Convergent synthesis of hydrophilic monomethyl dolastatin 10 based drug linkers for antibody–drug conjugation

2019 ◽  
Vol 17 (35) ◽  
pp. 8115-8124 ◽  
Author(s):  
Kanwen Yang ◽  
Bo Chen ◽  
Diego A. Gianolio ◽  
James E. Stefano ◽  
Michelle Busch ◽  
...  
Keyword(s):  
Convergent Synthesis ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Drug Conjugation ◽  
Hydrophilic Drug ◽  
Free Antibody ◽  
Antibody Drug ◽  
Dolastatin 10

A cytotoxic reagent-free fragment coupling methodology was developed to produce hydrophilic drug linkers to prepare aggregation free antibody–drug conjugates.

scholarly journals Monodisperse Polysarcosine-based Highly-loaded Antibody-Drug Conjugates

2018 ◽  
Author(s):  
Warren Viricel ◽  
Guy Fournet ◽  
Sabine Beaumel ◽  
Emeline Perrial ◽  
Sébastien Papot ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Drug Loading ◽  
Antitumor Efficacy ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Hydrophilic Drug ◽  
Highly Loaded ◽  
Antibody Drug

<div> <div> <div> <p>We report the synthesis of monodisperse (i.e. discrete) polysarcosine compounds and their use as a hydrophobicity masking entity for the construction of highly-loaded homogeneous β- glucuronidase-responsive antibody-drug conjugates (ADCs). The highly hydrophilic drug-linker platform described herein improves drug-loading, physicochemical properties, pharmacokinetics and in vivo antitumor efficacy of the resulting conjugates. </p> </div> </div> </div>

scholarly journals Influence of disulfide bond isoforms on drug conjugation sites in cysteine-linked IgG2 antibody-drug conjugates

mAbs ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 583-595 ◽  
Author(s):  
Lily Liu-Shin ◽  
Adam Fung ◽  
Arun Malhotra ◽  
Gayathri Ratnaswamy
Keyword(s):  
Disulfide Bond ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Drug Conjugation ◽  
Igg2 Antibody ◽  
Antibody Drug

scholarly journals Monodisperse Polysarcosine-based Highly-loaded Antibody-Drug Conjugates

2018 ◽  
Author(s):  
Warren Viricel ◽  
Guy Fournet ◽  
Sabine Beaumel ◽  
Emeline Perrial ◽  
Sébastien Papot ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Drug Loading ◽  
Antitumor Efficacy ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Hydrophilic Drug ◽  
Highly Loaded ◽  
Antibody Drug

<div> <div> <div> <p>We report the synthesis of monodisperse (i.e. discrete) polysarcosine compounds and their use as a hydrophobicity masking entity for the construction of highly-loaded homogeneous β- glucuronidase-responsive antibody-drug conjugates (ADCs). The highly hydrophilic drug-linker platform described herein improves drug-loading, physicochemical properties, pharmacokinetics and in vivo antitumor efficacy of the resulting conjugates. </p> </div> </div> </div>

Impact of Drug Conjugation on Pharmacokinetics and Tissue Distribution of Anti-STEAP1 Antibody–Drug Conjugates in Rats

2011 ◽  
Vol 22 (10) ◽  
pp. 1994-2004 ◽  
Author(s):  
C. Andrew Boswell ◽  
Eduardo E. Mundo ◽  
Crystal Zhang ◽  
Daniela Bumbaca ◽  
Nicole R. Valle ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Drug Conjugation ◽  
Antibody Drug

scholarly journals Construction of homogeneous antibody–drug conjugates using site-selective protein chemistry

2016 ◽  
Vol 7 (5) ◽  
pp. 2954-2963 ◽  
Author(s):  
Padma Akkapeddi ◽  
Saara-Anne Azizi ◽  
Allyson M. Freedy ◽  
Pedro M. S. D. Cal ◽  
Pedro M. P. Gois ◽  
...  
Keyword(s):  
Therapeutic Efficacy ◽  
Protein Chemistry ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Drug Conjugation ◽  
Selective Chemical ◽  
Site Selective ◽  
Antibody Drug

The use of site-selective chemical drug-conjugation strategies enables the construction of antibody–drug conjugates (ADCs) with superior therapeutic efficacy.”

ASCO-GU 2019: Metastasierte Urothelkarzinome

2019 ◽  
Vol 10 (03) ◽  
pp. 140-141
Author(s):  
Alexander Kretzschmar
Keyword(s):  
San Francisco ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Chapel Hill ◽  
Antibody Drug

Die Therapielandschaft des metastasierten Urothelkarzinoms hat sich seit der Zulassung der ersten Immun-Checkpoint-Inhibitoren verändert. Die neuen Therapien sind deutlich effektiver, allerdings erreichen die Responseraten der neuen Therapien nur bis zu etwa 30 %, beklagte Prof. Matthew Milowsky, Chapel Hill/USA, auf einer Oral Abstract Session auf dem ASCO-GU. In San Francisco gaben erste Vorträge und Poster bereits einen Einblick, wovon diejenigen Patienten profitieren könnten, die auf die etablierten Chemotherapien und die neuen Immuntherapien nicht ansprechen. Manche Onkologen sprechen bereits von der „Post-Checkpoint-Ära”. Als Kandidaten werden vor allem Antikörper-Wirkstoff-Konjugate (antibody-drug conjugates; ADC) gehandelt – und zwar nicht nur zur Therapie des metastasierten Blasenkarzinoms.

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