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Expert Rev Neurother. 2016 Jun;16(6):601-14. doi: 10.1080/14737175.2016.1174577. Epub 2016 Apr 25.

ITI-007 in the treatment of schizophrenia: from novel pharmacology to clinical outcomes.

Author information

a 3-D Pharmaceutical Consultants Inc ., San Diego , CA , USA.
b Department of Psychiatry , Northwell Health, The Zucker Hillside Hospital , Glen Oaks , NY , USA.
c Hofstra Northwell School of Medicine , Hempstead , NY , USA.
d The Feinstein Institute for Medical Research , Manhasset , NY , USA.

Erratum in


ITI-007 is an investigational drug being developed for schizophrenia and other neuropsychiatric/neurodegenerative diseases. ITI-007 has a unique pharmacological profile, combining potent 5-HT2a receptor antagonism with cell-type-specific dopamine and glutamate receptor modulation, plus serotonin reuptake inhibition. At dopamine-D2 receptors, ITI-007 acts as a post-synaptic antagonist and pre-synaptic partial agonist. Additionally, ITI-007 stimulates phosphorylation of glutamatergic NMDA-NR2B receptors, downstream of dopamine-D1 receptor intracellular signaling. Based on a large, placebo and risperidone controlled, Phase-II trial, ITI-007 60 mg was shown to be effective in reducing symptoms in patients with acutely exacerbated schizophrenia. The antipsychotic efficacy of ITI-007 60 mg in this patient population was confirmed in a recently completed Phase III study. ITI-007 was associated with minimal safety risk compared to risperidone (Phase II study) or placebo (both studies) for neuromotor disturbances, prolactin changes, weight gain and metabolic abnormalities. A second 6-week, placebo and risperidone-controlled Phase-III trial in acutely exacerbated schizophrenia is ongoing.


5HT2a receptors; Antipsychotic; NMDA receptors; dopamine D2 receptors; dopamine receptor phosphoprotein modulator; efficacy; neuropsychiatric disorders; safety; schizophrenia; serotonin reuptake transporter

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