Dopamine D₂ receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia.

ABSTRACT: Dopamine D₂ receptor occupancy (D₂RO) is a key feature of all currently approved antipsychotic medications. However, antipsychotic efficacy associated with high D₂RO is often limited by side effects such as motor disturbances and hyperprolactinemia. Lumateperone (ITI-007) is a first-in-class selective and simultaneous modulator of serotonin, dopamine and glutamate in development for the treatment of schizophrenia and other disorders. The primary objective of the present study was to determine D₂RO at plasma steady state of 60 mg ITI-007, a dose that previously demonstrated antipsychotic efficacy in a controlled trial, administered orally open-label once daily in the morning for two weeks in patients with schizophrenia (N = 10) and after at least

SUBMITTER: Vanover KE 

PROVIDER: S-EPMC6333832 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature