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Do not substitute ENHERTU for or with trastuzumab or trastuzumab emtansine.
Patient Selection for HER2-low Metastatic Breast Cancer: Select patients for treatment of unresectable or metastatic HER2-low breast cancer based on IHC 1+ or IHC 2+/ISH- tumor status.
Premedication: ENHERTU is emetogenic (see Adverse Reactions), which includes delayed nausea and/or vomiting. Prior to each dose of ENHERTU, patients should be premedicated with a combination regimen of two or three medicinal products (e.g., dexamethasone with either a 5-HT3 receptor antagonist and/or an NK1 receptor antagonist, as well as other medicinal products as indicated) for prevention of chemotherapy-induced nausea and vomiting.
Posology: The initial dose should be administered as a 90-minute intravenous infusion. If the prior infusion was well tolerated, subsequent doses of ENHERTU may be administered as 30-minute infusions.
The infusion rate of ENHERTU should be slowed or interrupted if the patient develops infusion-related symptoms. ENHERTU should be permanently discontinued in case of severe infusion reactions.
Metastatic Breast Cancer: The recommended dose of ENHERTU is 5.4 mg/kg given as an intravenous infusion once every 3 weeks (21-day cycle) until disease progression or unacceptable toxicity.
Locally Advanced or Metastatic Gastric Cancer: The recommended dose of ENHERTU is 6.4 mg/kg given as an intravenous infusion once every 3 weeks (21-day cycle) until disease progression or unacceptable toxicity.
Dose Modifications: Management of adverse reactions may require temporary interruption, dose reduction, or treatment discontinuation of ENHERTU per guidelines provided in Tables 5 and 6.
ENHERTU dose should not be re-escalated after a dose reduction is made. (See Tables 5 and 6.)
Click on icon to see table/diagram/image
Click on icon to see table/diagram/imageDelayed or Missed Dose: If a planned dose is delayed or missed, it should be administered as soon as possible without waiting until the next planned cycle. The schedule of administration should be adjusted to maintain a 3-week interval between doses. The infusion should be administered at the dose and rate the patient tolerated in the most recent infusion.
Special Populations: Geriatrics: No dose adjustment of ENHERTU is required in patients aged 65 years or older.
Of the 1590 patients with HER2-positive breast cancer treated with ENHERTU 5.4 mg/kg, 30.3% were 65 years or older and 5.3% were 75 years or older. No overall difference in efficacy was observed based on age. There was a higher incidence of Grade 3-4 adverse reactions observed in patients aged 65 years or older (55.1%) as compared to younger patients (48.9%).
Of the 125 patients with locally advanced or metastatic HER2-positive gastric or GEJ adenocarcinoma treated with ENHERTU 6.4 mg/kg in DESTINY-Gastric01, 56% were 65 years or older and 14% were 75 years or older. No overall difference in efficacy was observed based on age. There was a higher incidence of ≥Grade 3 adverse reactions observed in younger patients (87%) as compared to patients aged 65 years or older (76%).
Population pharmacokinetic analysis indicates that age does not have a clinically meaningful effect on the pharmacokinetics of trastuzumab deruxtecan.
Pediatrics: The safety and efficacy in children and adolescents below 18 years of age have not been established as there is no relevant use in the pediatric population.
Renal Impairment: No dose adjustment is required in patients with mild (creatinine clearance [CLcr] ≥60 and <90 mL/min) or moderate (CLcr ≥30 and <60 mL/min) renal impairment. Limited data are available in patients with severe renal impairment. A higher incidence of Grade 1 and 2 ILD/pneumonitis leading to an increase in discontinuation of therapy has been observed in patients with moderate renal impairment. Patients with moderate or severe renal impairment should be monitored carefully (see Precautions).
Hepatic Impairment: No dose adjustment is required in patients with mild (total bilirubin ≤ULN and any AST >ULN or total bilirubin >1 to 1.5 times ULN and any AST) hepatic impairment. There are insufficient data to make a recommendation on dose adjustment in patients with moderate (total bilirubin >1.5 to 3 times ULN and any AST) hepatic impairment. No data are available in patients with severe (total bilirubin >3 to 10 times ULN and any AST) hepatic impairment.
Method of Administration: ENHERTU is for intravenous use. It must be reconstituted and diluted by a healthcare professional and administered as an intravenous infusion. ENHERTU must not be administered as an intravenous push or bolus.
For instructions on reconstitution and dilution of ENHERTU before administration, see Special precautions for disposal and other handling under Cautions for Usage.
