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Zelatriazin (TAK-041; NBI-1065846) is a potent, selective, orally active small molecule agonist of the G protein-coupled receptor 139 (GPR139). Originally developed by Takeda Pharmaceutical Company and later licensed to Neurocrine Biosciences, the compound was investigated as an adjunctive therapy to antipsychotics for the treatment of negative symptoms and cognitive impairment associated with schizophrenia, specifically targeting motivational anhedonia. GPR139 is highly expressed in the habenula, a brain region involved in reward processing and motivation. In 2024, Neurocrine Biosciences announced the termination of its license agreement with Takeda for the development of this compound, effective April 2025.
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