/mds.28970. PMID 35218231.