zongertinib: HER2 TKI

Zongertinib (BI 1810631)* is a human epidermal growth factor receptor 2 (HER2) inhibitor that covalently binds to the tyrosine kinase domain of both wild type and mutated HER2 receptors, including those with an exon 20 insertion.^1,2

Clinical Trials: 

• Beamion LUNG-1 is a Phase I trial evaluating zongertinib in the treatment of advanced or metastatic solid tumors with HER2 mutations.^2,3

• Beamion LUNG-2 is a Phase III trial evaluating zongertinib as first-line treatment in patients with advanced non-small cell lung cancer harboring HER2 tyrosine kinase domain mutations.⁴

*This is an investigational compound and has not been approved. Its safety and efficacy have not been established.

Clinical development

Zongertinib is currently undergoing clinical investigation as a monotherapy in patients that had previously treated for advanced or metastatic solid tumors.^1-3 This study (Beamion LUNG-1) consists of two parts: the first (Phase Ia) is investigating the pharmacokinetics and safety of zongertinib in patients with solid tumors harboring HER2 aberrations, and the second (Phase Ib) is investigating safety and efficacy in patients with pre-treated NSCLC harboring HER2 mutations in the tyrosine kinase domain (TKD).^1,2 

A Phase III, open-label, randomized, active-controlled, multi-center trial (Beamion LUNG-2) is evaluating orally administered zongertinib compared with standard of care as first-line treatment in patients with unresectable, locally advanced or metastatic nonsquamous NSCLC harboring HER2 tyrosine kinase domain mutations.⁴