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Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7.
Cariprazine (Vraylar) is an oral atypical antipsychotic originated by Gedeon Richter. It is a potent dopamine D3 and D2 receptor partial agonist, which preferentially binds to the D3 receptor. Cariprazine also has partial agonist activity at serotonin 5-HT1A receptors. In September 2015, cariprazine received its first global approval in the USA for the treatment of schizophrenia and for the acute treatment of manic or mixed episodes associated with bipolar I disorder. It is also in development in a variety of countries for the treatment of schizophrenia with predominant negative symptoms (phase III), as adjunctive therapy for major depressive disorder (phase II/III) and for the treatment of bipolar depression (phase II). This article summarizes the milestones in the development of cariprazine leading to this first approval for schizophrenia and manic or mixed episodes associated with bipolar I disorder.
卡利拉嗪(Vraylar)是一种由杰德恩·理特公司开发的口服非典型抗精神病药物。它是一种有效的多巴胺 D3 和 D2 受体部分激动剂,优先与 D3 受体结合。卡利拉嗪还具有 5-羟色胺 5-HT1A 受体的部分激动活性。2015 年 9 月,卡利拉嗪在美国获得了第一个全球批准,用于治疗精神分裂症和双相 I 障碍相关的急性躁狂或混合发作。它还在多个国家开发用于治疗以阴性症状为主的精神分裂症(III 期)、作为辅助治疗重度抑郁症(II/III 期)和治疗双相抑郁症(II 期)。本文总结了卡利拉嗪开发过程中的重要里程碑,这些里程碑促成了它在精神分裂症和双相 I 障碍相关的急性躁狂或混合发作方面的首次批准。