[HTML][HTML] Exatecan antibody drug conjugates based on a hydrophilic polysarcosine drug-linker platform

L Conilh, G Fournet, E Fourmaux, A Murcia, EL Matera… - Pharmaceuticals, 2021 - mdpi.com
We herein report the development and evaluation of a novel HER2-targeting antibody–drug
conjugate (ADC) based on the topoisomerase I inhibitor payload exatecan, using our …

Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads

T Nakada, T Masuda, H Naito, M Yoshida… - Bioorganic & medicinal …, 2016 - Elsevier
Trastuzumab conjugates consisting of exatecan derivatives were prepared and their
biological activities and physicochemical properties were evaluated. The ADCs showed …

Antibody–exatecan conjugates with a novel self-immolative moiety overcome resistance in colon and lung cancer

W Weng, T Meng, Q Zhao, Y Shen, G Fu, J Shi… - Cancer Discovery, 2023 - AACR
Antibody–drug conjugates (ADC) using DNA topoisomerase I inhibitor DXd/SN-38 have
transformed cancer treatment, yet more effective ADCs are needed for overcoming …

A novel HER3-targeting antibody–drug conjugate, U3-1402, exhibits potent therapeutic efficacy through the delivery of cytotoxic payload by efficient internalization

Y Hashimoto, K Koyama, Y Kamai, K Hirotani… - Clinical Cancer …, 2019 - AACR
Purpose: HER3 is a compelling target for cancer treatment; however, no HER3-targeted
therapy is currently clinically available. Here, we produced U3-1402, an anti-HER3 antibody …

Synthesis and evaluation of camptothecin antibody–drug conjugates

W Li, KH Veale, Q Qiu, KW Sinkevicius… - ACS Medicinal …, 2019 - ACS Publications
Antibody–drug conjugates (ADCs) that incorporate the exatecan derivative DXd in their
payload are showing promising clinical results in solid tumor indications. The payload has …

Impact of cathepsin B-sensitive triggers and hydrophilic linkers on in vitro efficacy of novel site-specific antibody–drug conjugates

F Bryden, C Martin, S Letast, E Lles… - Organic & …, 2018 - pubs.rsc.org
Herein we describe the synthesis and evaluation of four novel HER2-targeting, cathepsin B-
sensitive antibody–drug conjugates bearing a monomethylauristatin E (MMAE) cytotoxic …

Wide application of a novel topoisomerase I inhibitor-based drug conjugation technology

Y Ogitani, Y Abe, T Iguchi, J Yamaguchi… - Bioorganic & medicinal …, 2016 - Elsevier
To establish a novel and widely applicable payload-linker technology for antibody–drug
conjugates (ADCs), we have focused our research on applying exatecan mesylate (DX …

[HTML][HTML] Rapid conjugation of antibodies to toxins to select candidates for the development of anticancer Antibody-Drug Conjugates (ADCs)

RM Hoffmann, S Mele, A Cheung… - Scientific reports, 2020 - nature.com
Abstract Antibody-Drug Conjugates (ADCs) developed as a targeted treatment approach to
deliver toxins directly to cancer cells are one of the fastest growing classes of oncology …

Tumor-selective, antigen-independent delivery of a pH sensitive peptide-topoisomerase inhibitor conjugate suppresses tumor growth without systemic toxicity

S Gayle, R Aiello, N Leelatian, JM Beckta… - NAR …, 2021 - academic.oup.com
Topoisomerase inhibitors are potent DNA damaging agents which are widely used in
oncology, and they demonstrate robust synergistic tumor cell killing in combination with DNA …

HER2 monoclonal antibodies that do not interfere with receptor heterodimerization-mediated signaling induce effective internalization and represent valuable …

BECG de Goeij, M Peipp, S de Haij, EN van den Brink… - MAbs, 2014 - Taylor & Francis
The human epidermal growth factor receptor (HER) 2 provides an excellent target for
selective delivery of cytotoxic drugs to tumor cells by antibody-drug conjugates (ADC) as has …