Cariprazine, a potent dopamine D3 and D2 receptor partial agonist antipsychotic with preferential binding to D3 receptors, is Food and Drug Administration approved for treating schizophrenia and manic or mixed episodes of bipolar I disorder. A post-hoc safety/tolerability analysis of data from the four acute trials in the cariprazine schizophrenia clinical development program (NCT00404573; NCT00694707; NCT01104766; NCT01104779) was carried out using the overall safety population (all patients who received ≥1 dose of study drug) and modal daily dose subgroups (1.5-3, 4.5-6, and 9-12 mg/day). These exploratory findings were summarized using descriptive statistics. Cariprazine was generally well tolerated. The incidence of treatment-emergent adverse events versus placebo was similar for cariprazine 1.5-3 mg/day and higher for cariprazine 4.5-6 and 9-12 mg/day; a dose-response relationship was observed for akathisia, extrapyramidal symptoms, and diastolic blood pressure. The mean changes in metabolic parameters were generally similar in cariprazine-treated and placebo-treated patients. There was no prolactin level increase or QTc value greater than 500 ms; small increases in mean body weight (∼1to2 kg) versus placebo were observed. Within the Food and Drug Administration-approved dose range (1.5-6 mg/day), cariprazine was generally safe and well tolerated in patients with schizophrenia.

中文翻译：

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Cariprazine在精神分裂症急性加重患者中的安全性和耐受性：两项II / III期随机，双盲，安慰剂对照研究的汇总分析。

Cariprazine是一种有效的多巴胺D3和D2受体部分激动剂，可与D3受体优先结合，是一种抗精神病药，已获得美国食品药品监督管理局的批准，可用于治疗精神分裂症和躁狂或躁郁症。使用总体安全性人群（所有接受≥1剂量研究药物的患者）对来自卡吡嗪精神分裂症临床开发计划（NCT00404573; NCT00694707; NCT01104766; NCT01104779）的四项急性试验的数据进行了事后安全性/耐受性分析）和模式每日剂量亚组（1.5-3、4.5-6和9-12 mg /天）。这些探索性发现使用描述性统计数据进行了总结。Cariprazine一般耐受良好。卡比拉嗪1.5-3 mg /天与安慰剂相比，治疗紧急不良事件的发生率相似，卡比拉嗪4则更高。5-6和9-12毫克/天；观察到静坐症，锥体束外症状和舒张压的剂量反应关系。代谢参数的平均变化通常在接受卡哌嗪治疗和安慰剂治疗的患者中相似。催乳素水平没有增加或QTc值大于500毫秒。与安慰剂相比，平均体重略有增加（约1-2kg）。在美国食品药品监督管理局批准的剂量范围（1.5-6 mg /天）内，对患有精神分裂症的患者而言，卡比拉嗪通常是安全且耐受性良好的。催乳素水平没有增加或QTc值大于500毫秒。与安慰剂相比，平均体重略有增加（约1-2kg）。在美国食品药品监督管理局批准的剂量范围（1.5-6 mg /天）内，对患有精神分裂症的患者而言，卡比拉嗪通常是安全且耐受性良好的。催乳素水平没有增加或QTc值大于500毫秒。与安慰剂相比，平均体重略有增加（约1-2kg）。在美国食品药品监督管理局批准的剂量范围（1.5-6 mg /天）内，对患有精神分裂症的患者而言，卡比拉嗪通常是安全且耐受性良好的。