Conjugates of methyltrithio antitumor agents and intermediates for their synthesis
申请人:AMERICAN CYANAMID COMPANY
公开号:EP0689845A2
公开(公告)日:1996-01-03
This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
本发明描述了由强效抗肿瘤抗生素卡利昔明家族的二硫类似物及其衍生物,以及相关抗肿瘤抗生素(如埃斯帕米星)的类似物制备的载体-药物共轭物。载体可以是一种抗体、生长因子或类固醇,它们可以靶向不需要的细胞群,如肿瘤细胞。整个蛋白质载体以及它们的抗原识别片段和经过化学或基因处理的对应物都可用于共轭物的靶向部分。本发明包括合成这些共轭物所需的化合物、载体-药物共轭物的适当药物组合物及其使用方法。