Abandoned PDE10A inhibitor
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]
^ a b "Balipodect" . AdisInsight . 30 January 2018. Retrieved 19 October 2024 .
^ a b "Delving into the Latest Updates on Balipodect with Synapse" . Synapse . 19 September 2024. Retrieved 19 October 2024 .
^ 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 .
^ 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 .
^ 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 .
^ 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 .
^ 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 .