HER2 inhibitor
HER2 kinase inhibitor
- Suppresses HER2-amplified tumors
- Used in breast cancer
- Cardiac HER2 blockade can impair myocardial function → monitor ejection fraction
- Cardiotoxicity with the antibody agents
Drugs with this mechanism (2)
- Lapatinib — Oral HER2/EGFR inhibitor used in combination for HER2-positive breast cancer; diarrhea, hepatotoxicity, and cardiac dysfunction.
- Tucatinib — HER2-selective kinase inhibitor that crosses into brain metastases; strong 3A4 inhibitor.
Self-check
- Which tumors are targeted by HER2 blockade?
HER2-amplified tumors. - What cardiac measure should be monitored during HER2 blockade?
Ejection fraction.
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