ARX788, a site-specific anti-HER2 antibody–drug conjugate, demonstrates potent and selective activity in HER2-low and T-DM1–resistant breast and gastric cancers

L Skidmore, S Sakamuri, NA Knudsen, AG Hewet… - Molecular cancer …, 2020 - AACR
First-generation antibody–drug conjugates (ADC) are heterogeneous mixtures that have
shown clinical benefit, but generally exhibited safety issues and a narrow therapeutic …

[HTML][HTML] Antibody–drug conjugates—a new wave of cancer drugs

H Bouchard, C Viskov, C Garcia-Echeverria - Bioorganic & medicinal …, 2014 - Elsevier
Antibody–drug conjugates (ADCs) consist of cytotoxic drugs covalently linked to monoclonal
antibodies directed to antigens differentially overexpressed in tumor cells. These loaded …

Qualitative analysis of antibody–drug conjugates (ADCs): an experimental comparison of analytical techniques of cysteine-linked ADCs

M Källsten, R Hartmann, K Artemenko, SB Lind… - Analyst, 2018 - pubs.rsc.org
Antibody–drug conjugates (ADCs) are an emerging type of biotherapeutics that utilize
multiple tissue-specific antibodies combined with a range of linker designs to enable the …

Bioorthogonal prodrug–antibody conjugates for on-target and on-demand chemotherapy

F Lin, L Chen, H Zhang, WS Ching Ngai… - CCS …, 2019 - chinesechemsoc.org
Current antibody–drug conjugates (ADCs) suffer from low tissue penetration and significant
side effects, largely due to the permanent linkage and/or premature release of cytotoxic …

[fam‐] trastuzumab deruxtecan, antitumor activity is dependent on HER2 expression level rather than on HER2 amplification

N Takegawa, J Tsurutani, H Kawakami… - … Journal of Cancer, 2019 - Wiley Online Library
Therapies targeted to human epidermal growth factor receptor 2 (HER2) have proven
effective against tumors positive for HER2 amplification, but there is an unmet clinical need …

Exposure‐response relationships in patients with HER2‐positive metastatic breast cancer and other solid tumors treated with trastuzumab deruxtecan

O Yin, H Iwata, CC Lin, K Tamura… - Clinical …, 2021 - Wiley Online Library
Trastuzumab deruxtecan (T‐DXd) is a HER2‐targeting antibody‐drug conjugate composed
of a novel enzyme‐cleavable linker and membrane‐permeable topoisomerase I inhibitor …

Engineering a HER2-specific antibody–drug conjugate to increase lysosomal delivery and therapeutic efficacy

JC Kang, W Sun, P Khare, M Karimi, X Wang… - Nature …, 2019 - nature.com
We improve the potency of antibody–drug conjugates (ADCs) containing the human
epidermal growth factor receptor 2 (HER2)-specific antibody pertuzumab by substantially …

Rapid and Efficient Generation of Stable Antibody–Drug Conjugates via an Encoded Cyclopropene and an Inverse‐Electron‐Demand Diels–Alder Reaction

B Oller‐Salvia, G Kym, JW Chin - … Chemie International Edition, 2018 - Wiley Online Library
Homogeneous antibody–drug conjugates (ADCs), generated by site‐specific toxin linkage,
show improved therapeutic indices with respect to traditional ADCs. However, current …

Orthogonal cysteine protection enables homogeneous multi‐drug antibody–drug conjugates

MR Levengood, X Zhang, JH Hunter… - Angewandte Chemie …, 2017 - Wiley Online Library
A strategy for the preparation of homogeneous antibody–drug conjugates (ADCs) containing
multiple payloads has been developed. This approach utilizes sequential unmasking of …

The resurgence of antibody drug conjugates in cancer therapeutics: novel targets and payloads

V Boni, MR Sharma, A Patnaik - American Society of Clinical …, 2020 - ascopubs.org
Antibody drug conjugates (ADCs) are an emerging class of therapeutics that consist of a
cytotoxic agent linked covalently to an antibody, which is directed toward a specific cell …