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 …

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 …

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 …

[HTML][HTML] Design and Evaluation of Phosphonamidate-Linked Exatecan Constructs for Highly Loaded, Stable, and Efficacious Antibody–Drug Conjugates

S Schmitt, P Machui, I Mai, S Herterich, S Wunder… - Molecular Cancer …, 2024 - AACR
Abstract Topoisomerase I (TOP1) Inhibitors constitute an emerging payload class to
engineer antibody–drug conjugates (ADC) as next-generation biopharmaceutical for cancer …

Potent antitumor activity of anti-HER2 antibody-topoisomerase I inhibitor conjugate based on self-immolative dendritic dimeric-linker

Y Liubomirski, G Tiram, A Scomparin, S Gnaim… - Journal of Controlled …, 2024 - Elsevier
Antibody-drug conjugates (ADCs) are a rapidly expanding class of anticancer therapeutics,
with 14 ADCs already approved worldwide. We developed unique linker technologies for …

Development of novel anti-CD19 antibody-drug conjugates for B-cell lymphoma treatment

Z Li, M Wang, X Yao, H Li, S Li, L Liu, D Yu, X Li… - International …, 2018 - Elsevier
B-cell lymphoma remains one of the most refractory tumors, and as such the development of
novel treatment approaches, such as antibody-drug conjugates (ADCs), is required. To …

[PDF][PDF] Current role of topoisomerase I inhibitors for the treatment of mesenchymal malignancies and their potential future use as payload of sarcoma-specific antibody …

P Schöffski, CC Wang, MP Schöffski… - Oncology Research and …, 2024 - karger.com
Background: Topoisomerase I is an enzyme that plays a crucial part in DNA replication and
transcription by the relaxation of supercoiled double-stranded DNA. Topoisomerase I …

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 …

[HTML][HTML] A comprehensive review of key factors affecting the efficacy of antibody drug conjugate

A Samantasinghar, NP Sunildutt, F Ahmed… - Biomedicine & …, 2023 - Elsevier
Abstract Antibody Drug Conjugate (ADC) is an emerging technology to overcome the
limitations of chemotherapy by selectively targeting the cancer cells. ADC binds with an …

[HTML][HTML] A versatile chemo-enzymatic conjugation approach yields homogeneous and highly potent antibody-drug conjugates

Y Xu, S Jin, W Zhao, W Liu, D Ding, J Zhou… - International Journal of …, 2017 - mdpi.com
The therapeutic efficacy of antibodies can be successfully improved through targeted
delivery of potent cytotoxic drugs in the form of antibody-drug conjugates. However …