ITI-007
ITI-007 is an investigational atypical antipsychotic which is currently under development by Intra-Cellular Therapies, licensed from Bristol-Myers Squibb, for the treatment of schizophrenia. It is also being developed by Intra-Cellular Therapies for the treatment of bipolar disorder, depression, and sleep and behavioral disturbance in dementia, autism, and other neuropsychiatric disorders. As of September 2015, ITI-007 has passed the first of two phase III clinical trials for schizophrenia.
Pharmacodynamics
Relative to presently-available antipsychotics, ITI-007 possesses a unique and novel mechanism of action. It acts as a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). It also possesses affinity for the D1 receptor (Ki = 52 nM) and weak affinity for the α1A- and α1B-adrenergic receptors (Ki = 173 nM at α1) and D4 receptor. ITI-007 does not significantly bind to the 5-HT2B, 5-HT2C, H1, or mACh receptors.