Site specific in vivo activation of therapeutic drugs
    9.
    发明授权
    Site specific in vivo activation of therapeutic drugs 失效
    治疗药物的体内活化位点特异性

    公开(公告)号:US5433955A

    公开(公告)日:1995-07-18

    申请号:US134520

    申请日:1993-10-08

    摘要: A method for site-specific in-vivo activation of a prodrug in an animal using an activator-targeting moiety conjugate to localize an activator at a predetermined site of use and a prodrug compound that is converted to an active drug in the presence of the activator. In the preferred embodiment, the targeting moiety, the activator, and the prodrug demonstrate little or no immunogenicity in the animal being treated. The targeting moiety is relatively specific for binding to the target tissue than to non-target tissue. The activator is not found or present in only small amounts in circulation or in non-target tissue, does not have a substrate for its activity in circulation or in non-target tissue, can be linked to the targeting moiety, and is capable of converting the prodrug to an active drug. The prodrug is selected for its ability to exert a cytotoxic activity on the target tissue after conversion by the activator.

    摘要翻译: 使用活化剂 - 靶向部分缀合物在动物中进行体内前体药物的位点特异性体内活化的方法,以在预定的使用位点定位活化剂,以及在活化剂存在下转化为活性药物的前药化合物 。 在优选的实施方案中,靶向部分,活化剂和前药在所治疗的动物中表现出很少的或不具有免疫原性。 靶向部分对于与非靶组织的结合相对于靶组织是相对特异的。 活化剂在循环或非靶组织中没有发现或仅存在少量,不具有其在循环中或非靶组织中的活性的底物,可以连接到靶向部分,并且能够转化 该前体药物为活性药物。 选择前体药物是通过活化剂转化后在靶组织上发挥细胞毒活性的能力。