The invention relates to conjugates of biologically active compounds, wherein such a conjugate is comprised of a sequence of amino acids containing a tripeptide that confers selective cleavage by tumor tissue homogenate for release of free drug and/or improves biodistribution into the tumor tissue in comparison to normal tissue homogenate from the same species, wherein the normal tissue is the site of an adverse event associated with administration to a human subject in need thereof of a therapeutically effective amount of a comparator conjugate whose amino acid sequence is a dipeptide known to be selectively cleavable by Cathepsin B.
该发明涉及
生物活性化合物的缀合物,其中所述缀合物包含一个
氨基酸序列,该序列包含一个三肽,该三肽能够通过肿瘤组织匀浆选择性裂解以释放自由药物和/或与同一物种的正常组织匀浆相比,改善了药物在肿瘤组织中的
生物分布,其中所述正常组织是与向需要治疗的人体受试者施用治疗有效量的比较缀合物相关的不良事件的发生部位,该比较缀合物的
氨基酸序列是已知可被
组织蛋白酶B选择性裂解的二肽。