Laszlovszky Istvan, Kiss Bela, Barabassy Agota, Kapas Margit, Nemeth Gyorgy
Richter Gedeon Nyrt., Kutatási Igazgatóság, Orvostudományi főosztály, Budapest, Hungary.
Neuropsychopharmacol Hung. 2019 Sep;21(3):103-118.
Dopamine D₂ receptor partial agonists represent a new generation of atypical antipsychotics. Cariprazine, which has received centralized market authorization from the European Medicines Agency in 2017 for the treatment of adult patients with schizophrenia (including those with predominant negative symptoms of schizophrenia) differs from the other two partial agonist antipsychotics aripiprazole and brexpiprazole due to its unique features. Cariprazine is a dopamine D₃ preferring D₃/D₂ partial agonist with very similar dopamine receptor subtype selectivity as dopamine. It has proven efficacy in the treatment of positive and negative symptoms of schizophrenia, as well as for relapse prevention. Further phase-3 clinical studies proved the efficacy of cariprazine in the acute treatment of manic or mixed episodes associated with bipolar I disorder, as well as in bipolar depression. For the adjunctive treatment of major depressive disorder, phase 3 studies are in progress.
多巴胺D₂受体部分激动剂代表了新一代非典型抗精神病药物。卡立哌嗪于2017年获得欧洲药品管理局的集中市场授权，用于治疗成年精神分裂症患者（包括以精神分裂症阴性症状为主的患者），因其独特特性，它与另外两种部分激动剂抗精神病药物阿立哌唑和布雷哌唑不同。卡立哌嗪是一种对多巴胺D₃有偏好的D₃/D₂部分激动剂，其多巴胺受体亚型选择性与多巴胺非常相似。它已被证明在治疗精神分裂症的阳性和阴性症状以及预防复发方面有效。进一步的3期临床研究证明了卡立哌嗪在急性治疗与双相I型障碍相关的躁狂或混合发作以及双相抑郁中的疗效。对于重度抑郁症的辅助治疗，3期研究正在进行中。
