Enhertu

Generic name: fam-trastuzumab deruxtecan [ FAM-tras-TOOZ-ue-mab-DER-ux-TEE-kan ]
Dosage form: intravenous infusion (100mg vial)
Drug class: HER2 inhibitors

Medically reviewed by Melisa Puckey, BPharm. Last updated on Feb 15, 2023.

What is Enhertu?

Enhertu (fam-trastuzumab-deruxtecan) is a targeted therapy cancer medicine that is used to treat types of HER2-positive and HER2-Low breast cancer, HER2 positive stomach cancer and non-small cell lung cancer (NSCLC) that has HER2 (ERBB2) mutations. 

Enhertu works by preventing cancer cells from multiplying which slows the cancer growth and progression, and then its second action is to damage or kill the cancer cells.

Enhertu is made up of two cancer-fighting medicines joined together, a monoclonal antibody (fam-trastuzumab) and a chemotherapy drug (topoisomerase I inhibitor). Enhertu is an HER2-directed antibody and topoisomerase inhibitor conjugate.

Enhertu is usually given as an infusion into a vein every 3 weeks. The first infusion will take over 90 minutes but your next infusions are usually given over 30 minutes.

Enhertu was first approved by the FDA on December 20, 2019.

How does Enhertu work?

Some cancer cells have too many copies of the human epidermal growth factor receptor 2 (HER2) gene which makes a protein called the HER2, these cancers are called HER2 positive.  HER2 is a protein that controls cell growth, if your cancer is HER2 positive it means it will more likely grow faster, spread or come back.  Some cancer cells that are HER2-negative still have a number of HER2 proteins on the surface of the cells, these cancer cells are called HER2-low. Cancer medicines that block HER2 reduce the cancers ability to grow and spread.

The fam-trastuzumab part of Enhertu attaches to the HER2 protein which stops the cancer from growing and multiplying.

The topoisomerase I inhibitor is the chemotherapy part of Enhertu and damages or kills the cancer cells.  As Enhertu is attached to cancer cells it is less likely to affect normal healthy cells.

Enhertu (fam-trastuzumab deruxtecan-nxki) is not the same medicine as trastuzumab (Herceptin, Herzuma, Kanjinti, Ogivri, Ontruzant, Trazimera). These medicines contain only the trastuzumab, they do not contain topoisomerase I inhibitor.

Enhertu (fam-trastuzumab deruxtecan-nxki) is not the same medicine as Kadcyla (ado-trastuzumab emtansine) which has a different antibody-drug conjugate.

What is Enhertu used for?

Enhertu is FDA-approved for use in adult patients who have:

Breast cancer that is (HER2)-positive

• that is not removable by surgery (unresectable) or has spread to other parts of your body (metastatic) and 
• have already had anti-HER2 breast cancer treatment:
  • for cancer that as spread to another part of your body, or
  • have breast cancer that has come back during treatment or within 6 months of completing treatment of early-stage breast cancer.
     

Breast cancer that is HER2-low (IHC 1+ or IHC 2+/ISH-)

• that is not removable by surgery or has spread to other parts of your body and
  • have already had chemotherapy for cancer that has spread (metastatic) or
  • cancer has returned during or within six months of completing adjuvant chemotherapy after surgery.  

Stomach cancer that is HER2-positive

• gastric or gastroesophageal junction (GEJ) adenocarcinoma cancer, and
• you have already had a trastuzumab-based regimen and cancer has
  • spread to areas near your stomach (locally advanced) or
  • that has spread to other parts of your body (metastatic).

Non-small cell lung cancer (NSCLC) that has activating HER2 (ERBB2) mutations

• that cannot be removed by surgery or cancer that has spread to other parts of your body (metastatic), and
• you have already had systemic therapy, and
• activating HER2 (ERBB2) mutations have been detected by a FDA-approved test.

Important information

Enhertu can cause serious side effects, including:

• Lung problems. These may be severe, life-threatening or may lead to death. If you develop lung problems while on the medicine you maybe prescribed a corticosteroid medicine. It is important to tell your healthcare provider right away if you get any of the following signs and symptoms of lung problems:
  • shortness of breath or trouble breathing
  • cough
  • fever
  • any change in breathing or any new or worsening breathing symptoms such as wheezing or chest tightness.

