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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.〔(【引用サイトリンク】 author = Intra-Cellular Therapies )〕 As of May 2015, ITI-007 is in 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.〔
ITI-007 shows a 60-fold difference in its affinities for the 5-HT2A and D2 receptors, which is far greater than that of most or all existing atypical antipsychotics, such as risperidone (12-fold), olanzapine (12.4-fold), and aripiprazole (0.18-fold).〔 It is thought that this property may improve the effectiveness and reduce the side effect profile of ITI-007 relative to currently-available antipsychotics, a hypothesis which is supported by the observation of minimal catalepsy in mice treated with the drug.〔〔 Moreover, it has been expressed that this property could result in full occupancy and blockade of the 5-HT2A at low doses, with dose-dependent adjustable modulation of the D2 receptor, as well as the SERT, possible with increasing doses, which would uniquely allow for clinical optimization of efficacy and side effect incidence.〔〔
Unlike most current antipsychotics, such as haloperidol, risperidone, and olanzapine, ITI-007 does not disrupt striatal dopamine signaling, a property which is likely due to partial agonism of presynaptic D2 receptors.〔 In accordance, similarly to aripiprazole, which is also a partial agonist of presynaptic D2 receptors, ITI-007 showed no striatum-based motor side effects (i.e., catalepsy) in animals.〔
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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