灵北（H.Lundbeck）和大冢（Otsuka）重磅精神病新药Rexulti（brexpiprazole），该药为每日口服一次的药物，于2015年7月13日获美国FDA批准：
（1）作为一种辅助药物用于重度抑郁症（MDD）成人患者的治疗；
（2）用于精神分裂症（schizophrenia）成人患者的治疗。
“精神分裂症及重度抑郁症可以令人致残，极大扰乱日常活动，”FDA药物评价与研究中心精神产品部门主任Mathis博士称。“药物对每个人的影响不同，所以拥有各种各样的治疗选择对精神疾病患者来说是非常重要的。”
Rexulti治疗精神分裂症的有效性在1310名受试者参与的两项周期为6周的临床试验中得到评价。Rexulti与安慰剂相比显示能够减少精神分裂症症状的发生。
Rexulti作为一种辅助治疗药物用于MDD的有效性在两项周期为6周的试验中得到评价，这两项试验在1046名受试者中将Rexulti加一种抗抑郁药与安慰剂加一种抗抑郁药进行了对比，这些受试者仅使用一种抗抑郁药已不能充分治疗他们的症状。以Rexulti治疗的受试者与安慰剂治疗受试者相比报道有更少的抑郁症症状。
Rexulti及其它用于治疗精神分裂症的药物均有一项黑框警告，提醒卫生保健专业人员超适应症使用这些药物治疗老年痴呆性精神病患者的行为障碍与死亡风险增加相关。
黑框警告还提醒卫生保健专业人员及患者儿童、青少年及青壮年服用抑郁药自杀想法或自杀行为的风险会增加。应该对患者的病情恶化及自杀想法及自杀行为的出现进行监控。Rexulti在配发时必须附带一份患者用药指南，该指南描述了有关该药物使用及风险的重要信息。
临床试验中，Rexulti用药患者最常报道的副作用包括体重增加及一种内在不安感，如感觉需要移动。Rexulti由位于东京的大冢制药有限公司生产。

HOW SUPPLIED
REXULTI™ 0.25mg brexpiprazole 30Tablets NDC 59148-035-13
REXULTI™ 0.5mg brexpiprazole 30Tablets NDC 59148-036-13
REXULTI™ 1mg brexpiprazole 30Tablets NDC 59148-037-13
REXULTI™ 2mg brexpiprazole 30Tablets NDC 59148-038-13
REXULTI™ 3mg brexpiprazole 30Tablets NDC 59148-039-13
REXULTI™ 4mg brexpiprazole 30Tablets NDC 59148-039-13
REXULTI片在20°C至25°C（68°F至77°F）;允许15°C至30°C（59°F至86°F），游览[见USP控制室温。

Rexulti (Brexpiprazole) for Major Depressive Disorder (MDD) and Schizophrenia
Rexulti (brexpiprazole) is a newly-discovered psychotropic compound indicated as an add-on therapy for major depressive disorder (MDD) and as a treatment for schizophrenia. The drug was discovered by Otsuka and is being co-developed with Lundbeck.
Rexulti was approved by US Food and Drug Administration (FDA) in July 2015 as an adjunctive treatment for adults with MDD and as a treatment for adults with schizophrenia. The new drug application (NDA) of Rexulti was accepted by the FDA in September 2014.
The drug will be available in the US in early August 2015 and will be co-marketed by the two companies. It will be available in the form of tablets in various dosages, including 0.25mg, 0.5mg, 1mg, 2mg, 3mg and 4mg for oral administration only.
REXULTI Rx
Pharmacological Class:
Atypical antipsychotic.
Active Ingredient(s):
Brexpiprazole 0.25mg, 0.5mg, 1mg, 2mg, 3mg, 4mg; tabs.
Company
Otsuka America Pharmaceutical, Inc.
Indication(s):
Adjunct to antidepressants for major depressive disorder (MDD). Treatment of schizophrenia.
Pharmacology:
The mechanism of brexpiprazole in treating MDD or schizophrenia is unknown. Its efficacy may be mediated through a combination of partial agonist activity at 5-HT1A and D2 receptors, and antagonist activity at 5-HT2A receptors.
Clinical Trials:
The efficacy of Rexulti for MDD was evaluated in two 6-week, double-blind, placebo-controlled, fixed-dose trials in adults who had an inadequate response to prior antidepressant therapy in the current episode and throughout the 8 weeks of prospective antidepressant treatment. The primary endpoint was change from baseline to Week 6 in the MADRS. In both studies, Rexulti 2mg/day and 3mg/day + antidepressant were superior to placebo + antidepressant in reducing mean MADRS total scores.
The efficacy of Rexulti for schizophrenia was evaluated in two 6-week, randomized, double-blind, placebo-controlled, fixed-dose trials in adults who met the DSM-IV-TR criteria. The primary efficacy endpoint was the change from baseline to Week 6 in the PANSS total score. In the first study, Rexulti at both 2mg/day and 4mg/day was superior to placebo, and in the second study, Rexulti 4mg/day was superior to placebo on the PANSS total score.
For more clinical trial data, see full labeling.
Legal Classification:
Rx
Adults:
MDD: initially 0.5mg or 1mg once daily; titrate weekly to target dose 2mg/day (max 3mg/day). Schizophrenia: initially 1mg once daily on Days 1–4; titrate to 2mg once daily on Day 5–7, then 4mg once daily on Day 8; target dose 2–4mg/day (max 4mg/day). Moderate-to-severe hepatic impairment, or moderate, severe or end-stage renal impairment: max 2mg/day for MDD and max 3mg/day for schizophrenia. CYP2D6 poor metabolizers: give ½ of usual dose; and if taking with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP2D6 or strong CYP3A4 inhibitors: give ½ of usual dose. Concomitant moderate/strong CYP2D6 with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP3A4 inducers: double usual dose over 1–2 weeks.
Children:
Not established.
Warnings/Precautions:
Elderly with dementia-related psychosis (not approved use); increased risk of death or cerebrovascular events (eg, stroke, TIA). Increased risk of suicidal thoughts and behavior in children, adolescents, and young adults; monitor closely for worsening or unusual changes in behavior in all patients. Cardio- or cerebrovascular disease. Discontinue immediately and treat if neuroleptic malignant syndrome occurs. Tardive dyskinesia. Pre-existing low WBCs or history of leukopenia/neutropenia; monitor CBCs during 1st few months of treatment; discontinue if WBCs decline. Monitor for hyperglycemia, dyslipidemia, weight gain. Risk of hypotension, aspiration pneumonia, seizures, or diabetes (do baseline fasting blood glucose). Exposure to extreme heat. Dehydration. CYP2D6 poor metabolizers. Renal or moderate-to-severe hepatic impairment. Write ℞ for smallest practical amount. Neonates: risk of extrapyramidal and/or withdrawal symptoms post-delivery (due to exposure during 3rd-trimester pregnancy). Pregnancy. Nursing mothers.
Interaction(s)
See Adults. May be potentiated by strong CYP3A4 inhibitors (eg, itraconazole, clarithromycin, ketoconazole) or strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine, quinidine). May be antagonized by strong CYP3A4 inducers (eg, rifampin, St. John’s wort). Potentiates antihypertensives. Caution with drugs that interfere with temperature regulation (eg, anticholinergics).
Adverse Reaction(s)
Weight gain, akathisia, headache, somnolence, tremor, nasopharyngitis, dizziness, anxiety, restlessness.
How Supplied:
Tabs—30
LAST UPDATED:
8/28/2015