MMP-cleavable linker platform for tumour-responsive homo- and heterobivalent antibody-drug conjugates.

Abstract:: Herein we report the development of a novel linker platform for tumour-responsive antibody-drug conjugates. A series of functionalised homo- and heterobivalent BisFab conjugates have been synthesised, comprising an MMP-cleavable peptide sequence which facilitates selective monomerisation in the tumour microenvironment of the BisFab into two smaller cytotoxic species. The platform was then expanded to produce bispecific BisFab conjugates.

Authors:: AJ Counsell, SJ Walsh, N Ashman, M Park, FM Dannheim, TA King, T Wharton, JS Carroll, DR Spring

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