Drug intelligence / Profile preview

zongertinib

Development stage
Approved
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Zongertinib is an investigational **oral, irreversible, covalent HER2-selective tyrosine kinase inhibitor** being developed by **Boehringer Ingelheim** primarily for **HER2-mutant non-small cell lung cancer**. It is designed to bind selectively to the **HER2 tyrosine kinase domain** while largely sparing wild-type **EGFR**, with the goal of reducing EGFR-related toxicities such as rash and diarrhea seen with less selective pan-ErbB inhibitors. Clinical data from the ongoing Beamion LUNG-1 program have shown meaningful antitumor activity in previously treated HER2-mutant NSCLC, including activity in patients with brain metastases and in some patients previously treated with HER2-directed antibody-drug conjugates, with a generally manageable safety profile. The drug is also being explored in other HER2-driven solid tumors, including breast cancer.

Other names
zongertinib
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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