[EN] SITE-SPECIFIC ANTIBODY-DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS SPÉCIFIQUE À UN SITE-MÉDICAMENT
申请人:VAN BERKEL PATRICIUS HENDRIKUS CORNELIS
公开号:WO2016166305A1
公开(公告)日:2016-10-20
Site-specific antibody-drug conjugates are described, in particular conjugates comprising an antibody, which binds MUC1 and comprises an amino acid substitution of an interchain cysteine residue by an amino acid that is not cysteine, and pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker. The site of conjugation, along with modification of the antibody moiety, allows for improved safety and efficacy of the ADC.
特定于部位的
抗体药物偶联物被描述,特别是包含一种
抗体的偶联物,该
抗体结合MUC1并且包括通过非半胱
氨酸替换间链半胱
氨酸残基的
氨基酸,以及具有以连接物形式的易降解保护基的
吡咯苯二氮卓啉(
PBDs)。偶联的部位以及
抗体部分的修饰,可以提高ADC的安全性和有效性。