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    Gefitnib Sensitivity-Related Gene Expression and Products and Methods Related Thereto
    4.
    发明申请
    Gefitnib Sensitivity-Related Gene Expression and Products and Methods Related Thereto 审中-公开
    吉非替尼敏感性相关基因表达及相关产品及方法

    公开(公告)号：US20100196366A1

    公开(公告)日：2010-08-05

    申请号：US12670052

    申请日：2008-07-23

    申请人： Paul A. Bunn ,  Christopher D. Coldren ,  Wilbur A. Franklin ,  Mark W. Geraci ,  Barbara A. Helfrich ,  Fred R. Hirsch ,  Razvan Lapadat ,  Michio Sugita ,  Samir E. Witta

    发明人： Paul A. Bunn ,  Christopher D. Coldren ,  Wilbur A. Franklin ,  Mark W. Geraci ,  Barbara A. Helfrich ,  Fred R. Hirsch ,  Razvan Lapadat ,  Michio Sugita ,  Samir E. Witta

    IPC分类号： A61K39/395 ,  C12Q1/68 ,  A61K31/5377 ,  A61K31/517 ,  A61K31/497

    CPC分类号： C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/136

    摘要： Disclosed is the identification, provision and use of a panel of biomarkers that predict sensitivity or resistance to EGFR inhibitors, and products and processes related thereto. In one embodiment, a method is described for selecting a cancer patient who is predicted to benefit from therapeutic administration of an EGFR inhibitor, an agonist thereof, or a drug having substantially similar biological activity as EGFR inhibitor. Also described is a method to identify molecules that interact with the EGFR pathway to allow or enhance responsiveness to EGFR inhibitors, as well as a plurality of polynucleotides or antibodies for detection of the expression of genes that are indicative of sensitivity or resistance to EGFR inhibitors, an agonist thereof, or a drug having substantially similar biological activity as EGFR inhibitors. A method to identify a compound with the potential to enhance the efficacy of EGFR inhibitors is also described.

    摘要翻译： 公开了鉴定，提供和使用一组预测对EGFR抑制剂的敏感性或抗性的生物标志物，以及与之相关的产品和方法。 在一个实施方案中，描述了一种用于选择预期从治疗性施用EGFR抑制剂，其激动剂或具有与EGFR抑制剂具有实质上相似的生物学活性的药物中受益的癌症患者的方法。 还描述了鉴定与EGFR途径相互作用以允许或增强对EGFR抑制剂的反应性的分子的方法，以及用于检测指示EGFR抑制剂的敏感性或抗性的基因表达的多个多核苷酸或抗体， 其激动剂，或具有与EGFR抑制剂基本相似的生物学活性的药物。 还描述了鉴定具有增强EGFR抑制剂功效潜力的化合物的方法。

    Flurbiprofen analogs and methods of use in treating cancer
    5.
    发明授权
    Flurbiprofen analogs and methods of use in treating cancer 有权
    氟比洛芬类似物和治疗癌症的方法

    公开(公告)号：US08575170B2

    公开(公告)日：2013-11-05

    申请号：US13035834

    申请日：2011-02-25

    申请人： Lajos Gera ,  Daniel C. Chan ,  Robert S. Hodges ,  Paul A. Bunn

    发明人： Lajos Gera ,  Daniel C. Chan ,  Robert S. Hodges ,  Paul A. Bunn

    IPC分类号： A61K31/495 ,  A61K31/4453 ,  C07D295/15

    CPC分类号： A61K31/19

    摘要： Flurbiprofen analog compounds having an amino acid derivatized at the flurbiprofen alkanoic acid carboxyl group and terminating at an ester or amide group are effective in inhibiting cancer cells in vitro and inhibiting the growth of cancers in viva. The compounds and pharmaceutical compositions containing them are particularly useful for the treatment of lung, pancreatic and head and neck cancers.

    摘要翻译： 在氟比洛芬链烷羧酸衍生化并终止于酯或酰胺基团的具有氨基酸的氟比洛芬类似物化合物在体外抑制癌细胞并抑制血液中癌症的生长是有效的。 含有它们的化合物和药物组合物特别可用于治疗肺，胰腺和头颈部癌症。

    Methods for Prediction of Clinical Outcome to Epidermal Growth Factor Receptor Inhibitors by Cancer Patients
    6.
    发明申请
    Methods for Prediction of Clinical Outcome to Epidermal Growth Factor Receptor Inhibitors by Cancer Patients 审中-公开
    用于预测癌症患者表皮生长因子受体抑制剂的临床结果的方法

    公开(公告)号：US20080090233A1

    公开(公告)日：2008-04-17

    申请号：US11568760

    申请日：2005-05-26

    申请人： Marileila Varella Garcia ,  Paul A. Bunn ,  Federico Cappuzzo ,  Wilbur A. Franklin ,  Fred R. Hirsch

    发明人： Marileila Varella Garcia ,  Paul A. Bunn ,  Federico Cappuzzo ,  Wilbur A. Franklin ,  Fred R. Hirsch

    IPC分类号： C12Q1/68 ,  C12Q1/00 ,  G01N33/483

    CPC分类号： C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/112 ,  C12Q2600/118 ,  C12Q2600/156 ,  C12Q2600/158

    摘要： Disclosed are biomarkers, methods and assay kits for the identification of cancer patients who are predicted to benefit, or not to benefit, from the therapeutic administration of an epidermal growth factor receptor (EGFR) inhibitor. The biomarkers of the present invention include detection of EGFR and HER 2 gene amplification and polysomy, EGFR protein expression, EGFR mutations, phosphorylated Akt protein expression, and various combinations of such biomarkers, as well as the combination of these biomarkers with mutations in the tyrosine kinase domain of the EGFR gene. Increased EGFR gene copy number, increased HER2 gene copy number, increased EGFR, protein expression, activated AKT protein expression (phosphorylated AKT) and EGFR mutations are all associated with better outcome for cancer patients treated with EGFR inhibitors. The invention provides a diagnostic paradigm based on each of these tests and combinations of these tests to select cancer patients who will benefit from EGFR inhibitor therapy, as well as a diagnostic paradigm to select cancer patients who will not benefit from EGFR inhibitor therapy.

    摘要翻译： 公开了用于鉴定预测从治疗性施用表皮生长因子受体（EGFR）抑制剂而受益或不受益的癌症患者的生物标志物，方法和测定试剂盒。 本发明的生物标志物包括检测EGFR和HER2基因扩增和多重，EGFR蛋白表达，EGFR突变，磷酸化Akt蛋白表达以及这些生物标志物的各种组合，以及这些生物标志物与酪氨酸突变的组合 激酶结构域。 增加的EGFR基因拷贝数，增加的HER2基因拷贝数，增加的EGFR，蛋白质表达，激活的AKT蛋白表达（磷酸化AKT）和EGFR突变都与用EGFR抑制剂治疗的癌症患者的更好的结果相关。 本发明提供了基于这些测试和这些测试的组合的诊断范例，以选择将受益于EGFR抑制剂治疗的癌症患者，以及选择不会从EGFR抑制剂治疗中获益的癌症患者的诊断范例。