ITI-002 was shown to be an orally active and a potent inhibitor of a novel intracellular target and was designed to amplify but not supplant ongoing activity of D1 receptive neurons, primarily in the prefrontal cortex. In behavioral studies, ITI-002 displayed acute and chronic activity as a cognitive enhancing agent in rodent models. ITI-002 has been shown to be safe in all preliminary evaluations and is advancing to pre-clinical development. It is envisioned that activation of D1 activity will improve the cognitive deficits seen in patients with schizophrenia.

ITI-002 refers to a novel family of compounds that are potent inhibitors aimed at potentiating the dopamine signal in dopamine target neurons. The target enzyme regulated by ITI-002 is part of the D1 dopamine receptor signaling pathway, which plays a critical role in working memory processes that are involved in maintaining and manipulating information in the brain. These processes guide higher-level behavior and high-level cognition, such as language, problem solving and reasoning. Preclinical data suggest that these compounds may have utility in treating disorders, as widely diverse as cognitive dysfunction in schizophrenia, attention deficit hyperactivity disorder and the cognitive deficits arising from Parkinson's and Alzheimer's diseases. ITI-002 also may be useful in treating the motor deficits that are associated with Parkinson's disease.