Trastuzumab deruxtecan

Trastuzumab deruxtecan also known as fam-trastuzumab deruxtecan and sold under the brand name Enhertu, is a medication used for the treatment of adults with unresectable (unable to be removed with surgery) or metastatic (when cancer cells spread to other parts of the body) HER2-positive breast cancer who have received two or more prior anti-HER2-based regimens in the metastatic setting.[1]

Trastuzumab deruxtecan
Monoclonal antibody
TypeWhole antibody
Clinical data
Trade namesEnhertu
Other namesDS-8201a, fam-trastuzumab deruxtecan-nxki
License data
Routes of
administration		IV
ATC code
  • none
Legal status
Legal status
Identifiers
CAS Number
PubChem SID
DrugBank
UNII
KEGG
Chemical and physical data
FormulaC6460H9972N1724O2014S44.(C52H57F1N9O13)8

Overview

Trastuzumab deruxtecan is an antibody-drug conjugate that includes a human epidermal growth factor receptor 2 (HER2)-directed antibody trastuzumab and a topoisomerase I inhibitor conjugate deruxtecan (a derivative of exatecan).[2][1] It was approved for use in the United States in December 2019.[1]

Side effects and label warnings

The most common side effects are nausea, fatigue, vomiting, alopecia (hair loss), constipation, decreased appetite, anemia (hemoglobin in blood is below the reference range), decreased neutrophil count (white blood cells that help lead your body's immune system response to fight infection), diarrhea, leukopenia (other white blood cells that help the immune system), cough and decreased platelet count (component of blood whose function is to react to bleeding from blood vessel injury by clumping, thereby initiating a blood clot).[1]

The prescribing information for fam-trastuzumab deruxtecan-nxki includes a boxed warning to advise health care professionals and patients about the risk of interstitial lung disease (a group of lung conditions that causes scarring of lung tissues) and embryo-fetal toxicity.[1] Interstitial lung disease and pneumonitis (inflammation of lung tissue), including cases resulting in death, have been reported with fam-trastuzumab deruxtecan-nxki.[1]

History

The U.S. Food and Drug Administration (FDA) approved fam-trastuzumab deruxtecan-nxki in December 2019.[1][3] The application for fam-trastuzumab deruxtecan-nxki was granted accelerated approval, fast track designation, and breakthrough therapy designation.[1]

The FDA approved fam-trastuzumab deruxtecan-nxki based on the results of one clinical trial enrolling 184 female patients with HER2-positive, unresectable and/or metastatic breast cancer who had received two or more prior anti-HER2 therapies in the metastatic setting.[1] These patients were heavily pretreated in the metastatic setting, receiving between two and 17 therapies prior to receiving fam-trastuzumab deruxtecan-nxki.[1] Patients in the clinical trial received fam-trastuzumab deruxtecan-nxki every three weeks and tumor imagining was obtained every six weeks.[1] The overall response rate was 60.3%, which reflects the percentage of patients that had a certain amount of tumor shrinkage with a median duration of response of 14.8 months.[1]

The FDA granted the approval of Enhertu to Daiichi Sankyo.[1]

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References
  1. "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.
  2. A HER2-Targeting Antibody–Drug Conjugate, Trastuzumab Deruxtecan (DS-8201a), Enhances Antitumor Immunity in a Mouse Model
  3. "Drug Trials Snapshot: Enhertu". U.S. Food and Drug Administration (FDA). 20 December 2019. Retrieved 24 January 2020. This article incorporates text from this source, which is in the public domain.

Further reading
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