Fam-trastuzumab deruxtecan-nxki

What is Fam-trastuzumab deruxtecan-nxki?

• Fam-trastuzumab deruxtecan-nxki (Enhertu) is a HER2-directed antibody and topoisomerase inhibitor conjugate used for the treatment of breast cancer or for the treatment of gastric or gastroesophageal adenocarcinoma.

What are the uses of this medicine?

This medicine is used in adults to treat human epidermal growth factor receptor 2 (HER2)-positive:

• breast cancer that cannot be removed by surgery or that has spread to other parts of your body (metastatic), and who have received two or more prior anti-HER2 breast cancer treatments.
• stomach cancer called gastric or gastroesophageal junction (GEJ) adenocarcinoma that has spread to areas near your stomach (locally advanced) or that has spread to other parts of your body (metastatic), and who have received a prior trastuzumab-based regimen.

How does this medicine work?

• Fam-trastuzumab deruxtecan-nxki is a HER2-directed antibody-drug conjugate.
• The antibody is a humanized anti-HER2 IgG1.
• The small molecule, DXd, is a topoisomerase I inhibitor attached to the antibody by a cleavable linker.
• Following binding to HER2 on tumor cells, fam-trastuzumab deruxtecan-nxki undergoes internalization and intracellular linker cleavage by lysosomal enzymes. Upon release, the membrane-permeable DXd causes DNA damage and apoptotic cell death.

Who Should Not Use this medicine ?

• This medicine have no usage limittations.

Is this medicine FDA approved?

• It was approved for use in the United States in 2019.

How should this medicine be used?

• Select patients with locally advanced or metastatic gastric cancer based on HER2 protein overexpression or HER2 gene amplification.

Recommended Dosage

Recommended Dosage for Metastatic Breast Cancer

• The recommended dosage 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.

Recommended Dosage for Locally Advanced or Metastatic Gastric Cancer

• The recommended dosage 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.

• Management of adverse reactions (ILD, neutropenia, thrombocytopenia, or left ventricular dysfunction) may require temporary interruption, dose reduction, or discontinuation of Enhertu.

Administration

• You will receive Enhertu into your vein through an intravenous (IV) line by your healthcare provider.
• Enhertu is given 1 time every three weeks (21-day treatment cycle).
• Your healthcare provider will decide how many treatments you need.
• Your healthcare provider may slow down or temporarily stop your infusion of Enhertu if you have an infusion-related reaction, or permanently stop Enhertu if you have severe infusion reactions.
• If you miss a planned dose of Enhertu, call your healthcare provider right away to schedule an appointment. Do not wait until the next planned treatment cycle.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As injection: 100 mg lyophilized powder in a single-dose vial

This medicine is available in fallowing brand namesː

• Enhertu

What side effects can this medication cause?

The most common side effects of this medicine include:

The most common side effects of Enhertu, when used in people with breast cancer, include:

• nausea
• low white blood cell counts
• low red blood cell counts
• feeling tired
• vomiting
• hair loss
• increased liver function tests
• low platelet counts
• constipation
• decreased appetite
• diarrhea
• low levels of blood potassium
• cough

The most common side effects of Enhertu, when used in people with stomach cancer, include:

• low red blood cell counts
• low white blood cell counts
• low platelet counts
• nausea
• decreased appetite
• increased liver function tests
• feeling tired
• diarrhea
• low levels of blood potassium
• vomiting
• constipation
• fever
• hair loss

Enhertu can cause serious side effects, including:

• Lung problems that may be severe, life-threatening or that may lead to death
• Low white blood cell count (neutropenia)
• Heart problems that may affect your heart's ability to pump blood

What special precautions should I follow?

• Monitor complete blood counts prior to initiation of Enhertu and prior to each dose, and as clinically indicated. Manage through treatment interruption or dose reduction.
• Patients treated with Enhertu may be at increased risk of developing left ventricular dysfunction. Assess LVEF prior to initiation of Enhertu and at regular intervals during treatment as clinically indicated. Manage through treatment interruption or discontinuation. Permanently discontinue Enhertu in patients with symptomatic congestive heart failure (CHF).

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Based on its mechanism of action, Enhertu can cause fetal harm when administered to a pregnant woman.
• There are no available data on the use of Enhertu in pregnant women.

Can this medicine be used in children?

• Safety and effectiveness of Enhertu have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: fam-trastuzumab deruxtecan-nxki.
• Inactive Ingredients: L-histidine, L-histidine hydrochloride monohydrate, polysorbate 80, and sucrose.

Who manufactures and distributes this medicine?

Manufactured by: Daiichi Sankyo, Inc., Basking Ridge, NJ 07920 U.S. License No. 2128 Marketed by: Daiichi Sankyo, Inc., Basking Ridge, NJ 07920 and AstraZeneca Pharmaceuticals LP, Wilmington, DE 19850 Enhertu® is a registered trademark of Daiichi Sankyo Company, Ltd.

What should I know about storage and disposal of this medication?

• Store vials in a refrigerator at 2°C to 8°C (36°F to 46°F) in the original carton to protect from light until time of reconstitution.
• Do not freeze.
• Do not shake the reconstituted or diluted solution.

Special Handling

• Enhertu (fam-trastuzumab deruxtecan-nxki) is a cytotoxic drug. Follow applicable special handling and disposal procedures.

• Dailymed label info on Fam-trastuzumab deruxtecan-nxki
• FDA Fam-trastuzumab deruxtecan-nxki

Fam-trastuzumab deruxtecan-nxki Resources
Latest articles Most recent articles Ongoing trials	Wikipedia