Foliglurax

{{Short description|Chemical compound}}

{{Drugbox

| Verifiedfields =

| Watchedfields =

| verifiedrevid =

| IUPAC_name = 4-[3-[4-nitroso-2-(5H-thieno[3,2-c]pyridin-6-ylidene)chromen-6-yl]propyl]morpholine

| image = Foliglurax tautomer skeletal.svg

| width = 250px

| tradename =

| pregnancy_AU =

| pregnancy_US =

| pregnancy_category =

| legal_AU =

| legal_CA =

| legal_UK =

| legal_US =

| legal_status =

| routes_of_administration =

| bioavailability =

| protein_bound =

| metabolism =

| elimination_half-life =

| excretion =

| CAS_number_Ref =

| CAS_number = 1883329-53-0

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = FR50CP1D6W

| CAS_supplemental =
1883329-51-8 (dihydrochloride)

| class =

| ATC_prefix =

| ATC_suffix =

| ATC_supplemental =

| PubChem = 135565465

| IUPHAR_ligand =

| DrugBank_Ref =

| DrugBank =

| ChemSpiderID_Ref =

| ChemSpiderID = 59718537

| KEGG =

| ChEBI =

| ChEMBL =

| synonyms = DT2331; PXT-002331; PXT-2331

| C=23 | H=23 | N=3 | O=3 | S=1

| SMILES = C1COCCN1CCCC2=CC3=C(C=C2)OC(=C4C=C5C(=CN4)C=CS5)C=C3N=O

| StdInChI_Ref =

| StdInChI = 1S/C23H23N3O3S/c27-25-19-13-22(20-14-23-17(15-24-20)5-11-30-23)29-21-4-3-16(12-18(19)21)2-1-6-26-7-9-28-10-8-26/h3-5,11-15,24H,1-2,6-10H2

| StdInChIKey_Ref =

| StdInChIKey = XHRLGFLGWZIPEE-UHFFFAOYSA-N

}}

Foliglurax (developmental code names PXT-002331, DT2331) is a positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4),{{cite journal | vauthors = 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 | display-authors = 6 | title = 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 = Journal of Medicinal Chemistry | volume = 60 | issue = 20 | pages = 8515–8537 | date = October 2017 | pmid = 28902994 | doi = 10.1021/acs.jmedchem.7b00991 | doi-access = free }} which is under development by Prexton Therapeutics for the treatment of Parkinson's disease.{{cite web | title = Foliglurax - Lundbeck | url = http://adisinsight.springer.com/drugs/800044176 | work = Adis Insight | publisher = Springer Nature Switzerland AG }}{{cite journal | vauthors = Jankovic J, Aguilar LG | title = Current approaches to the treatment of Parkinson's disease | journal = Neuropsychiatric Disease and Treatment | volume = 4 | issue = 4 | pages = 743–57 | date = August 2008 | pmid = 19043519 | doi = 10.1016/j.bmcl.2017.07.075 | pmc = 2536542 }}{{cite journal | vauthors = Volpi C, Fallarino F, Mondanelli G, Macchiarulo A, Grohmann U | title = Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4 | journal = Expert Opinion on Drug Discovery | volume = 13 | issue = 5 | pages = 411–423 | date = May 2018 | pmid = 29486616 | doi = 10.1080/17460441.2018.1443076 | s2cid = 4572251 }} 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.{{cite journal | vauthors = Gonzalez-Latapi P, Bhowmick SS, Saranza G, Fox SH | title = Non-Dopaminergic Treatments for Motor Control in Parkinson's Disease: An Update | journal = CNS Drugs | volume = 34 | issue = 10 | pages = 1025–1044 | date = October 2020 | pmid = 32785890 | doi = 10.1007/s40263-020-00754-0 | s2cid = 221111043 | url = }}{{cite journal | vauthors = Rascol O, Medori R, Baayen C, Such P, Meulien D | title = A Randomized, Double-Blind, Controlled Phase II Study of Foliglurax in Parkinson's Disease | journal = Movement Disorders | volume = 37| issue = 5| pages = 1088–1093| date = February 2022 | pmid = 35218231 | doi = 10.1002/mds.28970 | pmc = 9303267 | s2cid = 247129161 }}

File:Foliglurax skeletal.svgic form of foliglurax.]]

{{Clear left}}

References