Evidence on the New Drug Lumateperone (ITI-007) for Psychiatric and Neurological Disorders

CNS Neurol Disord Drug Targets. 2020;19(4):243-247. doi: 10.2174/1871527319666200601145653.

Abstract

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.

Keywords: Alzheimer`s disease; ITI-007; Lumateperone; novel antipsychotics; personalized medicine; schizophrenia.

Publication types

  • Review

MeSH terms

  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / psychology
  • Bipolar Disorder / drug therapy
  • Dementia / drug therapy
  • Dementia / psychology
  • Dopamine D2 Receptor Antagonists / pharmacology
  • Dopamine D2 Receptor Antagonists / therapeutic use*
  • Drug Partial Agonism
  • Heterocyclic Compounds, 4 or More Rings / pharmacology
  • Heterocyclic Compounds, 4 or More Rings / therapeutic use*
  • Humans
  • Receptor, Serotonin, 5-HT2A / drug effects
  • Receptors, Dopamine D1 / drug effects
  • Receptors, Dopamine D2 / drug effects
  • Schizophrenia / drug therapy*
  • Serotonin 5-HT2 Receptor Antagonists / pharmacology
  • Serotonin 5-HT2 Receptor Antagonists / therapeutic use*
  • Serotonin Plasma Membrane Transport Proteins / drug effects
  • Sleep Wake Disorders / drug therapy*

Substances

  • Dopamine D2 Receptor Antagonists
  • Heterocyclic Compounds, 4 or More Rings
  • Receptor, Serotonin, 5-HT2A
  • Receptors, Dopamine D1
  • Receptors, Dopamine D2
  • Serotonin 5-HT2 Receptor Antagonists
  • Serotonin Plasma Membrane Transport Proteins
  • lumateperone