Trastuzumab Deruxtecan

Trastuzumab Deruxtecan is a prescription medication used for the treatment of breast cancer, non-small cell lung cancer, and gastric cancer

• Trastuzumab Deruxtecan is available under various brand names: Enhertu, fam-trastuzumab Deruxtecan-nxki

Common side effects of Trastuzumab Deruxtecan include:

• nausea,
• vomiting,
• loss of appetite,
• diarrhea,
• constipation,
• cough,
• tiredness,
• hair loss, and
• low blood cell counts

Serious side effects of Trastuzumab Deruxtecan include:

• hives,
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• chest tightness,
• wheezing,
• cough,
• new or worsening shortness of breath,
• fever,
• tiredness,
• dizziness,
• pounding heartbeats,
• fluttering in the chest,
• swelling in the lower legs,
• sudden weight gain,
• lightheadedness,
• chills,
• tiredness,
• mouth sores,
• skin sores,
• easy bruising,
• unusual bleeding,
• pale skin, and
• cold hands and feet sweating, and
• tremor.

Rare side effects of Trastuzumab Deruxtecan include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Injection, lyophilized powder for reconstitution

• 100 mg/vial

HER2-Positive Breast Cancer

Adult dosage

• 5.4 mg/kg IV every 3 weeks  (21-day cycle)

HER2-Low Breast Cancer

Adult dosage

• 5.4 mg/kg IV every 3 weeks (21-day cycle)

Non-small Cell Lung Cancer

Adult dosage

• 5.4 mg/kg IV every 3 weeks (21-day cycle)

Gastric Cancer

Adult dosage

• 6.4 mg/kg IV every 3 weeks (21-day cycle)

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Trastuzumab Deruxtecan has no noted severe interactions with any other drugs.
• Trastuzumab Deruxtecan has no noted serious interactions with any other drugs.
• Trastuzumab Deruxtecan has no noted moderate interactions with any other drugs.
• Trastuzumab Deruxtecan has no noted minor interactions with any other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Trastuzumab Deruxtecan?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Trastuzumab Deruxtecan?”

Cautions

• Severe, life-threatening, or fatal interstitial lung disease (ILD), including pneumonitis, can occur
• Decrease in neutrophil count reported in metastatic breast cancer and HER2-mutant solid tumor (5.4 mg/kg); median time to the first onset of decreased neutrophil count 22 days; in local advanced or metastatic gastric cancer (6.4 mg/kg) or GEJ adenocarcinoma, decrease in neutrophil count also reported; median time to first onset of decreased neutrophil count 16 days
• Febrile neutropenia was reported; monitor complete blood cell counts before initiation and before each dose, and as clinically indicated
• Left ventricular ejection fraction (LVEF) decrease reported in metastatic breast cancer and HER2-mutant solid tumors and locally advanced or metastatic gastric cancer; may be at increased risk of developing left ventricular dysfunction; asymptomatic LVEF decrease reported
• May cause fetal harm when administered to a pregnant female
• Interstitial lung disease
  • Promptly investigate evidence of ILD; evaluate suspected ILD by radiographic imaging
  • Consider pulmonology consult
  • See Dosage Modifications for details regarding corticosteroid treatment
  • Permanently discontinue for Grade ≥2
• Drug interaction overview
  • Trastuzumab Deruxtecan is a substrate of OATP1B1, OATP1B3, MATE2-K, P-gp, CYP3A4, MRP1, and BCRP; in vitro studies did not show evidence of meaningful clinical impact

Pregnancy & Lactation

• Based on its mechanism of action, fetal harm may occur when administered to pregnant women
• No data are available on use in pregnant women
• Monitor women who received trastuzumab Deruxtecan during pregnancy or within 7 months before conception for oligohydramnios; if oligohydramnios occurs, perform fetal testing that is appropriate for gestational age and consistent with community standards of care
• Advise patients of potential fetal risks
• Clinical considerations
  • Monitor women who received treatment during pregnancy or within 7 months before conception for oligohydramnios
  • If oligohydramnios occurs, perform fetal testing that is appropriate for gestational age and consistent with community standards of care
• Contraception
  • Females of reproductive potential: Use effective contraception during treatment and for at least 7 months following the last dose
  • Males with female partners of reproductive potential: Use effective contraception during treatment and for at least 4 months following the last dose
• Infertility
  • Based on findings in animal toxicity studies, may impair male reproductive function and fertility persist for an unknown duration; whether therapy affects male fertility is unknown
• Lactation
  • There is no data regarding the presence of fam-trastuzumab Deruxtecan-nxki in human milk, the effects on the breastfed child, or the effects on milk production
  • Advise women not to breastfeed during treatment and for 7 months after the last dose