新型多靶点5-羟色胺受体抑制剂ITI-007

A new multi-targeted serotonin receptor antagonist: anti-schizophrenia ITI-007

ITI-007是Intra-Cellular Therapies有限公司开发的一种非典型抗精神分裂症药物。到目前为止,在已完成的临床前和临床试验中,该药表现出了结合强效5-HT2A受体拮抗剂、多巴胺受体磷酸化调节剂(DPPM)、谷氨酸调节剂以及5-羟色胺再摄取抑制剂于一身的特点,可用于治疗急性及残留型精神分裂症,为上述症状的单一结构候选药物。ITI-007同时还具有改善睡眠质量的效果,并能减少精神分裂症的阴性症状,对抑郁、焦虑以及与受损的社会功能相关的其他症状也有一定效果。与许多其他抗精神病药物如利培酮不同,ITI-007不会导致糖尿病和心血管疾病风险的增加,因此与许多现有抗精神分裂症药物相比,后者在长期的安全性和耐受性方面可能会有明显改善。

ITI-007 is an atypical antipsychotic drug which is currently under development by Intra-Cellular Therapies Co. Ltd. In pre-clinical and clinical trials to date, ITI-007 combines potent serotonin 5-HT2 A receptor antagonism, dopamine receptor phosphoprotein modulation（DPPM）, glutamatergic modulation, and serotonin reuptake inhibition into a single drug candidate for the treatment of acute and residual schizophrenia. ITI-007 has demonstrated significantly improvements in quality of sleep, and reducing the negative symptoms of schizophrenia, and has certain effects in treatment of depression, anxiety, and other symptoms associated with impaired social function. Different from many other antipsychotics such as risperidone, ITI-007 may not cause an increase in the risk of diabetes or cardiovascular disease. Therefore ITI-007 may prove to be a significant improvement relative to many existing antipsychotic drugs in terms of long-term safety and tolerability.