Fam-trastuzumab deruxtecan-nxki

What is Fam-trastuzumab deruxtecan-nxki?[edit | edit source]

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?[edit | edit source]

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?[edit | edit source]

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 ?[edit | edit source]

This medicine have no usage limittations.

Is this medicine FDA approved?[edit | edit source]

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

How should this medicine be used?[edit | edit source]

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?[edit | edit source]

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?[edit | edit source]

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?[edit | edit source]

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?[edit | edit source]

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?[edit | edit source]

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?[edit | edit source]

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

What are the active and inactive ingredients in this medicine?[edit | edit source]

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

Who manufactures and distributes this medicine?[edit | edit source]

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?[edit | edit source]

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.

Fam-trastuzumab deruxtecan-nxki Resources
Need Help Finding a Doctor? Need help finding a doctor or specialist anywhere in the world? Explore our world directory. WikiMD's DocFinder can assist you in locating millions of physicians.	Medical Knowledge Access the latest research - Most recent articles Ongoing trials.