ANTI-TROP2 ANTIBODY-DRUG CONJUGATE

To provide a method for producing an antibody-drug conjugate useful as an anti-tumor drug.SOLUTION: The present invention provides a method for producing an antibody-drug conjugate that comprises the following drug-linker structure:-(Succinimid-3-yl-N)-CH2CH2CH2CH2CH2-C(=O)-GGFG-NH-CH2CH2-O-CH2-C(=O)-(NH-DX) bound to an anti-TROP2 antibody through a thioether bond, the method including the step in which the anti-TROP2 antibody is treated in a reducing condition and thereafter reacted with the following compound: (maleimid-N-yl)-CH2CH2CH2CH2CH2-C(=O)-GGFG-NH-CH2CH2-O-CH2-C(=O)-(NH-DX), where -(NH-DX) is a group represented by the following formula, where a nitrogen atom of an amino group at position 1 is a connecting position.SELECTED DRAWING: None 【課題】抗腫瘍薬として有用な抗体－薬物コンジュゲートの製造方法を提供する。【解決手段】抗ＴＲＯＰ２抗体を還元条件で処理した後に次の化合物：(maleimid-N-yl)-CH2CH2CH2CH2CH2-C(=O)-GGFG-NH-CH2CH2-O-CH2-C(=O)-(NH-DX)を反応させる工程を含む、次の薬物－リンカー構造：-(Succinimid-3-yl-N)-CH2CH2CH2CH2CH2-C(=O)-GGFG-NH-CH2CH2-O-CH2-C(=O)-(NH-DX)をチオエーテル結合を介して抗ＴＲＯＰ２抗体に結合させた抗体－薬物コンジュゲートの製造方法。式中、-(NH-DX)は、次式で示される、１位のアミノ基の窒素原子が結合部位となっている基である。JPEG2023085465000046.jpg4453【選択図】なし