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]
^ abc"Enhertu". Therapeutic Goods Administration (TGA). 18 October 2021. Archived from the original on 23 October 2021. Retrieved 22 October 2021.
^"Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 21 December 2022. Archived from the original on 3 April 2022. Retrieved 2 January 2023.
^"AusPAR: Trastuzumab deruxtecan". Therapeutic Goods Administration (TGA). 27 June 2022. Archived from the original on 18 July 2022. Retrieved 17 July 2022.
^"Enhertu (AstraZeneca Pty Ltd)". Therapeutic Goods Administration (TGA). 16 February 2023. Archived from the original on 18 March 2023. Retrieved 9 April 2023.
^"Summary Basis of Decision (SBD) for Enhertu". Health Canada. 23 October 2014. Archived from the original on 30 May 2022. Retrieved 29 May 2022.
^"Enhertu 100 mg powder for concentrate for solution for infusion - Summary of Product Characteristics (SmPC)". (emc). 1 July 2022. Archived from the original on 19 April 2021. Retrieved 1 July 2022.
^"Enhertu- fam-trastuzumab deruxtecan-nxki injection, powder, lyophilized, for solution". DailyMed. Archived from the original on 22 January 2021. Retrieved 15 January 2021.
^ ab"Enhertu EPAR". European Medicines Agency (EMA). 9 December 2020. Archived from the original on 23 March 2021. Retrieved 31 March 2021.
^"Enhertu Product information". Union Register of medicinal products. Archived from the original on 5 March 2023. Retrieved 3 March 2023.
^ abCite error: The named reference AstraZeneca PR 20210120 was invoked but never defined (see the help page).
^"A HER2-Targeting Antibody–Drug Conjugate, Trastuzumab Deruxtecan (DS-8201a), Enhances Antitumor Immunity in a Mouse Model" (PDF). Archived (PDF) from the original on 24 September 2020. Retrieved 23 December 2019.
^ abc"FDA approves new treatment option for patients with HER2-positive breast cancer who have progressed on available therapies". U.S.Food and Drug Administration (FDA) (Press release). 20 December 2019. Archived from the original on 20 December 2019. Retrieved 20 December 2019. This article incorporates text from this source, which is in the public domain.
^ abCite error: The named reference FDA 20210115 was invoked but never defined (see the help page).
^"Enhertu Approved in Japan for Treatment of Patients with HER2 Positive Unresectable or Metastatic Breast Cancer" (Press release). Daiichi Sankyo. 25 March 2020. Archived from the original on 28 January 2021. Retrieved 21 January 2021 – via Business Wire.
^"FDA Approves First Targeted Therapy for HER2-Low Breast Cancer". U.S. Food and Drug Administration (FDA) (Press release). 5 August 2022. Archived from the original on 6 August 2022. Retrieved 5 August 2022. This article incorporates text from this source, which is in the public domain.
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