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公开(公告)号：EP3192529B1
公开(公告)日：2020-03-25
申请号：EP17158119.2
申请日：2010-04-08
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2.发明公开AMATOXIN-ARMED THERAPEUTIC CELL SURFACE BINDING COMPONENTS DESIGNED FOR TUMOUR THERAPY 审中-公开以AMATOXIN为基础的治疗性细胞表面结合成分设计用于肿瘤治疗
公开(公告)号：EP3192529A1
公开(公告)日：2017-07-19
申请号：EP17158119.2
申请日：2010-04-08
摘要： The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of a toxin and a target-binding moiety, e.g. an antibody, which are useful in the treatment of cancer. In particular, the toxin is an amatoxin, and the target-binding moiety is preferably directed against tumour-associated antigens. In particular, the amatoxin is conjugated to the antibody by linker moieties. In particular the linker moieties are covalently bound to functional groups located in positions of the amatoxin proved as preferred positions for the attachment of linkers with respect to optimum antitumor activity. In a further aspect the invention relates to pharmaceutical compositions comprising such target-binding moiety toxin conjugates and to the use of such target-binding moiety toxin conjugates for the preparation of such pharmaceutical compositions. The target-binding moiety toxin conjugates and pharmaceutical compositions of the invention are useful for the treatment of cancer.
摘要翻译： 本发明涉及肿瘤治疗。 在一个方面，本发明涉及毒素与靶标结合部分的缀合物，例如， 抗体，其可用于治疗癌症。 特别地，毒素是amatoxin，并且靶标结合部分优选针对肿瘤相关抗原。 特别地，amatoxin通过接头部分与抗体缀合。 具体而言，接头部分共价结合到位于阿萨木辛位置的官能团，所述官能团被证明为关于最佳抗肿瘤活性的连接物连接的优选位置。 另一方面，本发明涉及包含此类靶结合部分毒素缀合物的药物组合物，并涉及这种靶结合部分毒素缀合物用于制备此类药物组合物的用途。 本发明的靶结合部分毒素偶联物和药物组合物可用于治疗癌症。
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3.发明公开
公开(公告)号：EP3485912A1
公开(公告)日：2019-05-22
申请号：EP18214020.2
申请日：2010-04-08
摘要： The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of a toxin and a target-binding moiety, e.g. an antibody, which are useful in the treatment of cancer. In particular, the toxin is an amatoxin, and the target-binding moiety is preferably directed against tumour-associated antigens. In particular, the amatoxin is conjugated to the antibody by linker moieties. In particular the linker moieties are covalently bound to functional groups located in positions of the amatoxin proved as preferred positions for the attachment of linkers with respect to optimum antitumor activity. In a further aspect the invention relates to pharmaceutical compositions comprising such target-binding moiety toxin conjugates and to the use of such target-binding moiety toxin conjugates for the preparation of such pharmaceutical compositions. The target-binding moiety toxin conjugates and pharmaceutical compositions of the invention are useful for the treatment of cancer.
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