POLYOXAZOLINE ANTIBODY DRUG CONJUGATES
    4.
    发明公开
    POLYOXAZOLINE ANTIBODY DRUG CONJUGATES 审中-公开
    聚恶唑啉抗体药物偶联物

    公开(公告)号:EP3180388A1

    公开(公告)日:2017-06-21

    申请号:EP15826412.7

    申请日:2015-07-31

    IPC分类号: C08G73/06 C08G69/00 C08G75/02

    摘要: In the present disclosure, polymer conjugates, including polymer-antibody-drug conjugates (polymer ADCs) are described, as well as the use of such conjugates to treat human disease. The polymer conjugates can contain a large number of polymer-bound agents, thus effectively increasing the drug antibody ration (DAR) of the antibody significantly beyond the currently available technology. This may be of particular importance when antibodies to low density antigens are used as target antibodies. The described polymer-ADCs have improved pharmacokinetics and solubility relative to traditional ADCs. The linker between agent and the polymer can be tailored to provide release of toxin at the desired site and under the desired conditions within the tumor. An additional feature of the polymer-ADCs of the current disclosure is that a purification moiety can be attached to the polymer backbone to provide ease of purification of the polymer-ADCs.

    摘要翻译: 在本公开中,描述了聚合物缀合物,包括聚合物 - 抗体 - 药物缀合物(聚合物ADC),以及这种缀合物用于治疗人类疾病的用途。 聚合物缀合物可以含有大量聚合物结合剂,因此有效地增加了抗体的药物抗体比(DAR),超出了目前可用的技术。 当将低密度抗原的抗体用作靶抗体时,这可能特别重要。 所述聚合物-ADC相对于传统ADC具有改善的药代动力学和溶解度。 试剂和聚合物之间的连接体可以定制为在期望的部位和肿瘤内的期望的条件下释放毒素。 本公开内容的聚合物-ADCs的另一个特征是纯化部分可以连接到聚合物主链上以提供聚合物-ADC的纯化容易性。