申请人:Jiangsu Hengrui Medicine Co., Ltd.
公开号:EP3603663A1
公开(公告)日:2020-02-05
A method for preparing an antibody-drug conjugate (ADC). In particular, the method mainly utilizes a combination of antibody biomolecules and an ion exchange carrier through electrostatic interaction to realize solid phase preparation of an ADC drug. Elution conditions are optimized, to control a drug-to-antibody coupling ratio (DAR) and separate a polymer-coupled drug, reduce the amount of a drug used in a coupling reaction, and enhance the targeted therapeutic effect of an ADC drug. The preparation method features fewer steps, simple operation, and programmable control, facilitating industrial scale-up production, and also realizing zero retention of reducing agents and organic solvents in the preparation process, significantly improving drug safety and reducing production costs.
一种制备抗体药物共轭物(ADC)的方法。具体而言,该方法主要利用抗体生物大分子与离子交换载体通过静电作用结合,实现 ADC 药物的固相制备。通过优化洗脱条件,控制药物与抗体的偶联比(DAR),分离聚合物偶联药物,减少偶联反应中的药物用量,提高ADC药物的靶向治疗效果。该制备方法具有步骤少、操作简单、可编程控制等特点,有利于工业化放大生产,同时实现了还原剂和有机溶剂在制备过程中的零残留,大大提高了药物的安全性,降低了生产成本。