# Zongertinib

Source: https://onco.cc/drugs/zongertinib/  
OnCo record `zongertinib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

Zongertinib was the first oral HER2 inhibitor for lung cancer with HER2 mutations, approved in 2025 and moved to first line in 2026.

## Summary

Zongertinib is an irreversible HER2-selective tyrosine kinase inhibitor that spares EGFR, which limits the rash and diarrhoea seen with pan-HER inhibitors; it is taken as 120 mg once daily. Beamion LUNG-1 showed a response rate of about 71% in previously treated HER2-mutant NSCLC, leading to accelerated approval in August 2025, and in Q1 2026 it was approved as first-line therapy for HER2-mutant non-squamous NSCLC, the first oral HER2 inhibitor for this setting. Boehringer Ingelheim developed it. Diarrhoea, rash, raised liver enzymes, nausea and fatigue are the main adverse events. It competes with trastuzumab deruxtecan and with sevabertinib (Bayer, approved late 2025), and the best sequence between a pill and an antibody-drug conjugate is unresolved. For a newcomer: the first pill for lung cancers driven by HER2 mutations.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-04
- Brand: Hernexeos
- Modality: Small-molecule kinase inhibitor (HER2)
- Mechanism: Irreversible HER2-selective TKI sparing EGFR.
- Approvals: US 2025: HER2-mutant NSCLC, previously treated (accelerated); US 2026: First-line HER2-mutant non-squamous NSCLC
- Dosing: Oral; 120 mg once daily

## Sources

- FDA label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Zongertinib

## Connected records

- biomarkers: [HER2 (ERBB2) activating mutation](https://onco.cc/biomarkers/her2-mutation/)
- cancers: [HER2-mutant non-small-cell lung cancer](https://onco.cc/cancers/her2-mutant-nsclc/), [Lung cancer (all types)](https://onco.cc/cancers/lung-cancer/), [Non-small-cell lung cancer](https://onco.cc/cancers/nsclc/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [HER2](https://onco.cc/targets/her2/)
- companies: [Boehringer Ingelheim](https://onco.cc/companies/boehringer-ingelheim/)
- trials: [Beamion 44: A Study to Test How Well Zongertinib is Tolerated by People With Advanced Non-small Cell Lung Cancer With HER2 Mutations When Given in Combination With Chemotherapy With or Without Pembrolizumab](https://onco.cc/trials/nct07486817/), [Beamion BCGC-1: A Study to Find a Suitable Dose of Zongertinib Used Alone and in Combination With Other Treatments to Test Whether it Helps People Wit](https://onco.cc/trials/nct06324357/), [Beamion LUNG-1](https://onco.cc/trials/beamion-lung-1/), [Beamion LUNG-2: A Study to Test Whether Zongertinib (BI 1810631) Helps People With Advanced Non-small Cell Lung Cancer With HER2 Mutations Compared With Standard Treatment](https://onco.cc/trials/nct06151574/), [Beamion LUNG-3: Adjuvant Zongertinib vs Standard Treatment in People With Completely Resected Stage II-IIIB NSCLC Harboring Activating HER2 TKD Mutati](https://onco.cc/trials/nct07195695/), [Beamion PANTUMOR-1: A Study to Test Whether Zongertinib Helps People With Advanced Cancers With HER2 Alterations](https://onco.cc/trials/nct06581432/)
- drugs: [Sevabertinib](https://onco.cc/drugs/sevabertinib/)
- key papers: [Beamion LUNG-1: zongertinib in previously treated HER2-mutant non-small-cell lung cancer](https://onco.cc/key-papers/paper-beamion-lung-1-zongertinib-nejm-2025/)
- pathways: [Non-small cell lung cancer (KEGG map)](https://onco.cc/pathways/nsclc-signalling/), [Receptor tyrosine kinase activation](https://onco.cc/pathways/rtk-activation/)

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