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; Vijay Chudasama

doi:10.1039/C7RA04606E

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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,^a Vessela Vassileva,^b Eifion Robinson,^a Maurício Morais,

^a Mark E. B. Smith,^a R. Barbara Pedley,^b Stephen Caddick,^a James R. Baker

*^a and Vijay Chudasama

*^ac

Author affiliations

* Corresponding authors

^a Department of Chemistry, University College London, London, WC1H 0AJ, UK
E-mail: j.r.baker@ucl.ac.uk, v.chudasama@ucl.ac.uk
Tel: +44 (0)20 7679 2653

^b UCL Cancer Institute, 72 Huntley Street, London, UK

^c Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Lisbon, Portugal

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).

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DOI: https://doi.org/10.1039/C7RA04606E
Article type: Paper
Submitted: 24 Apr 2017
Accepted: 28 Apr 2017
First published: 10 May 2017
This article is Open Access

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RSC Adv., 2017,7, 24828-24832

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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)

J. P. M. Nunes, V. Vassileva, E. Robinson, M. Morais, M. E. B. Smith, R. B. Pedley, S. Caddick, J. R. Baker and V. Chudasama, RSC Adv., 2017, 7, 24828 DOI: 10.1039/C7RA04606E

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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)†

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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)

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