The latest research and development into the antibody–drug conjugate,[fam-] trastuzumab deruxtecan (DS-8201a), for HER2 cancer therapy

T Nakada, K Sugihara, T Jikoh, Y Abe… - Chemical and …, 2019 - jstage.jst.go.jp
A major limitation of traditional chemotherapy for cancer is dose-limiting toxicity, caused by
the exposure of non-tumor cells to cytotoxic agents. Use of molecular targeted drugs, such …

Ado-trastuzumab emtansine (T-DM1): an antibody–drug conjugate (ADC) for HER2-positive breast cancer

JM Lambert, RVJ Chari - 2014 - ACS Publications
Ado-trastuzumab emtansine (T-DM1) is an antibody–drug conjugate that combines the
antitumor properties of the humanized anti-human epidermal growth factor receptor 2 …

[HTML][HTML] A bifunctional molecule-based strategy for the development of theranostic antibody-drug conjugate

D Xiao, L Zhao, F Xie, S Fan, L Liu, W Li, R Cao, S Li… - Theranostics, 2021 - ncbi.nlm.nih.gov
Antibody-drug conjugates (ADCs) are being developed worldwide with the potential to
revolutionize current cancer treatment strategies. Developing novel theranostic ADCs with …

PF-06804103, a site-specific anti-HER2 antibody–drug conjugate for the treatment of HER2-expressing breast, gastric, and lung cancers

EI Graziani, M Sung, D Ma, B Narayanan… - Molecular cancer …, 2020 - AACR
The approval of ado-trastuzumab emtansine (T-DM1) in HER2+ metastatic breast cancer
validated HER2 as a target for HER2-specific antibody–drug conjugates (ADC). Despite its …

Branched pegylated linker-auristatin to control hydrophobicity for the production of homogeneous minibody-drug conjugate against HER2-positive breast cancer

E Douez, E Allard-Vannier, IAM Amar, L Jolivet… - Journal of Controlled …, 2024 - Elsevier
Trastuzumab emtansine (Kadcyla®) was the first antibody-drug conjugate (ADC) approved
by the Food and Drug Administration in 2013 against a solid tumor, and the first ADC to treat …

Site-specifically labeled antibody–drug conjugate for simultaneous therapy and immunoPET

P Adumeau, D Vivier, SK Sharma, J Wang… - Molecular …, 2018 - ACS Publications
The conjugation of antibodies with cytotoxic drugs can alter their in vivo pharmacokinetics.
As a result, the careful assessment of the in vivo behavior, and specifically the tumor …

Nonclinical development of next-generation site-specific HER2-targeting antibody–drug conjugate (ARX788) for breast cancer treatment

P Nagaraja Shastri, J Zhu, L Skidmore, X Liang… - Molecular cancer …, 2020 - AACR
Conventional antibody–drug conjugates (ADC) utilize native surface-exposed lysines or
cysteines on the antibody of interest to conjugate cytotoxic payload. The nonspecific …

Optimization of a PEGylated glucuronide-monomethylauristatin E linker for antibody–drug conjugates

PJ Burke, JZ Hamilton, SC Jeffrey, JH Hunter… - Molecular Cancer …, 2017 - AACR
The emergence of antibody–drug conjugates (ADC), such as brentuximab vedotin and ado-
trastuzumab emtansine, has led to increased efforts to identify new payloads and develop …

Impact of drug conjugation on pharmacokinetics and tissue distribution of anti-STEAP1 antibody–drug conjugates in rats

CA Boswell, EE Mundo, C Zhang… - Bioconjugate …, 2011 - ACS Publications
Antibody–drug conjugates (ADCs) are designed to combine the exquisite specificity of
antibodies to target tumor antigens with the cytotoxic potency of chemotherapeutic drugs. In …

Bystander killing effect of DS‐8201a, a novel anti‐human epidermal growth factor receptor 2 antibody–drug conjugate, in tumors with human epidermal growth factor …

Y Ogitani, K Hagihara, M Oitate, H Naito… - Cancer …, 2016 - Wiley Online Library
Antibody–drug conjugates deliver anticancer agents selectively and efficiently to tumor
tissue and have significant antitumor efficacy with a wide therapeutic window. DS‐8201a is …