balipodect

{{Short description|Abandoned PDE10A inhibitor}}

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{{Infobox drug

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| image = Balipodect.svg

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| class = Phosphodiesterase inhibitor; PDE10A inhibitor; Antipsychotic

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| CAS_number = 1238697-26-1

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| PubChem = 46848915

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| DrugBank = DB14774

| ChemSpiderID = 35035198

| UNII = 6650W303H0

| KEGG = D11245

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| ChEMBL = 3989972

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| synonyms = TAK-063; TAK063

| IUPAC_name = 1-(2-fluoro-4-pyrazol-1-ylphenyl)-5-methoxy-3-(2-phenylpyrazol-3-yl)pyridazin-4-one

| C=23 | H=17 | F=1 | N=6 | O=2

| SMILES = COC1=CN(N=C(C1=O)C2=CC=NN2C3=CC=CC=C3)C4=C(C=C(C=C4)N5C=CC=N5)F

| StdInChI = 1S/C23H17FN6O2/c1-32-21-15-29(19-9-8-17(14-18(19)24)28-13-5-11-25-28)27-22(23(21)31)20-10-12-26-30(20)16-6-3-2-4-7-16/h2-15H,1H3

| StdInChIKey = KVHRYLNQDWXAGI-UHFFFAOYSA-N

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Balipodect ({{Abbrlink|INN|International Nonproprietary Name}}, {{Abbrlink|USAN|United States Adopted Name}}; developmental code name TAK-063) is a selective phosphodiesterase 10A (PDE10A) inhibitor which was under development by Takeda for the treatment of schizophrenia.{{cite web | title=Balipodect | website=AdisInsight | date=30 January 2018 | url=https://adisinsight.springer.com/drugs/800036538 | access-date=19 October 2024}}{{cite web | title=Delving into the Latest Updates on Balipodect with Synapse | website=Synapse | date=19 September 2024 | url=https://synapse.patsnap.com/drug/a81359946a1d416886e944e1e1d05839 | access-date=19 October 2024}}{{cite journal | vauthors = Suzuki K, Kimura H | title = TAK-063, a novel PDE10A inhibitor with balanced activation of direct and indirect pathways, provides a unique opportunity for the treatment of schizophrenia | journal = CNS Neuroscience & Therapeutics | volume = 24 | issue = 7 | pages = 604–614 | date = July 2018 | pmid = 29318783 | pmc = 6489916 | doi = 10.1111/cns.12798 }}

It is active in animal models of antipsychotic-like activity, including inhibition of hyperlocomotion induced by the NMDA receptor antagonist dizocilpine (MK-801) or the dopamine releasing agent methamphetamine, inhibition of conditioned avoidance responses, and reversal of prepulse inhibition deficits.{{cite journal | vauthors = Menniti FS, Chappie TA, Schmidt CJ | title = PDE10A Inhibitors-Clinical Failure or Window Into Antipsychotic Drug Action? | journal = Frontiers in Neuroscience | volume = 14 | issue = | pages = 600178 | date = 2020 | pmid = 33551724 | pmc = 7855852 | doi = 10.3389/fnins.2020.600178 | doi-access = free }}

The drug reached phase 2 clinical trials for this indication but its development was discontinued. It was reported to be poorly effective or ineffective for schizophrenia in clinical trials.{{cite journal | vauthors = Bondarev AD, Attwood MM, Jonsson J, Chubarev VN, Tarasov VV, Liu W, Schiöth HB | title = Recent developments of phosphodiesterase inhibitors: Clinical trials, emerging indications and novel molecules | journal = Frontiers in Pharmacology | volume = 13 | issue = | pages = 1057083 | date = 2022 | pmid = 36506513 | pmc = 9731127 | doi = 10.3389/fphar.2022.1057083 | doi-access = free }}{{cite journal | vauthors = Neef J, Palacios DS | title = Progress in mechanistically novel treatments for schizophrenia | journal = RSC Medicinal Chemistry | volume = 12 | issue = 9 | pages = 1459–1475 | date = September 2021 | pmid = 34671731 | pmc = 8459322 | doi = 10.1039/d1md00096a }}{{cite journal | vauthors = Krogmann A, Peters L, von Hardenberg L, Bödeker K, Nöhles VB, Correll CU | title = Keeping up with the therapeutic advances in schizophrenia: a review of novel and emerging pharmacological entities | journal = CNS Spectrums | volume = 24 | issue = S1 | pages = 38–69 | date = August 2019 | pmid = 31482779 | doi = 10.1017/S109285291900124X | doi-access = free }}