Improved linker-payload for antibody binding, pharmaceutical composition and its applications

Abstract

The present invention provides a linker-payload complex containing a bioorthogonal group and a hydrophilic moiety. The improved linker-payload and improved antibody-drug conjugate (ADC) for antibody complexation exhibit greater stability in blood circulation and improve drug delivery and release efficiency in target cells. The present invention also relates to pharmaceutical compositions comprising antibodies against several antigen targets (e.g., TROP2, HER2, Nectin-4, etc.), their antigen-binding fragments, and ADCs. Furthermore, methods for using ADCs for the treatment of subjects with pathological conditions are also provided.

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