Enhertu works by preventing cancer cells from multiplying, which slows down the growth and progression of cancer, and then its second action is to damage or kill cancer cells.
Enhertu consists of two anti-cancer drugs combined: a monoclonal antibody (fam-trastuzumab) and a chemotherapy drug (a topoisomerase I inhibitor). Enhertu is a conjugate of anti-HER2 antibodies and a topoisomerase inhibitor.
Enhertu is usually given intravenously every 3 weeks. The first infusion will take over 90 minutes, but your next infusions are usually over 30 minutes.
Enhertu was first approved by the FDA on December 20, 2019.
How does Enertu work?
Some cancer cells have too many copies of the human epidermal growth factor receptor 2 (HER2) gene, which makes a protein called HER2, these cancers are called HER2 positive. HER2 is a protein that controls cell growth. If your cancer is HER2 positive, it means it is more likely to grow faster, spread, or come back. Some cancer cells that are HER2 negative still have a number of HER2 proteins on the cell surface, these cancer cells are called HER2-low. Cancer drugs that block HER2 reduce the ability of cancer to grow and spread.
Part of the fam-trastuzumab Enhertu attaches to the HER2 protein, which stops the growth and reproduction of cancer.
The topoisomerase I inhibitor is part of Enhertu’s chemotherapy and damages or kills cancer cells. Because Enhertu attaches itself to cancer cells, it is less likely to affect normal healthy cells.
Enhertu (Fam-trastuzumab Deruxtecan-nkski) is not the same medicine as trastuzumab (Herceptin, Herzuma, Canjinti, Revri, Ontrusant, Trasimera). These drugs contain only trastuzumab, they do not contain a topoisomerase I inhibitor.
Enhertu (fam-trastuzumab derukstecan-nkski) is not the same drug as Kadcyla (ado-trastuzumab emtansine), which has a different antibody-drug conjugate.
What is Enertu used for?
Enhertu is FDA approved for use in adult patients who have:
Breast cancer that is (HER2) positive
that is not removed surgically (unresectable) or has spread to other parts of the body (metastatic) and
have already undergone anti-HER2 treatment for breast cancer:
for cancer that has spread to another part of your body, or
you have breast cancer that returned during treatment or within 6 months of completing early breast cancer treatment.
Low HER2 breast cancer (IHC 1+ or IHC 2+/ISH-)
that cannot be removed surgically or has spread to other parts of the body and
have already had chemotherapy for cancer that has spread (metastatic) or
the cancer returned during or within six months of completing adjuvant chemotherapy after surgery.
Stomach cancer that is HER2 positive
cancer of the stomach or gastroesophageal junction (GEJ) adenocarcinoma, and
you already had a trastuzumab-based regimen and cancer
spread to areas near the stomach (locally advanced) or
that has spread to other parts of your body (metastatic).
Non-small cell lung cancer (NSCLC) with HER2 activating mutations (ERBB2)
that cannot be removed surgically, or cancer that has spread to other parts of the body (metastatic), and
you have already had systemic therapy, and
HER2 (ERBB2) activating mutations have been detected using an FDA-approved test.
Related/similar drugs
Ibrance, Opdivo, Retevmo, Rybrevant, Lumacras, methotrexate, Keytruda
Important information
Enhertu can cause serious side effects, including:
Lung problems. They can be severe, life-threatening or can lead to death. If you have lung problems while taking this medicine, you may have been prescribed a corticosteroid medicine. It is important to tell your healthcare provider right away if you develop any of the following signs and symptoms of lung problems:
shortness of breath or difficulty breathing
cough
heat
any changes in breathing or any new or worsening breathing symptoms such as wheezing or chest tightness.
