[EN] SITE-SPECIFIC ANTIBODY-DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT SPÉCIFIQUES À UN SITE
申请人:VAN BERKEL PATRICIUS HENDRIKUS CORNELIS
公开号:WO2016166341A1
公开(公告)日:2016-10-20
Site-specific antibody-drug conjugates are described, in particular conjugates comprising an antibody, which binds CD25 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.
描述了特定于位点的抗体药物共轭物,特别是包括一种抗体的共轭物,该抗体结合CD25并包括通过氨基酸替换使一个链间半胱氨酸残基成为非半胱氨酸的氨基酸,以及具有以连接物形式的易降解保护基团的吡咯苯并二氮杂环己烯酮(PBDs)。结合位点以及抗体部分的修饰,可提高ADC的安全性和有效性。