PRACTICAL GLYCAN ENGINEERING METHOD FOR THE PREPARATION OF HOMOGENOUS ANTIBODY CONJUGATES

Abstract: an acetal- or ketal-containing disaccharide that is useful as a linker in antibody-drug conjugation. the disaccharide comprises a hexose linked to a n-acetylglucosamine oxazoline, and further comprises an acetal or ketal moiety bonded at a 4-position hydroxyl oxygen atom and a 6-position hydroxyl oxygen atom of the hexose. the acetal or ketal group can bear a variety of functional groups. also provided are an antibody drug conjugate comprising an antibody linked to a therapeutic drug via the disaccharide. also provided is a two-step method of making the acetal- or ketal-containing disaccharide.

Inventor(s): Weiping Tang, Deqin Cai, Yuan Zhao

CPC Classification: A61K47/6889 (PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms ; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles ; soap compositions ))

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