【药物简讯】豪森重磅新药氟马替尼递交上市申请

一.白血病新药递交NDA！

Source:Pharnex datamonitor,CDE

二.产品描述：

1.本品英文名：flumatinib mesylate，结构式如上图。

2.2008年获国家科技重大专项支持，2012年获江苏省科技成果转化专项支持。

3.适应症：拟用于治疗费城染色体阳性的慢性髓性白血病（Ph+ CML）。

4.作用机制：甲磺酸氟马替尼明显抑制细胞内Bcr-abl酪氨酸激酶的活性，作用强于甲磺酸伊马替尼；甲磺酸氟马替尼对Bcr-abl的下游信号如extracellualar-regulated kinase (ERK)以及血小板衍生生长因子受体(PDGFR)也有抑制作用；但对其它受体酪氨酸激酶活性如表皮生长因子受体(EGFR)、血管内皮细胞生长因子受体2(VEGFR2/KDR)则没有明显的抑制作用。

5.Flumatinib Mesylate is the orally bioavailable, mesylate salt form of the tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity. Upon administration, flumatinib inhibits the wild-type forms of Bcr-Abl, platelet-derived growth factor receptor (PDGFR) and mast/stem cell growth factor receptor (SCFR; c-Kit) and forms of these proteins with certain point mutations. This results in the inhibition of both Bcr-Abl-, PDGFR- and c-Kit-mediated signal transduction pathways, and the proliferation of tumor cells in which these kinases are overexpressed. Bcr-Abl fusion protein is an abnormal, constitutively active enzyme expressed in Philadelphia chromosome positive chronic myeloid leukemia (CML), acute lymphoblastic leukemia (ALL) or acute myelogenous leukemia (AML). PDGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to cell migration and the development of the microvasculature. c-kit, a receptor tyrosine kinase mutated and constitutively activated in certain tumors, plays a key role in tumor cell survival, proliferation, and differentiation.

6.专利：

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