Last reviewed 2026-04-20 · How we verify

Hernexeos (ZONGERTINIB)

Hernexeos works by blocking the HER2 tyrosine kinase domain, which is a protein that helps cancer cells grow and divide.

Hernexeos (zongertinib) is a small molecule kinase inhibitor developed by Boehringer Ingelheim, targeting unresectable or metastatic non-squamous non-small cell lung cancer (NSCLC) with HER2 (ERBB2) tyrosine kinase domain activating mutations. It was FDA-approved in 2025 and is currently patented. Key safety considerations include its half-life of 12 hours and bioavailability of 76%. Hernexeos is a treatment option for patients with specific NSCLC mutations. Its commercial status is patented, with no generic manufacturers available.

At a glance

Mechanism of action

Zongertinib is a kinase inhibitor of human epidermal growth factor receptor 2 (HER2). In vitro, zongertinib inhibited phosphorylation of HER2, downstream signaling of HER2 (phosphorylation of ERK), and proliferation of lung cancer cells harboring HER2 tyrosine kinase domain activating mutations. In vivo, zongertinib demonstrated anti-tumor activity in mouse xenograft models of NSCLC harboring HER2 tyrosine kinase domain activating mutations.

Approved indications

• Non-squamous NSCLC with HER2 mutations

Common side effects

• Diarrhea
• Rash
• Hepatotoxicity
• Fatigue
• Nausea
• Musculoskeletal pain
• Upper respiratory tract infection
• Decreased lymphocytes
• Increased alanine aminotransferase
• Increased aspartate aminotransferase
• Increased gamma glutamyl transferase
• Decreased potassium

Drug interactions

• Strong CYP3A Inducers
• Strong CYP3A Inducers
• BCRP Substrates
• BCRP Substrates
• Zongertinib
• Zongertinib
• BCRP Substrates
• BCRP Substrates
• Zongertinib
• Other BCRP Substrates
• Other BCRP Substrates
• Other BCRP Substrates

Key clinical 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 (PHASE2)
• 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 (PHASE3)
• 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 With Different Types of HER2+ Cancer That Has Spread (PHASE1,PHASE2)
• Beamion LUNG-3: A Study to Test Whether Zongertinib Helps People With Surgically Removed, Non-small Cell Lung Cancer With HER2 Mutations Compared With Standard Treatment (PHASE3)
• Beamion PANTUMOR-1: A Study to Test Whether Zongertinib Helps People With Advanced Cancers With HER2 Alterations (PHASE2)
• Beamion LUNG-1: A Study to Test Different Doses of Zongertinib in People With Different Types of Advanced Cancer (Solid Tumours With Changes in the HER2 Gene) (PHASE1)
• A Study in Healthy Men to Test Whether Zongertinib Influences the Amount of 4 Other Medicines (Dabigatran, Rosuvastatin, Metformin, and Furosemide) in the Blood (PHASE1)
• A Study in Healthy Men to Test Whether Zongertinib Affects How 3 Other Medicines (Midazolam, Omeprazole, and Repaglinide) Are Taken up and Processed by the Body (PHASE1)

Patents

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Hernexeos CI brief — competitive landscape report
• Hernexeos updates RSS · CI watch RSS
• Boehringer Ingelheim portfolio CI