Foliglurax Explained

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, 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]

Notes and References

  1. Charvin D, Pomel V, Ortiz M, Frauli M, Scheffler S, Steinberg E, Baron L, Deshons L, Rudigier R, Thiarc D, Morice C, Manteau B, Mayer S, Graham D, Giethlen B, Brugger N, Hédou G, Conquet F, Schann S . 6 . 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 . 28902994 . 10.1021/acs.jmedchem.7b00991 . free .
  2. Web site: Foliglurax - Lundbeck . Adis Insight . Springer Nature Switzerland AG .
  3. Jankovic J, Aguilar LG . Current approaches to the treatment of Parkinson's disease . Neuropsychiatric Disease and Treatment . 4 . 4 . 743–57 . August 2008 . 19043519 . 10.1016/j.bmcl.2017.07.075 . 2536542 .
  4. Volpi C, Fallarino F, Mondanelli G, Macchiarulo A, Grohmann U . Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4 . Expert Opinion on Drug Discovery . 13 . 5 . 411–423 . May 2018 . 29486616 . 10.1080/17460441.2018.1443076 . 4572251 .
  5. Gonzalez-Latapi P, Bhowmick SS, Saranza G, Fox SH . Non-Dopaminergic Treatments for Motor Control in Parkinson's Disease: An Update . CNS Drugs . 34 . 10 . 1025–1044 . October 2020 . 32785890 . 10.1007/s40263-020-00754-0 . 221111043 .
  6. Rascol O, Medori R, Baayen C, Such P, Meulien D . A Randomized, Double-Blind, Controlled Phase II Study of Foliglurax in Parkinson's Disease . Movement Disorders . 37. 5. 1088–1093. February 2022 . 35218231 . 10.1002/mds.28970 . 9303267 . 247129161 .

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