Which medications in the drug class Antineoplastics, Anti-HER2 are used in the treatment of Gastric Cancer?

Updated: Feb 23, 2021
  • Author: Elwyn C Cabebe, MD; Chief Editor: N Joseph Espat, MD, MS, FACS  more...
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Answer

Antineoplastics, Anti-HER2

Monoclonal antibodies are a form of drug delivery that specifically targets the tumor cells, thus reducing the systemic side effects of chemotherapy and at the same time being more effective than routine forms of chemotherapy agents.

Trastuzumab (Herceptin)

Trastuzumab is a monoclonal antibody that binds to the human epidermal growth factor receptor 2 protein (HER-2) extracellular domain. It inhibits the proliferation of cells overexpressing HER-2 protein.

Trastuzumab deruxtecan (Enhertu, Fam-trastuzumab deruxtecan-nxki)

This conjugate comprises trastuzumab, a humanized anti-HER2 monoclonal antibody, attached to deruxteca, which is composed of a cleavable linker and topoisomerase inhibitor (DXd). The drug binds to HER2 on tumors and undergoes internalization and intracellular linker cleavage by lysosomal enzymes. Upon release, DXd causes DNA damage and apoptotic cell death. It is approved for locally advanced and metastatic HER2-positive gastric or GE junction adenocarcinoma in patients who were previously treated with a trastuzumab-based regimen.


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