Mabplex International Co., Ltd

Lele Li

Changjiang Huang

Youxiang Sun

Lina Liu

Provided is a method for producing an antibody-drug conjugate intermediate by addition of acid. An acid additive is used to convert the monomethyl auristatin derivative into a salt thereof to participate in the reaction. The addition of the acid additive can significantly improve the yield of the final product. In addition, the low price of the acid additive greatly reduces the production cost of the final ADC product. Moreover, the method of the present invention adopts a one-step preparation process, in addition to a higher yield of the final product, not only reducing the cost of the consumables, labor, equipment, site, raw materials and the like in the production, but also greatly reducing the production of the waste liquid, and thus reducing production costs and improving production efficiency, and making the method suitable for industrial large-scale production.

Method for producing antibody-drug conjugate intermediate by addition of acid and use thereof

Provided is an antibody-drug conjugate (ADC) using one or more cysteine or derivatives thereof as linkers to couple one or more drugs at the limited binding sites of an antibody, making it possible to produce an ADC product with high drug payload, or to choose a drug with less toxicity, thereby obtaining an ADC product with wide therapeutic window. In addition, since a plurality of drugs may be coupled to one binding site, the ADC products obtained by the method of the present disclosure have better uniformity in the case of same DAR value. Moreover, the amount of antibody required for production may be greatly reduced, thereby lowering the cost. Compared with the antibody-drug conjugates coupled only one drug, the antibody-drug conjugates produced by the method of the present disclosure have the same inhibition or killing effect on tumor cells while using fewer drugs for coupling to the same site.

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Shandong, China

Lele Li