申请人:Novartis AG
公开号:EP3960767A2
公开(公告)日:2022-03-02
The present application provides specific sites for modifying antibodies or antibody fragments by replacing at least one native amino acid in the constant region of a parental antibody or antibody fragment with cysteine, which can be used as a site of attachment for a payload or linker-payload combination. In one embodiment, the antibodies are modified with cysteines at positions 152 and 375 of the heavy chain constant region, as defined by EU numbering format. In another embodiment, the antibodies are modified with cysteines at position 360 of the heavy chain constant region, and position 107 of the kappa light chain constant region, as defined by EU numbering format.
本申请通过用半胱氨酸取代亲代抗体或抗体片段恒定区中的至少一个原生氨基酸,提供了修饰抗体或抗体片段的特定位点,这些位点可用作有效载荷或连接子-有效载荷组合的连接位点。在一个实施方案中,抗体在重链恒定区的 152 位和 375 位被半胱氨酸修饰,如欧盟编号格式所定义。在另一个实施方案中,抗体在重链恒定区的 360 位和 kappa 轻链恒定区的 107 位被半胱氨酸修饰,如欧盟编号格式所定义。