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    Tumor affinity peptide, and radioactive diagnostic agent and radioactive therapeutic agent containing the peptide
    1.
    发明授权
    Tumor affinity peptide, and radioactive diagnostic agent and radioactive therapeutic agent containing the peptide 失效
    肿瘤亲和肽，放射性诊断剂和含有该肽的放射性治疗剂

    公开(公告)号：US5827498A

    公开(公告)日：1998-10-27

    申请号：US463230

    申请日：1995-06-05

    申请人： Ikuya Seki ,  Yoshitoshi Itaya ,  Yoshifumi Shirakami ,  Komei Washino

    发明人： Ikuya Seki ,  Yoshitoshi Itaya ,  Yoshifumi Shirakami ,  Komei Washino

    IPC分类号： A61K38/00 ,  A61K51/10 ,  C07K16/18 ,  C07K16/30 ,  A61K51/00 ,  A61M36/14

    CPC分类号： A61K51/1018 ,  A61K51/1045 ,  C07K16/18 ,  C07K16/30 ,  A61K38/00

    摘要： A peptide having affinity with tumor or a salt thereof, which comprises an amino acid sequence containing 20 or less amino acid residues, said amino acid sequence being described as X.sub.1 -YCAREPPT-X.sub.2 wherein A, C, E, P, R, T and Y represent amino acid residues expressed by standard one-letter symbols, each of amino acid residues A, C, R and Y in the amino acid sequence YCAR may be in either L-form or D-form, X.sub.1 represents a basic organic compound having 1-3 amino groups, and X.sub.2 represents any given amino acid sequence, is provided together with a radioactive diagnostic agent and a radioactive therapeutic agent containing the above peptide or a salt thereof. The present tumor affinity peptide is high in radioactive metal labeling yield, useful for imaging and treating pathological tissues such as of breast cancer, ovarian cancer and colon cancer of mammals including human, and difficult to be readily metabolized in organisms and to accumulate in normal tissues especially at kidney and liver.

    摘要翻译： 一种与肿瘤或其盐具有亲和力的肽，其包含含有20个或更少氨基酸残基的氨基酸序列，所述氨基酸序列描述为X1-YCAREPPT-X2，其中A，C，E，P，R，T和 Y代表由标准单字母符号表示的氨基酸残基，氨基酸序列YCAR中的氨基酸残基A，C，R和Y中的每一个可以是L-型或D-型，X1表示具有 1-3个氨基，X2代表任何给定的氨基酸序列，与放射性诊断剂和含有上述肽或其盐的放射性治疗剂一起提供。 本发明的肿瘤亲和肽具有放射性金属标记产率高，可用于成像和治疗诸如乳腺癌，卵巢癌和包括人在内的哺乳动物的结肠癌的病理组织，并且难以在生物体中代谢并积累在正常组织中 特别是在肾脏和肝脏。

    Radiation-protecting agent
    4.
    发明授权
    Radiation-protecting agent 失效
    防辐射剂

    公开(公告)号：US6027710A

    公开(公告)日：2000-02-22

    申请号：US923002

    申请日：1997-09-16

    申请人： Kazuo Higashi ,  Komei Washino

    发明人： Kazuo Higashi ,  Komei Washino

    IPC分类号： A61K51/04 ,  A61P39/00 ,  A61K51/00 ,  A61M36/14

    CPC分类号： A61K51/0478

    摘要： The present invention provides a radiation-protecting agent which protects the active ingredient of radiopharmaceuticals against the radiolysis caused by a reaction of the active ingredient with water radicals formed by radiolysis of water, without decomposing the reactive active ingredient such as readily reducible active ingredient. The radiation-protecting agent of the present invention is characterized by comprising an organic compound usable in medical drugs and having high physiological acceptability and protecting the radiolabeled active ingredient of radiopharmaceuticals against the action of radiation. The reaction rate constant of said organic compound with OH radical, H radical or hydrated electron must be in the range of from 1.times.10.sup.8 to 5.times.10.sup.10 M.sup.-1 s.sup.-1, and when added to radiopharmaceuticals, molar concentration of the organic compound must be at least 50 times as high as molar concentration of the active ingredient.

    摘要翻译： 本发明提供了一种放射线保护剂，其保护放射性药物的活性成分免受由活性成分与水分解形成的水分反应引起的放射线分解，而不会分解活性成分如容易还原的活性成分。 本发明的放射线保护剂的特征在于，包含可用于药物的有机化合物，具有高的生理可接受性，并且防止放射性药物的放射性标记的活性成分抵抗辐射的作用。 所述有机化合物与OH自由基，H自由基或水合电子的反应速率常数必须在1×10 8至5×10 10 M -1 s -1的范围内，当加入到放射性药物中时，有机化合物的摩尔浓度必须至少为50 时间高达活性成分的摩尔浓度。