Markovic Marija, Gallipani Alyssa, Patel Krina H, Maroney Megan
1 Rutgers, The State University of New Jersey, Piscataway Township, NJ, USA.
2 The Brooklyn Hospital Center, Brooklyn, NY, USA.
Ann Pharmacother. 2017 Apr;51(4):315-322. doi: 10.1177/1060028016678262. Epub 2016 Dec 15.
To review the pharmacology and clinical data for brexpiprazole in schizophrenia and major depressive disorder (MDD).
An English-language literature search using PubMed and MEDLINE was performed using the term brexpiprazole. All articles containing human clinical trial data published up to September 2016 were evaluated for inclusion as well as information from the manufacturer's product labeling.
STUDY SELECTION/DATA EXTRACTION: Phase 3 trials for brexpiprazole were evaluated. Key in vitro and animal data were incorporated into the pharmacology and pharmacokinetic sections where appropriate.
Four phase 3 trials have evaluated the use of brexpiprazole as a primary therapy for schizophrenia or as an antidepressant adjunct for MDD. For its schizophrenia indication, brexpiprazole was studied in 2 placebo-controlled trials of approximately 1300 patients, with 4 mg of brexpiprazole consistently showing superiority over placebo. For MDD, brexpiprazole was compared with placebo as an adjunct to antidepressants in approximately 1000 patients who had failed trials of 1 to 3 prior antidepressants. The 2-mg and 3-mg dosages of brexpiprazole showed consistent superiority over placebo in the MDD trials. Common treatment emergent adverse effects included akathisia and weight gain.
Brexpiprazole showed efficacy for the treatment of schizophrenia in the range of 2 to 4 mg/d and as an adjunct to antidepressant therapy in MDD when dosed at 2 to 3 mg/d. Advantages of this drug include once-daily dosing, good tolerability, and lack of effect on sexual function. Disadvantages include the lack of long-term safety data and potentially high cost.
综述布雷哌唑用于治疗精神分裂症和重度抑郁症（MDD）的药理学及临床数据。
使用PubMed和MEDLINE以“布雷哌唑”为关键词进行英文文献检索。对截至2016年9月发表的所有含人类临床试验数据的文章以及来自制造商产品标签的信息进行纳入评估。
研究选择/数据提取：对布雷哌唑的3期试验进行评估。在适当情况下，关键的体外和动物数据被纳入药理学和药代动力学部分。
四项3期试验评估了布雷哌唑作为精神分裂症的一线治疗药物或作为MDD的抗抑郁辅助药物的使用情况。对于精神分裂症适应症，在两项约1300例患者的安慰剂对照试验中研究了布雷哌唑，4mg布雷哌唑始终显示出优于安慰剂的效果。对于MDD，在约1000例先前使用1至3种抗抑郁药治疗失败的患者中，将布雷哌唑与安慰剂作为抗抑郁药的辅助药物进行比较。在MDD试验中，2mg和3mg剂量的布雷哌唑始终显示出优于安慰剂的效果。常见的治疗中出现的不良反应包括静坐不能和体重增加。
布雷哌唑在2至4mg/d的剂量范围内对精神分裂症治疗有效，在MDD中作为抗抑郁治疗的辅助药物时，剂量为2至3mg/d。该药物的优点包括每日一次给药、耐受性良好以及对性功能无影响。缺点包括缺乏长期安全性数据以及潜在的高成本。
