靶向药azd9291的说明.docxVIP

胃溶胶囊，空腹服用，每天一次，单药每天 80mg 胃溶胶囊，空腹服用，每天一次，单药每天 80mg，联合使用20-40mg 。 AZD9291 的专利 WO 2013014448 A1 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer AZD9291 的说明 更新于2014年12月21日星期日 阿斯利康的 AZD9291 ，是一种口服的小分子第三代表皮生长因子酪氨酸激酶抑制剂 （EGFR-TKI），能同时对付非小细胞肺癌的 EGFR基因突变（包括18,19,21突变）和EGFR-TKI 获得性耐药（T790M ）。AZD9291与 WZ4002和CO-1686 一样，也是基于嘧啶骨架。 AZD9291 一 Leading 3rd Generation EGFR TKI Aging populations in the US, EU and Japan and high levels ofsmoking in China influence the upward nsclc trends TlEfficacy of AZDS^i in PC^ (exome 忖deletion) xenograft mode)VitllEHIrMBB 暮儁护尸|?J? mpw _x Vr「Ha trwfttpn^nEAZ09291 is an Tl Efficacy of AZDS^i in PC^ (exome 忖deletion) xenograft mode) VitllEH IrMBB 暮儁护尸 |?J? mpw _x V r「 Ha trwfttpn^nE AZ09291 is an irreversible inhibitor for EGFRM and T790M AZD9291 targets both the activating mutant, EGFRrm- and the resistance mutation, T790M, whilst maintaining a margin (a aclivity versus wild lype EGFR A2D9291 entered Phase I clinical trials in March 2013 ■ Preliminary Phase I data on AZD9291 was reported at the ECCO ! ESMO rrieetinq in Amsterdam in September 2013 ? 1 T * 1 IDO 1? 1E4 Davs dosarl CONFIOEMT1AL CAS#: 1421373-65-0 分子式：C28H33N7O2 分子量：499.62 化学名： N-(2-((2-(dimethylami no)ethyl)(methyl)ami no)-4-methoxy-5-((4-(1-methyl-1H-i ndol-3-yl) pyrimidi n-2-yl)ami no)phe nyl)acrylamide. AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM) 临床形态是AZD9291 mesylate （甲磺酸盐），分子量为595.71。 剂量换算：临床量/非正版量=1 : 1.2，那么40mg AZD9291=48mg ，80mg AZD929仁96mg Figure 1 r AZD9291 significantly delays ngistance in EGFR-mutant PC9 (EGFR eson 19 deletion) cells in vitro nib n=6 ? Atatini n=5 丄l WZ4O2 r-6 ? AZD9291 n：Q Irrflai ccrknflnfrstion wjir 审甲wlI io th* prolifAratiUMR half-maximfli inhibiior^ 屛cnu#rtrBtiori (ICJ1 pmuktusly Hfit^rrTiinflcI for eacn inhibitor： gefitinic 20 nM. nfatirib O.fl nM, WZ40C2 30 nM. AZM291 10