2017年4月28日，美国食品和药物管理局（FDA）加速批准了Brigatinib (商品名Alunbrig, 日本武田药品公司美国分公司ARIAD制药公司生产）用于经克唑替尼（Crizotinib，商品名Xalkori）治疗后病情进展的，或对克唑替尼不能耐受的ALK阳性的局部晚期或转移性非小细胞肺癌。 这项批准是基于临床试验的有效结果。患有ALK阳性的局部晚期或转移性非小细胞肺癌的患者，经过克唑替尼治疗后有病情进展，被随机分配接受每天Brigatinib 90毫克或第一周每天90毫克，如可以耐受，以后每天增加到180毫克的治疗。结果显示，Brigatinib 90毫克的总体有效率为48%，180毫克的总体有效率为53%。两种计量的平均有效时间都为13.8个月。Brigatinib 90毫克对脑部转移的有效率为42%，180毫克的有效率为67%。在对脑部转移有效的患者中，78%的经90毫克治疗的患者和68%的经180毫克治疗的患者有效时间至少在4个月以上。 Brigatinib(商品名Alunbrig）的推荐计量为第一周每天90毫克，如可以耐受，以后每天增加到180毫克。 包装规格 30mg*21和180瓶 90mg*7和30瓶 完整的处方信息，请访问： https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf. Alunbrig Granted Accelerated Approval for Metastatic NSCLC The Food and Drug Administration (FDA) has granted accelerated approval to Alunbrig (brigatinib; ARIAD) tablets for the treatment of metastatic anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC) in patients who have progressed or are intolerant to crizotinib. The accelerated approval was based on data from the ALTA trial, a non-comparative, 2-arm, open-label, multicenter clinical trial showing a clinically meaningful and durable overall response rate (ORR) in patients with locally advanced or metastatic ALK-positive NSCLC who progressed on crizotinib. Study patients were randomized to oral brigatinib 90mg daily (n=112) or brigatinib 180mg daily (n=110) after a 7-day lead-in of 90mg daily. ORR in the 90mg arm was 48% (95% CI: 39%, 58%) and was 53% (95% CI: 43%, 62%) in the 180mg arm. The median duration of responses (DOR) was 13.8 months in both treatment arms.   Among patients with measurable brain metastases data, intracranial ORR was 42% (95% IC: 23%, 63%) in the 90mg arm and 67% (95% CI: 41%, 87%) in the 180mg arm. The median intracranial DOR was 5.6 months in the 180mg arm; it was not calculable in the 90mg arm. Moreover, 78% and 68% of patients in the 90mg and 180mg arms who had an intracranial response, respectively, maintained this response for ≥4 months. The most common adverse events (occurring ≥25%) were nausea, diarrhea, fatigue, cough, and headache. The most common serious adverse events were pneumonia and interstitial lung disease (ILD)/pneumonitis. Brigatinib is an investigational oral anaplastic lymphoma kinase (ALK) inhibitor that has activity at clinically achievable concentrations against multiple kinases including ALK, ROS1, insulin-like growth factor-1 receptor (IGF-1R), and FLT-3 as well as EGFR deletion and point mutations. Brigatinib exhibited in vivo anti-tumor activity against four mutant forms of EML4-ALK, including G1202R and L1196M mutants identified in NSCLC tumors in patients who have progressed on crizotinib. Alunbrig will be available as 30mg strength tablets in 21- and 180-count bottles and as 90mg strength tablets in 7- and 30-count bottles.