De Berardis Domenico, Orsolini Laura, Iasevoli Felice, Prinzivalli Emiliano, de Bartolomeis Andrea, Serroni Nicola, Mazza Monica, Valchera Alessandro, Fornaro Michele, Vecchiotti Roberta, Carano Alessandro, Sepede Gianna, Vellante Federica, Matarazzo Ilaria, Pompili Maurizio, Perna Giampaolo, Conti Chiara, Segura-García Cristina, Martinotti Giovanni, Di Giannantonio Massimo
National Health Service, Department of Mental Health, Psychiatric Service of Diagnosis and Treatment, "G. Mazzini" Hospital, p.zza Italia 1, 64100 Teramo, Italy.
Curr Pharm Des. 2016;22(33):5144-5162. doi: 10.2174/1381612822666160701084447.
Cariprazine (RGH-188) is a novel antipsychotic drug that exerts partial agonism of dopamine D2/D3 receptors with preferential binding to D3 receptor, antagonism of 5HT2B receptors and partial agonism of 5HT1A. Currently, cariprazine is in late-stage clinical development (phase III clinical trials) in patients with schizophrenia (S) and in patients with bipolar disorder (BD), as well as an adjunctive treatment in patients with Major Depressive Disorder (MDD) and drug-resistant MDD. Cariprazine has completed phase III trials for the acute treatment of schizophrenia and bipolar mania, phase II trials for the bipolar depression and MDD whilst it is undergoing phase III trials as an adjunct to antidepressants. The present review aims at proving a comprehensive summary of the current evidence on the safety, tolerability and efficacy of cariprazine in the treatment of schizophrenia, BD (manic/mixed/ depressive episode) and MDD. A systematic search was conducted on PubMed/Medline/ Scopus and the database on Clinical Trials from inception until April 2015 by typing a set of specified keywords. Available evidence seems to support cariprazine efficacy in the treatment of cognitive and negative symptoms of schizophrenia. Preliminary findings suggest its antimanic activity whilst it is still under investigation its efficacy in the treatment of bipolar depression and MDD. Furthermore, the available data seems not to allow judgements about its antipsychotic potential in comparison with currently prescribed antipsychotics. Further studies should be carried out to better investigate its pharmacodynamic and clinical potential, particularly as alternative to current antipsychotic drugs.
卡立普嗪（RGH - 188）是一种新型抗精神病药物，对多巴胺D2/D3受体具有部分激动作用，对D3受体具有优先结合力，对5HT2B受体具有拮抗作用，对5HT1A具有部分激动作用。目前，卡立普嗪正处于精神分裂症（S）患者和双相情感障碍（BD）患者的晚期临床开发阶段（III期临床试验），以及重度抑郁症（MDD）和难治性MDD患者的辅助治疗阶段。卡立普嗪已完成精神分裂症和双相躁狂急性治疗的III期试验、双相抑郁和MDD的II期试验，同时正在进行作为抗抑郁药辅助药物的III期试验。本综述旨在全面总结目前关于卡立普嗪治疗精神分裂症、双相情感障碍（躁狂/混合/抑郁发作）和重度抑郁症的安全性、耐受性和疗效的证据。通过输入一组特定关键词，对PubMed/Medline/Scopus以及临床试验数据库进行了从创建到2015年4月的系统检索。现有证据似乎支持卡立普嗪在治疗精神分裂症认知和阴性症状方面的疗效。初步研究结果表明其具有抗躁狂活性，而其在治疗双相抑郁和MDD方面的疗效仍在研究中。此外，现有数据似乎无法对其与目前处方的抗精神病药物相比的抗精神病潜力做出判断。应开展进一步研究，以更好地探究其药效学和临床潜力，特别是作为当前抗精神病药物的替代药物。
