Technology & Products
ITI-007

ITI-007 has a novel combination of pharmacologic properties that will define the next generation of antipsychotic drugs. As an orally bioavailable compound, ITI-007 combines potent 5HT_2A receptor antagonism with cell-type-specific modulation of phosphoprotein pathways downstream of dopamine receptors. As a Dopamine receptor phosphoprotein modulator (DPPM), ITI-007 has dual properties, acting as a post-synaptic antagonist and as a pre-synaptic partial agonist depending on the dopamine receptor context. The combination of ITI-007's high potency blockade of 5HT_2A receptors and unique dopamine receptor activity will make it possible, for the first time, to select a clinical dose capable of saturating 5HT_2A receptors, while permitting the "dialing in" of an optimal amount of dopamine receptor modulation. The ability to optimize the level of dopamine receptor modulation holds promise for the reduction of psychotic symptoms without incurring high levels of dopamine antagonism that cause motor disturbances and other deleterious side effects. Importantly, ITI-007 also has a low propensity, much lower than currently marketed antipsychotic drugs, to bind receptors that mediate deleterious cardiovascular events, profound sedation and rapid and significant weight gain.

CNSProfile™ technology revealed that ITI-007 is a novel phosphoprotein modulator, selectively blocking overactive dopamine responsive phosphoprotein pathways without stimulating compensatory dopamine synthesis, giving ITI-007 unique, partial agonist-like properties. We believe these attributes will give ITI-007 major advantages over all currently marketed antipsychotics. ITI-007 will start Phase I clinical trials shortly for the treatment of acute psychotic symptoms associated with schizophrenia.