A HER2-targeting antibody–drug conjugate, trastuzumab deruxtecan (DS-8201a), enhances antitumor immunity in a mouse model

TN Iwata, C Ishii, S Ishida, Y Ogitani, T Wada… - Molecular cancer …, 2018 - AACR
Abstract Trastuzumab deruxtecan (DS-8201a), a HER2-targeting antibody–drug conjugate
with a topoisomerase I inhibitor exatecan derivative (DX-8951 derivative, DXd), has been …

Dual intra-and extracellular release of monomethyl auristatin E from a neutrophil elastase-sensitive antibody-drug conjugate

IAM Amar, S Huvelle, E Douez, S Letast… - European Journal of …, 2022 - Elsevier
Antibody-drug conjugates (ADCs) are targeted therapies, mainly used in oncology,
consisting in a three-component molecular architecture combining a highly potent drug …

Site-specific dolasynthen antibody–drug conjugates exhibit consistent pharmacokinetic profiles across a wide range of drug-to-antibody ratios

SM Clardy, A Uttard, B Du, KC Catcott… - Molecular Cancer …, 2024 - AACR
Key defining attributes of an antibody–drug conjugate (ADC) include the choice of the
targeting antibody, linker, payload, and the drug‐to‐antibody ratio (DAR). Historically, most …

[HTML][HTML] Bivalent EGFR-targeting DARPin-MMAE conjugates

L Karsten, N Janson, V Le Joncour, S Alam… - International Journal of …, 2022 - mdpi.com
Epidermal growth factor receptor (EGFR) is a validated tumor marker overexpressed in
various cancers such as squamous cell carcinoma (SSC) of the head and neck and gliomas …

Azobenzene‐Based Linker Strategy for Selective Activation of Antibody–Drug Conjugates

D Xiao, L Liu, F Xie, J Dong, Y Wang, X Xu… - Angewandte …, 2024 - Wiley Online Library
Existing antibody–drug conjugate (ADC) linkers, whether cleavable or non‐cleavable, are
designed to release highly toxic payloads or payload derivatives upon internalisation of the …

Pharmacokinetics of trastuzumab deruxtecan (T-DXd), a novel anti-HER2 antibody-drug conjugate, in HER2-positive tumour-bearing mice

H Okamoto, M Oitate, K Hagihara, H Shiozawa… - Xenobiotica, 2020 - Taylor & Francis
Abstract Trastuzumab deruxtecan (T-DXd, DS-8201a) is an antibody-drug conjugate (ADC),
comprising an anti-HER2 antibody (Ab) at a drug-to-Ab ratio of 7–8 with the topoisomerase I …

[HTML][HTML] Antibody–drug conjugates (ADCs) for personalized treatment of solid tumors: a review

JM Lambert, CQ Morris - Advances in therapy, 2017 - Springer
Attaching a cytotoxic “payload” to an antibody to form an antibody–drug conjugate (ADC)
provides a mechanism for selective delivery of the cytotoxic agent to cancer cells via the …

Generation and characterization of iduronidase-cleavable ADCs

S Jäger, D Könning, N Rasche, F Hart… - Bioconjugate …, 2023 - ACS Publications
A crucial design feature for the therapeutic success of antibody-drug conjugates (ADCs) is
the linker that connects the antibody with the drug. Linkers must be stable in circulation and …

[HTML][HTML] A biparatopic HER2-targeting antibody-drug conjugate induces tumor regression in primary models refractory to or ineligible for HER2-targeted therapy

JY Li, SR Perry, V Muniz-Medina, X Wang, LK Wetzel… - Cancer cell, 2016 - cell.com
Antibody-drug conjugate (ADC) which delivers cytotoxic drugs specifically into targeted cells
through internalization and lysosomal trafficking has emerged as an effective cancer …

Reductively cleavable polymer-drug conjugates based on dendritic polyglycerol sulfate and monomethyl auristatin E as anticancer drugs

N Rades, K Achazi, M Qiu, C Deng, R Haag… - Journal of Controlled …, 2019 - Elsevier
Stimuli-responsive polymer-drug conjugates (PDCs) provide promising approaches in
anticancer treatment. Here, we report the synthesis and biological evaluation of PDCs made …