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Common name: fam-trastuzumab deruxtecan
Trade name: Enhertu
Full names: Trastuzumab recombinant lyophilized powder injection, Enhertu, fam-trastuzumab deruxtecan, fam-trastuzumab deruxtecan-nxki, DS8201
Indications:
ENHERTU is a conjugate of an antibody and topoisomerase inhibitor directed against HER2, indicated for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2-based treatment regimens in the metastatic setting.
Do not use trastuzumab or trastuzumab-metansin conjugate (TDM-1) as a substitute for ENHERTU.
The recommended dose of ENHERTU is 5.4 mg/kg as an intravenous infusion every 3 weeks (21-day cycle) until disease progression or unacceptable toxicity.
The first infusion should take more than 90 minutes. If the previous infusion is well tolerated, the infusion time is longer than 30 minutes. If the patient develops infusion-related symptoms, slow down or interrupt the infusion rate. If a serious infusion reaction occurs, permanently discontinue ENHERTU.
If a scheduled dose is delayed or missed, administer the dose as soon as possible; do not wait until the next scheduled cycle. Adjust the dosing schedule to maintain a 3-week interval between doses. Administer the infusion at the dose and rate that the patient tolerated during the most recent infusion.
Adverse reactions:
The most common adverse reactions are interstitial lung disease/pneumonitis, neutropenia, left ventricular dysfunction, etc.
Taboos:
None.
Interstitial lung disease/pneumonitis (ILD): In Enhertu clinical trials, the incidence of interstitial lung disease/pneumonitis (ILD) was 9%, of which 2.6% were fatal. The median time of onset was 4.1 months (range 1.2-8.3 months). Patients should report promptly when they develop cough, difficulty breathing, fever, and/or any new or worsening respiratory symptoms. Use CT to evaluate suspected ILD. For grade 1 ILD, use ≥0.5 mg/kg prednisone or equivalent corticosteroid and withhold Enhertu until recovery. For grade 2+ ILD, use ≥1 mg/kg prednisone or equivalent corticosteroid and permanently discontinue Enhertu.
Neutropenia: In the Enhertu clinical trial, 16% of breast cancer patients developed grade 3 or 4 neutropenia, including 1.7% of neutropenic fever. The median onset time was 1.4 months (range 0.3-18.2 months). Blood routine should be tested before each dose.
Left ventricular dysfunction: In the Enhertu clinical trial, 2 (0.9%) breast cancer patients developed asymptomatic decreased left ventricular ejection fraction. If the patient develops congestive heart failure, or the left ventricular ejection fraction is less than 40%, or the left ventricular ejection fraction decreases or increases by 20% relative to the absolute value before treatment, permanently discontinue Enhertu. Left ventricular ejection fraction should be measured before each dose.
Embryotoxicity: Enhertu should be avoided in pregnant women. Effective contraception should be used during use and for 7 months thereafter.
Refrigerate at 2°C to 8°C (36°F to 46°F). Do not freeze or shake.
fam-trastuzumab deruxtecan-nxki is a HER2-directed antibody-drug conjugate. This antibody is humanized anti-HER2 IgG1. The small molecule DXd is a topoisomerase I inhibitor that is linked to the antibody through a cleavable linker. Upon binding to HER2 on tumor cells, fam-trastuzumab deruxtecan-nxki undergoes internalization and intracellular linker cleavage by lysosomal enzymes. Upon release, membrane-permeable DXd causes DNA damage and apoptotic cell death.