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Balipodect

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Abandoned PDE10A inhibitor

Pharmaceutical compound
Balipodect
Clinical data
Other namesTAK-063; TAK063
Drug classPhosphodiesterase inhibitor; PDE10A inhibitor; Antipsychotic
Identifiers
IUPAC name
  • 1-(2-fluoro-4-pyrazol-1-ylphenyl)-5-methoxy-3-(2-phenylpyrazol-3-yl)pyridazin-4-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC23H17FN6O2
Molar mass428.427 g·mol
3D model (JSmol)
SMILES
  • COC1=CN(N=C(C1=O)C2=CC=NN2C3=CC=CC=C3)C4=C(C=C(C=C4)N5C=CC=N5)F
InChI
  • InChI=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
  • Key:KVHRYLNQDWXAGI-UHFFFAOYSA-N

Balipodect (INNTooltip International Nonproprietary Name, USANTooltip 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.

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.

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.

See also

References

  1. ^ "Balipodect". AdisInsight. 30 January 2018. Retrieved 19 October 2024.
  2. ^ "Delving into the Latest Updates on Balipodect with Synapse". Synapse. 19 September 2024. Retrieved 19 October 2024.
  3. Suzuki K, Kimura H (July 2018). "TAK-063, a novel PDE10A inhibitor with balanced activation of direct and indirect pathways, provides a unique opportunity for the treatment of schizophrenia". CNS Neuroscience & Therapeutics. 24 (7): 604–614. doi:10.1111/cns.12798. PMC 6489916. PMID 29318783.
  4. Menniti FS, Chappie TA, Schmidt CJ (2020). "PDE10A Inhibitors-Clinical Failure or Window Into Antipsychotic Drug Action?". Frontiers in Neuroscience. 14: 600178. doi:10.3389/fnins.2020.600178. PMC 7855852. PMID 33551724.
  5. Bondarev AD, Attwood MM, Jonsson J, Chubarev VN, Tarasov VV, Liu W, et al. (2022). "Recent developments of phosphodiesterase inhibitors: Clinical trials, emerging indications and novel molecules". Frontiers in Pharmacology. 13: 1057083. doi:10.3389/fphar.2022.1057083. PMC 9731127. PMID 36506513.
  6. Neef J, Palacios DS (September 2021). "Progress in mechanistically novel treatments for schizophrenia". RSC Medicinal Chemistry. 12 (9): 1459–1475. doi:10.1039/d1md00096a. PMC 8459322. PMID 34671731.
  7. Krogmann A, Peters L, von Hardenberg L, Bödeker K, Nöhles VB, Correll CU (August 2019). "Keeping up with the therapeutic advances in schizophrenia: a review of novel and emerging pharmacological entities". CNS Spectrums. 24 (S1): 38–69. doi:10.1017/S109285291900124X. PMID 31482779.
Phosphodiesterase inhibitors
PDE1
PDE2
PDE3
PDE4
PDE5
PDE7
PDE9
PDE10
PDE11BC11-38
Non-selective
Unsorted
See also: Receptor/signaling modulators
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