Trastuzumab deruxtecan - Wikipedia
WEBTrastuzumab deruxtecan, sold under the brand name Enhertu, is an antibody-drug conjugate consisting of the humanized monoclonal antibody trastuzumab (Herceptin) covalently linked to the topoisomerase I inhibitor deruxtecan (a derivative of exatecan).
Deruxtecan - Wikipedia
WEBDeruxtecan is a chemical compound and a derivative of exatecan that acts as topoisomerase I inhibitor. [1] It is available linked to specific monoclonal antibody (antibody–drug conjugate), such as: Trastuzumab deruxtecan. It is licensed for the treatment of breast cancer or gastric or gastroesophageal adenocarcinoma. [2]
Discovery and development of trastuzumab deruxtecan and …
WEBMay 16, 2021 · Trastuzumab deruxtecan (T-DXd, DS-8201) is an anti-HER2 human monoclonal IgG1 antibody, with the same amino acid sequence as trastuzumab, covalently linked to deruxtecan, which consists of an enzymatically cleavable peptide-based linker and a novel topoisomerase I inhibitor exatecan derivative (DXd), …
Trastuzumab Deruxtecan: Changing the Destiny of HER2 …
WEBApr 30, 2021 · Trastuzumab deruxtecan (T-DXd) is a novel HER2-directed antibody drug conjugate showing significant anti-tumor activity in heavily pre-treated HER2-positive breast and gastric cancer patients. Preliminary data have shown promising objective response rates in patients with HER2-positive NSCLC and colorectal cancer.
TOP1-DNA trapping by exatecan and combination therapy with …
WEBJul 7, 2022 · We demonstrate the value of SLFN11 expression and homologous recombination (HR)-deficiency (HRD) as predictive biomarkers of response to exatecan. We also show that exatecan kills cancer cells synergistically with the clinical ATR inhibitor ceralasertib (AZD6738).
TOP1-DNA Trapping by Exatecan and Combination Therapy with …
WEBJul 5, 2022 · Cancer cell–specific targeting with the exatecan derivative Deruxtecan has shown remarkable results in multiple clinical trials, which led to the FDA approval of trastuzumab deruxtecan (Enhertu; ref. 16).
TOP1-DNA Trapping by Exatecan and Combination Therapy with …
WEBJul 5, 2022 · Exatecan and deruxtecan are antineoplastic camptothecin derivatives in development as tumor-targeted-delivery warheads in various formulations including peptides, liposomes, polyethylene glycol nanoparticles, and antibody-drug conjugates. Here, we report the molecular pharmacology of exatecan compar ….
A HER2-Targeting Antibody-Drug Conjugate, Trastuzumab Deruxtecan …
WEBTrastuzumab deruxtecan (DS-8201a), a HER2-targeting antibody-drug conjugate with a topoisomerase I inhibitor exatecan derivative (DX-8951 derivative, DXd), has been reported to exert potent antitumor effects in xenograft mouse models and clinical trials.
Trastuzumab Deruxtecan (DS-8201a): The Latest Research and ... - PubMed
WEBTrastuzumab deruxtecan (DS-8201a) is a next-generation antibody-drug conjugate composed of a monoclonal anti-HER2 antibody and a topoisomerase I inhibitor, an exatecan derivative (DX-8951f).
Antitumor Activity and Safety of Trastuzumab Deruxtecan in …
WEBFeb 14, 2020 · Trastuzumab deruxtecan (T-DXd; formerly DS-8201a) is a novel HER2-targeted antibody drug conjugate (ADC) that was designed to effectively deliver a potent topoisomerase I inhibitor payload (an exatecan derivative) to HER2-expressing cancer cells and thereby limit potential systemic toxicity. 11-13 …