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)

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)

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...

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Veröffentlicht in:RSC advances 2017-01, Vol.7 (40), p.24828-24832
Hauptverfasser: Nunes, João P. M., Vassileva, Vessela, Robinson, Eifion, Morais, Maurício, Smith, Mark E. B., Pedley, R. Barbara, Caddick, Stephen, Baker, James R., Chudasama, Vijay
Format: Artikel
Sprache:eng
Schlagworte:
Antibodies
Biotechnology
Blood
Conjugates
Conjugation
Criteria
Cysteine
Serums
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Zusammenfassung: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).
ISSN:2046-2069
2046-2069
DOI:10.1039/C7RA04606E