lumateperone Tosylate (ITI-007) in stock CAS NO.1187020-80-9

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lumateperone (iti-722/iti-007) is a novel, first-in-class dual 5ht2a receptor antagonist/dopamine phosphoprotein modulator (dppm) for schizophrenia. it is an orally available compound which combines potent 5ht2a receptor antagonism with cell-type-specific modulation of phosphoprotein pathways downstream of dopamine receptors. as of may 2015, lumateperone is in phase iii clinical trials for schizophrenia.

pharmacodynamics

standard pharmacologic assays have confirmed lumateperone (iti-722/iti-007)'s partial agonist properties at the presynaptic dopamine d2 receptor and confirmed serotonin transporter antagonist activity which may be of added benefit to patients with schizoaffective disorder and other diseases associated with mood alterations. lumateperone (iti-722/iti-007) has a much lower propensity than several currently marketed antipsychotic drugs to bind receptors that mediate deleterious cardiovascular events, sedation and rapid and significant weight gain.

mechanism of action

as a dopamine receptor phosphoprotein modulator (dppm), iti-007 has dual properties; it acts as a post-synaptic antagonist and as a pre-synaptic partial agonist. the combination of lumateperone (iti-722/iti-007) high-potency blockade of 5ht2a receptors and unique dopamine receptor activity will make it possible for the first time, to select a clinical dose capable of saturating 5ht2a 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. in addition, the wide separation of affinity at 5ht2a and d2 receptors may allow for administration of the appropriate amount of dopamine modulation for antipsychotic maintenance therapy and the treatment of bipolar disorders.