Lumateperone (ITI-007) is a tosylate salt with binding affinities to receptors implicated in
the therapeutic actions of antipsychotic medications, including the serotonin 5HT2A receptors, dopamine
D2 and D1 receptors and the serotonin transporter. It has a unique mechanism of action because it
simultaneously modulates serotonin, dopamine, and glutamate neurotransmission, implicated in serious
mental illness. It can be considered a multi-target-directed ligand and a multifunctional modulator
of serotoninergic system with possible precognitive, antipsychotic, antidepressant and anxiolytic properties.
Lumateperone has been investigated as a novel agent for the treatment of schizophrenia, but it
represents a new potential option for other psychiatric and neurological diseases, such as behavioural
symptoms of dementia or Alzheimer’s disease, sleep disturbances, bipolar depression. Besides, it has
demonstrated a favourable safety profile without significant extrapyramidal side effects, hyperprolactinemia
or changes in cardiometabolic or endocrine factors versus placebo. Additional studies are warranted
to confirm and examine the benefit of lumateperone and possible therapeutic targets. This paper
is a comprehensive and thorough summary of the most important findings and potential future role of
this particular compound in personalized treatments.