• Low white blood cell count (neutropenia). It is common for this medicine to cause low white blood cell counts, and this can sometimes be severe. You should have your white blood cell levels checked before starting this medicine and again before starting each dose. If you develop any signs or symptoms of an infection or have fever or chills during treatment with this medicine, it is important to tell your healthcare provider right away.
• Heart problems. This medicine may affect the heart's ability to pump blood. You should have your heart function checked before starting treatment. If you get any of the following signs and symptoms, it is important to tell your healthcare provider right away:
  • irregular heartbeat
  • sudden weight gain
  • swelling of your ankles or legs
  • new or worsening shortness of breath
  • coughing
  • feeling tired
  • dizziness or feeling light-headed
  • loss of consciousness.

During your treatment with this medicine, your healthcare provider will check you for any of the side effects above. Your healthcare provider may reduce your dose, delay treatment or completely stop treatment with this medicine if you have severe side effects.

• Harm to your unborn baby. Tell your healthcare provider right away if you become pregnant or think you might be pregnant during treatment with this medicine.
  • If you are able to become pregnant, your healthcare provider should do a pregnancy test before you start treatment with this medicine.
  • See the section below for more information about pregnancy, breastfeeding, and this medicine.
  • Males who have female partners that are able to become pregnant should use effective birth control (contraception) during treatment with this medicine and for at least 4 months after the last dose.

What should I tell my healthcare provider before using Enhertu?

Before starting this medicine, you should tell your healthcare provider about all of your medical conditions, especially if you:

• have any lung or breathing issues.
• have symptoms or signs of infection.
• have or have had in the past any heart problems.

Pregnancy

You should not take Enhertu if you are pregnant or planning a pregnancy, as it can harm your unborn baby.

• If you are able to become pregnant, your healthcare provider should do a pregnancy test before you start treatment with this medicine.
• Females who are able to become pregnant should use effective birth control (contraception) during treatment with this medicine and for at least 7 months after the last dose.
• Males who have female partners that are able to become pregnant should use effective birth control (contraception) during treatment with Enhertu and for at least 4 months after the last dose.
• This medicine may cause fertility problems in males, which may affect the ability to father children. Talk to your healthcare provider if you have concerns about fertility.

Breastfeeding

Enhertu and breastfeeding:

• It is not known if Enhertu passes into your breast milk.
• Do not breastfeed during treatment with Enhertu and for 7 months after the last dose.

Dosing information

Do not substitute Enhertu for or with trastuzumab (Herceptin, Herzuma, Kanjinti, Ogivri, Ontruzant, Trazimera) or adotrastuzumab emtansine (Kadcyla). They are not the same medicine.

Enhertu is given into your vein as an intravenous infusion once every three weeks. The first infusion will take over 90 minutes, but your next infusions are usually given over 30 minutes.

Enhertu may make your feel sick, and you may vomit. Your doctor may prescribe a medicine to prevent nausea and vomiting.

During an infusion it is possible to have an infusion-related reaction. If this happens, your healthcare provider may slow down or temporarily stop your infusion, if you have a severe infusion reaction, your healthcare provider may stop this treatment permanently.

If you develop side effects or your cancer progresses, your dose reduce may be reduced, treatment may be paused or even stopped.

The dose you will receive will depend on how much you weigh and your type of cancer.

What are the possible side effects of Enhertu?

Enhertu can cause serious side effects. See "Important information” above.

The most common side effects of Enhertu when used for metastatic breast cancer, HER2-mutant non-small cell lung cancer, HER2-positive gastric, or GEJ adenocarcinoma include:

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

When Enhertu was used for metastatic breast cancer and HER2-mutant non-small cell lung cancer patients another most common side effect was:

• cough
• muscle or bone pain

When Enhertu was used for HER2-positive gastric or GEJ adenocarcinoma another most common side effect was:

• fever.

Enhertu may cause fertility problems in males, which may affect the ability to father children. If you have concerns about your fertility talk to your healthcare provider.

These are not all of the possible side effects of this medicine. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Interactions

Some medications interact with Enhertu, so it is important to tell your doctor about any medicines that you are currently taking, or if you start or stop any medicine while you are having cancer treatment. Also tell your doctor about any vaccinations, over-the-counter medicines, vitamins, minerals or herbal products that you take.

Storage

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

What are the ingredients in Enhertu?

Active Ingredient: fam-trastuzumab deruxtecan-nxki.

Inactive Ingredients: L-histidine, L-histidine hydrochloride monohydrate, polysorbate 80, and sucrose.

Manufacturer

Enhertu is manufactured by: Daiichi Sankyo, Inc., Basking Ridge, NJ 07920 U.S. License No. 2128.

Enhertu is marketed by: Daiichi Sankyo, Inc., Basking Ridge, NJ 07920 and AstraZeneca Pharmaceuticals LP, Wilmington, DE 19850.

 

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Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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