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Use of a next generation maleimide in combination with THIOMAB™ antibody technology delivers a highly stable, potent and near homogeneous THIOMAB™ antibody-drug conjugate (TDC)†
João P. M. Nunes,Vessela Vassileva,Eifion Robinson,Maurício Morais,Mark E. B. Smith,R. Barbara Pedley,Stephen Caddick,James R. Baker
RSC Advances Pub Date : 05/10/2017 00:00:00 , DOI:10.1039/C7RA04606E
Abstract

Herein we demonstrate that conjugation of a next generation maleimide (NGM) to engineered cysteines in a THIOMAB™ antibody delivers a THIOMAB™ antibody-drug conjugate (TDC) with a drug loading of ca. 2. This TDC is highly stable in blood serum conditions, selective and potent towards HER2 expressing cell lines and meets the current criteria for optimised antibody-drug conjugates (ADCs).

Graphical abstract: Use of a next generation maleimide in combination with THIOMAB™ antibody technology delivers a highly stable, potent and near homogeneous THIOMAB™ antibody-drug conjugate (TDC)
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