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). Issue 40 (10th May 2017)

• Record Type: Journal Article
• Authors: Nunes, João P. M.; Vassileva, Vessela; Robinson, Eifion; Morais, Maurício; Smith, Mark E. B.; Pedley, R. Barbara; Caddick, Stephen; Baker, James R.; Chudasama, Vijay
• Is Part Of: RSC advances. Volume 7:Issue 40(2017)
• Page Start: 24828
• Page End: 24832
• Publication Date: 2017-05-10
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c7ra04606e
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : Conjugation of next generation maleimides to engineered cysteines in a THIOMAB™ antibody delivers a highly stable and potent THIOMAB™ antibody-drug conjugate. 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).