Monoclonal antibody | |
---|---|
Type | Whole antibody |
Source | Humanized |
Target | HER2 |
Clinical data | |
Trade names | Enhertu |
Other names | DS-8201a, fam-trastuzumab deruxtecan-nxki |
AHFS/Drugs.com | Monograph |
MedlinePlus | a620006 |
License data | |
Pregnancy category | |
Routes of administration | Intravenous |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
CAS Number | |
PubChem SID | |
DrugBank | |
UNII | |
KEGG | |
ChEMBL | |
Chemical and physical data | |
Formula | C6460H9972N1724O2014S44.(C52H57F1N9O13)8 |
Trastuzumab 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).[11][12] It is licensed for the treatment of breast cancer or gastric or gastroesophageal adenocarcinoma.[12][13] Trastuzumab binds to and blocks signaling through epidermal growth factor receptor 2 (HER2/neu) on cancers that rely on it for growth. Additionally, once bound to HER2 receptors, the antibody is internalized by the cell, carrying the bound deruxtecan along with it, where it interferes with the cell's ability to make DNA structural changes and replicate its DNA during cell division, leading to DNA damage when the cell attempts to replicate itself, destroying the cell.[13]
It was approved for medical use in the United States in December 2019,[12] in Japan in March 2020,[14] in the European Union in January 2021,[8][10] and in Australia in October 2021.[1]
Trastuzumab deruxtecan is the first approved therapy by the US Food and Drug Administration (FDA) targeted to people with the HER2-low breast cancer subtype subset of HER2-negative breast cancer.[15]
AstraZeneca PR 20210120
was invoked but never defined (see the help page).FDA 20210115
was invoked but never defined (see the help page).