Zongertinib (marketed as Hernexeos) is an oral, irreversible, HER2-selective tyrosine kinase inhibitor (TKI) approved for previously treated, advanced, or metastatic HER2-mutant non-small-cell lung cancer (NSCLC).
An oral, irreversible tyrosine kinase inhibitor that selectively inhibits HER2 while sparing wild type epidermal growth factor receptor (EGFR), minimizing associated to toxic effects.
It acts by targeting HER2 mutations while sparing wild-type EGFR to reduce toxicity.
Common side effects include diarrhea, fatigue, and nausea.
Selectively inhibits HER2 tyrosine kinase, with significant efficacy in patients with HER2-mutated solid tumors.
< 90 kg: 120 mg orally once daily. 90 kg or more: 180 mg orally once daily.
Side Effects: The most common adverse effect is diarrhea (approximately 50% of patients), which is usually low-grade (1 or 2) and manageable with medication like loperamide.
Other reported, less common side effects include fatigue, nausea, rash, and increased ALT/AST.
Efficacy: In the Beamion LUNG-1 trial, zongertinib demonstrated a 71%–77% objective response rate in pre-treated HER2-mutant NSCLC patients.
It showed sustained efficacy in previously untreated patients or metastatic HER2 mutant NSCLC.