[HTML][HTML] Designing antibodies as therapeutics

PJ Carter, A Rajpal - Cell, 2022 - cell.com
Antibody therapeutics are a large and rapidly expanding drug class providing major health
benefits. We provide a snapshot of current antibody therapeutics including their formats …

[HTML][HTML] Antibody–drug conjugates: The last decade

N Joubert, A Beck, C Dumontet, C Denevault-Sabourin - Pharmaceuticals, 2020 - mdpi.com
An armed antibody (antibody–drug conjugate or ADC) is a vectorized chemotherapy, which
results from the grafting of a cytotoxic agent onto a monoclonal antibody via a judiciously …

Antitumor activity and safety of trastuzumab deruxtecan in patients with HER2-low–expressing advanced breast cancer: results from a phase Ib study

S Modi, H Park, RK Murthy, H Iwata… - Journal of Clinical …, 2020 - ascopubs.org
PURPOSE Trastuzumab deruxtecan (T-DXd, formerly DS-8201a) is a novel human
epidermal growth factor receptor 2 (HER2)-targeted antibody drug conjugate (ADC) with a …

The dawn of a new era: targeting the “undruggables” with antibody-based therapeutics

L Qian, X Lin, X Gao, RU Khan, JY Liao, S Du… - Chemical …, 2023 - ACS Publications
The high selectivity and affinity of antibodies toward their antigens have made them a highly
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …

Precision oncology in metastatic colorectal cancer—from biology to medicine

F Di Nicolantonio, PP Vitiello, S Marsoni… - Nature reviews Clinical …, 2021 - nature.com
Remarkable progress has been made in the development of biomarker-driven targeted
therapies for patients with multiple cancer types, including melanoma, breast and lung …

Datopotamab deruxtecan, a novel TROP2-directed antibody–drug conjugate, demonstrates potent antitumor activity by efficient drug delivery to tumor cells

D Okajima, S Yasuda, T Maejima, T Karibe… - Molecular cancer …, 2021 - AACR
Trophoblast cell surface antigen 2 (TROP2) is highly expressed on various epithelial tumors
and correlates with poor prognosis. We developed the novel TROP2-directed antibody–drug …

Strategies and challenges for the next generation of antibody–drug conjugates

A Beck, L Goetsch, C Dumontet… - Nature reviews Drug …, 2017 - nature.com
Antibody–drug conjugates (ADCs) are one of the fastest growing classes of oncology
therapeutics. After half a century of research, the approvals of brentuximab vedotin (in 2011) …

Targeting HER2 with trastuzumab deruxtecan: a dose-expansion, phase I study in multiple advanced solid tumors

J Tsurutani, H Iwata, I Krop, PA Jänne, T Doi… - Cancer discovery, 2020 - AACR
HER2-targeted therapies are approved only for HER2-positive breast and gastric cancers.
We assessed the safety/tolerability and activity of the novel HER2-targeted antibody–drug …

Trastuzumab deruxtecan (DS-8201a) in patients with advanced HER2-positive breast cancer previously treated with trastuzumab emtansine: a dose-expansion …

K Tamura, J Tsurutani, S Takahashi, H Iwata… - The Lancet …, 2019 - thelancet.com
Background Trastuzumab deruxtecan (DS-8201a) is a novel HER2-targeted antibody–drug
conjugate with a humanised anti-HER2 antibody, cleavable peptide-based linker, and …

DS-8201a, a novel HER2-targeting ADC with a novel DNA topoisomerase I inhibitor, demonstrates a promising antitumor efficacy with differentiation from T-DM1

Y Ogitani, T Aida, K Hagihara, J Yamaguchi, C Ishii… - Clinical Cancer …, 2016 - AACR
Purpose: An anti-HER2 antibody–drug conjugate with a novel topoisomerase I inhibitor, DS-
8201a, was generated as a new antitumor drug candidate, and its preclinical pharmacologic …