On September 3, 2025 Boehringer Ingelheim reported HERNEXEOS (zongertinib tablets) has been granted Breakthrough Therapy Designation by the U.S. Food and Drug Administration (FDA) for first-line 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 (Press release, Boehringer Ingelheim, SEP 3, 2025, View Source [SID1234655737]).

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"Exploring accelerated review pathways is part of Boehringer’s strategy to have an unprecedented and generational impact on people facing cancer. We are incredibly pleased that HERNEXEOS has received Breakthrough Therapy Designation for first-line use in patients living with HER2-mutant non-small cell lung cancer," said Vicky Brown, Senior Vice President and Head of Immunology, Oncology, and Eye Health, Boehringer Ingelheim. "This pathway was designed to expedite the development and review of promising medicines for serious diseases, and clearly highlights the potential of HERNEXEOS."

Breakthrough Therapy Designation is given to expedite the development and review of medicines for serious conditions where preliminary clinical evidence indicates that the medicine may demonstrate substantial improvement over currently available therapies.

HERNEXEOS was recently approved by the U.S. FDA for adult patients with unresectable or metastatic non-squamous NSCLC whose tumors have HER2 (ERBB2) tyrosine kinase domain (TKD) activating mutations, as detected by an FDA-approved test, and who have received prior systemic therapy. This indication is approved under accelerated approval based on objective response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.

Boehringer will present new and updated HERNEXEOS data at the upcoming World Conference on Lung Cancer (WCLC) in September and European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) in October.

About HERNEXEOS
HERNEXEOS is an irreversible tyrosine kinase inhibitor (TKI) that selectively inhibits HER2 while sparing wild-type EGFR, thereby limiting associated toxicities. Boehringer Ingelheim is investigating HERNEXEOS across a range of advanced solid tumors with HER2 alterations.

The therapy was conditionally approved for use as a monotherapy by China’s National Medical Products Administration (NMPA) for the treatment of adult patients with unresectable, locally advanced or metastatic NSCLC whose tumors have activating HER2 (ERBB2) mutations and who have received at least one line of prior systemic therapy. It also recently received Breakthrough Therapy Designation from the Center for Drug Evaluation (CDE) of China’s NMPA for the first line treatment of adult patients with unresectable or metastatic NSCLC harboring activating mutations in the HER2 TKD. This orally administered, targeted therapy has also been granted Orphan Drug Designation in Japan.

About non-small cell lung cancer (NSCLC)
Lung cancer claims more lives than any other cancer type and the incidence is set to increase to over 3 million cases worldwide by 2040.1,2 NSCLC is the most common type of lung cancer.3 Due to a lack of symptoms and misdiagnoses,4 most patients with NSCLC present at stage III or IV, where the disease has metastasized locally or to other organs.5 The estimated 5-year survival rate historically has been less than 10% for metastatic disease.6,7,8 People living with advanced NSCLC can experience a detrimental physical, psychological, and emotional impact on their daily lives.9,10,11

About the Beamion clinical trial program
Beamion LUNG-1 (NCT04886804): An open-label, Phase I dose escalation trial, with dose confirmation and expansion, of zongertinib as monotherapy in people with unresectable or metastatic solid tumors with HER2 alterations. The study has 2 parts. The first part is open to adults with different types of advanced cancer with HER2 alterations that include mutations, amplifications, over-expression and fusions for whom previous treatment was not successful. The second part is open to people with HER2-mutant non-small cell lung cancer.

Beamion LUNG-2 is a Phase III, open label, randomized, active-controlled study that will enroll 416 patients with unresectable, or metastatic non-squamous NSCLC harboring HER2 tyrosine kinase domain mutations to evaluate zongertinib compared with standard of care.