Balipodect

Last updated

Balipodect
Balipodect.svg
Clinical data
Other namesTAK-063; TAK063
Drug class Phosphodiesterase inhibitor; PDE10A inhibitor; Antipsychotic
Identifiers
  • 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
Formula C23H17FN6O2
Molar mass 428.427 g·mol−1
3D model (JSmol)
  • COC1=CN(N=C(C1=O)C2=CC=NN2C3=CC=CC=C3)C4=C(C=C(C=C4)N5C=CC=N5)F
  • 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 (INN Tooltip International Nonproprietary Name, USAN Tooltip 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. [1] [2] [3]

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. [4]

The drug reached phase 2 clinical trials for this indication but its development was discontinued. [1] [2] It was reported to be poorly effective or ineffective for schizophrenia in clinical trials. [5] [6] [7]

See also

References

  1. 1 2 "Balipodect". AdisInsight. 30 January 2018. Retrieved 19 October 2024.
  2. 1 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.
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