Enhertu

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Brand name: Enhertu

Chemical name: Fam-trastuzumab-deruxtecan-nxki

Class: Antibody-drug conjugate targeted therapy. Enhertu is made up of three parts:

  • fam-trastuzumab: an anti-HER2 medicine that has the same basic structure as Herceptin (chemical name: trastuzumab)
  • a topoisomerase I inhibitor chemotherapy called DXd: topoisomerase-I inhibitors work by interfering with the cancer cells’ ability to replicate; this type of chemotherapy is not typically used to treat HER2-positive breast cancers, so researchers believe it is less likely that the cancers will develop resistance to it
  • a compound that links the fam-trastuzumab molecule to the topoisomerase I inhibitor chemotherapy molecule

The combination of the topoisomerase I inhibitor and the linking compound is called deruxtecan. The linking compound attaches (conjugates) the fam-trastuzumab to the topoisomerase I inhibitor chemotherapy.

Kadcyla is another antibody-drug conjugate targeted therapy used to treat breast cancer.

Uses: Enhertu is used to treat unresectable (not able to be removed with surgery) and metastatic HER2-positive breast cancer that has been treated with two or more anti-HER2 therapies.

How it’s given: Enhertu is given intravenously, which means the medicine is delivered directly into your bloodstream through an IV or port.

Additional information: The topoisomerase I inhibitor chemotherapy part of Enhertu, like other chemotherapy medicines, interferes with cells’ ability to replicate. The topoisomerase I inhibitor isn’t a targeted medicine, which means it can affect healthy cells as well as cancer cells. Enhertu was designed to deliver the topoisomerase I inhibitor to cancer cells in a targeted way by attaching the topoisomerase I inhibitor to the fam-trastuzumab. The fam-trastuzumab then carries the topoisomerase I inhibitor to the HER2-positive cancer cells. This way, the topoisomerase I inhibitor is less toxic to healthy cells and more effective in treating cancer cells.

Side effects:

Read more about Enhertu.


Reference

  1. Enhertu prescribing information, 2019. Available at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/761139s000lbl.pdf (PDF).
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