Zongertinib is zongertinib is an orally bioavailable, selective tyrosine kinase inhibitor that irreversibly targets activating HER2 mutations, including exon 20 insertions, used to inhibit downstream oncogenic signaling in patients with HER2-mutant non-small cell lung cancer. It covalently binds to the HER2 receptor, including exon 20 insertions, and inhibits downstream signaling pathways while sparing wild-type epidermal growth factor receptor (EGFR), which serves to limit associated toxicities.
- Mechanism
- Curator reviewed · 8 references
Human epidermal growth factor receptor 2 (HER2) mutations have emerged as important oncogenic drivers in non-small cell lung cancer (NSCLC), leading to uncontrolled cell growth and survival.
Zongertinib is an irreversible tyrosine kinase inhibitor of HER2. Its acrylamide moiety forms a covalent bond with the cysteine 805 residue of the HER2 receptor, thereby inhibiting HER2 phosphorylation and the activation of downstream signaling pathways, including extracellular signal-regulated kinase (ERK), mitogen-activated protein kinases (MAPK), and PI3K/Akt. The inhibition of these pathways leads to a reduction in the proliferation of lung cancer cells harboring HER2 tyrosine kinase domain activating mutations.
- Primary indication
- Zongertinib is indicated for the treatment of adult patients with unresectable or metastatic non-squamous non-small cell lung cancer (NSCLC) whose tumors have HER2 (ERBB2) tyrosine kinase domain activating mutations.Curator reviewed · 2 structured indications
- Formula / weight
- C29H29N9O2 · 535.612 g/mol (avg)
- First approval
- United States, 2025
- Code names
- BI-1810631
- Brand names
Resolves to
YSGNGFPNTLERCR-UHFFFAOYSA-NSMILESCN1C=NC2=CC(OC3=CC=C(NC4=NC=NC5=CN=C(N=C45)N4CCC(CC4)NC(=O)C=C)C=C3C)=CC=C12What you can answer from here — as of September 23, 2026
Which drugs share a target with Zongertinib, and which of those have an active Phase 3 trial?
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