DR5 LIGAND DRUG CONJUGATES
    4.
    发明申请
    DR5 LIGAND DRUG CONJUGATES 审中-公开
    DR5配对药物联合

    公开(公告)号:US20150079114A1

    公开(公告)日:2015-03-19

    申请号:US14389959

    申请日:2013-04-23

    IPC分类号: A61K47/48 C07K16/28

    摘要: Ligand Drug Conjugates are provided having a DRS binding moiety attached via linking groups andor spacers to a therapeutic agent that are effective in treatment of various cancers. In some embodiments, the Ligand Drug Conjugate has the formula: L-(LU-D)p, where L is a Ligand unit, LU is a Linker unit and D is a Drug unit (or cytotoxic agent). The subscript p is an integer of from 1 to 20. Accordingly, the Ligand Drug Conjugates comprise a Ligand unit covalently linked to at least one Drug unit. The Drug units can be covalently linked directly or via a Linker unit (-LU-). The Ligand unit is a DR5 binding agent, such as an anti-DRS antibody.

    摘要翻译: 配体药物缀合物具有通过连接基团和隔离物连接的DRS结合部分与有效治疗各种癌症的治疗剂。 在一些实施方案中,配体药物缀合物具有下式:L-(LU-D)p,其中L是配体单元,LU是连接子单元,D是药物单位(或细胞毒性剂)。 下标p是1至20的整数。因此,配体药物缀合物包含与至少一个药物单元共价连接的配体单元。 药物单位可以直接或通过链接单元(-LU-)共价连接。 配体单元是DR5结合剂,例如抗DRS抗体。