印度代购提示：美国食品药物管理局(FDA)于2018年11月28日批准了吉瑞替尼(Gilteritinib)用于治疗FLT3突变及复发或难治性AML成人患者的新药上市申请，使该药成为FDA批准用于治疗此类疾病的首个也是唯一FLT3靶向制剂。高效的缓解率和较低的药物毒性促使吉瑞替尼被列入NCCN指南2019年第1版，用于治疗复发难治性AML.

The U.S. Food and Drug Administration (FDA) approved a new Drug application for Gilteritinib for the treatment of adult patients with FLT3 mutation and relapsed or refractory AML on November 28, 2018, making Gilteritinib the first and only FLT3-targeted agent approved for the treatment of this disease. The high response rate and low drug toxicity have led to the inclusion of geritinib in the 2019 First edition of the NCCN guidelines for the treatment of relapse-resistant AML.

　　印度代购提示：吉瑞替尼是第二代FLT3抑制剂，对FLT3突变具有高选择性，抑制作用更强，脱靶效应更小。多项临床试验证实，吉瑞替尼（gilteritinib）已显示对两种FLT3突变—— 即FLT3内部串联重复（FLT3-ITD）和FLT3酪氨酸激酶结构域（FLT3 tyrosine kinase domain, FLT3-TKD）有显著的抑制作用。FLT3突变的复发或难治性急性髓系白血病患者亟需全新的治疗选择。

吉瑞替尼

　　印度代购提示：临床研究评估吉瑞替尼联合7+3诱导化疗和大剂量阿糖胞苷巩固化疗、以及作为单药维持疗法在新确诊的18岁及以上AML（不包括核心结合因子[CBF]易位）成人患者中的安全性、耐受性和抗肿瘤活性。截止2018年7月2日，共入组62例患者，60例被纳入安全性分析组。大多数受试者为男性（66.7%，年龄中位数为59.5岁，32例[52.3%]携带FLT3突变[n=23]）。在剂量递增期间，40mg/天队列d1-d14接受吉瑞替尼的2例受试者经历了剂量限制性毒性（DLT:中性粒细胞减少症、血小板减少症、射血分数降低）。吉瑞替尼诱导计划表改变后，在此剂量下不再发生DLT.200mg/天队列中有2例受试者经历DLT.最大耐受剂量和推荐的扩展剂量确定为120mg/天。

The clinical study evaluated the safety, tolerability, and antitumor activity of geritinib in combination with 7+3 induction chemotherapy and high-dose cytarabine consolidation chemotherapy, as well as as single-agent maintenance therapy in newly diagnosed AML in adults 18 years and older (excluding core binding factor [CBF] translocation). As of July 2, 2018, a total of 62 patients were enrolled, and 60 patients were included in the safety analysis group. Most subjects were male (66.7%, median age 59.5 years, 32 [52.3%] with FLT3 mutations [n=23]). During dose escalation, two subjects in the 40mg/ day cohort d1-d14 receiving geritinib experienced dose-limiting toxicity (DLT: neutropenia, thrombocytopenia, reduced ejection fraction). DLT did not occur at this dose after the change in the induction schedule of gerritinib. Two subjects in the 200mg/ day cohort experienced DLT. The maximum tolerated dose and recommended extended dose were determined to be 120mg/ day.