From Wikipedia, the free encyclopedia
Chemical compound
Zelatriazin (NBI-1065846 or TAK-041 ) is a small-molecule agonist of
GPR139 . It was developed for schizophrenia and
anhedonia in depression but trials were unsuccessful and its development was discontinued in 2023.
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References
^ Kamel, Amin; Bowlin, Steve; Hosea, Natalie; Arkilo, Dimitrios; Laurenza, Antonio (February 2021).
"In Vitro Metabolism of Slowly Cleared G Protein–Coupled Receptor 139 Agonist TAK-041 Using Rat, Dog, Monkey, and Human Hepatocyte Models (HepatoPac): Correlation with In Vivo Metabolism" . Drug Metabolism and Disposition . 49 (2): 121–132.
doi :
10.1124/dmd.120.000246 .
PMID
33273044 .
S2CID
227282766 .
^ Schiffer, Hans; Atienza, Josephine; Reichard, Holly; Mulligan, Victoria; Cilia, Jackie; Monenschein, Holger; Collia, Deanna; Ray, Jim; Kilpatrick, Gavin; Brice, Nicola; Carlton, Mark; Hitchcock, Steve; Corbett, Ged; Hodgson, Robert (18 May 2020).
"S180. The Selective Gpr139 Agonist Tak-041 Reverses Anhedonia and Social Interaction Deficits in Rodent Models Related to Negative Symptoms in Schizophrenia" . Schizophrenia Bulletin . 46 (Supplement_1): S106–S107.
doi :
10.1093/schbul/sbaa031.246 .
PMC
7234360 .
^ Yin, Wei; Han, David; Khudyakov, Polyna; Behrje, Rhett; Posener, Joel; Laurenza, Antonio; Arkilo, Dimitrios (August 2022).
"A phase 1 study to evaluate the safety, tolerability and pharmacokinetics of TAK-041 in healthy participants and patients with stable schizophrenia" . British Journal of Clinical Pharmacology . 88 (8): 3872–3882.
doi :
10.1111/bcp.15305 .
PMC
9544063 .
PMID
35277995 .
S2CID
247407736 .
^ Rabiner, Eugenii A.; Uz, Tolga; Mansur, Ayla; Brown, Terry; Chen, Grace; Wu, Jingtao; Atienza, Joy; Schwarz, Adam J.; Yin, Wei; Lewis, Yvonne; Searle, Graham E.; Dennison, Jeremy M. T. J.; Passchier, Jan; Gunn, Roger N.; Tauscher, Johannes (June 2022).
"Endogenous dopamine release in the human brain as a pharmacodynamic biomarker: evaluation of the new GPR139 agonist TAK-041 with [11C]PHNO PET" . Neuropsychopharmacology . 47 (7): 1405–1412.
doi :
10.1038/s41386-021-01204-1 .
PMC
9117280 .
PMID
34675381 .
^ Reichard, Holly A.; Schiffer, Hans H.; Monenschein, Holger; Atienza, Josephine M.; Corbett, Gerard; Skaggs, Alton W.; Collia, Deanna R.; Ray, William J.; Serrats, Jordi; Bliesath, Joshua; Kaushal, Nidhi; Lam, Betty P.; Amador-Arjona, Alejandro; Rahbaek, Lisa; McConn, Donavon J.; Mulligan, Victoria J.; Brice, Nicola; Gaskin, Philip L. R.; Cilia, Jackie; Hitchcock, Stephen (12 August 2021). "Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia". Journal of Medicinal Chemistry . 64 (15): 11527–11542.
doi :
10.1021/acs.jmedchem.1c00820 .
PMID
34260228 .
S2CID
235908256 .
^ Münster, Alexandra; Sommer, Susanne; Kúkeľová, Diana; Sigrist, Hannes; Koros, Eliza; Deiana, Serena; Klinder, Klaus; Baader-Pagler, Tamara; Mayer-Wrangowski, Svenja; Ferger, Boris; Bretschneider, Tom; Pryce, Christopher R.; Hauber, Wolfgang; von Heimendahl, Moritz (August 2022).
"Effects of GPR139 agonism on effort expenditure for food reward in rodent models: Evidence for pro-motivational actions" . Neuropharmacology . 213 : 109078.
doi :
10.1016/j.neuropharm.2022.109078 .
PMID
35561791 .
S2CID
248574904 .
^ Taylor, Nick Paul (10 November 2023).
"Neurocrine hit with one-two punch as Takeda and Xenon pacts deliver midphase flops" . Fierce Biotech . Retrieved 4 December 2023 .