Zongertinib

Zongertinib
Clinical data
Trade namesHernexeos
Other namesBI-1810631, BI1810631
License data
Routes of
administration		By mouth
Drug classAntineoplastic, epidermal growth factor receptor 2 (HER2) inhibitor
ATC code
  • None
Legal status
Legal status
Identifiers
  • N-(1-{4-[3-methyl-4-(1-methylbenzimidazol-5-yl)oxyanilino]pyrimido[5,4-d]pyrimidin-6-yl}piperidin-4-yl)prop-2-enamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC29H29N9O2
Molar mass535.612 g·mol−1
3D model (JSmol)
  • C=CC(=O)NC1CCN(c2ncc3ncnc(Nc4ccc(Oc5ccc6c(c5)ncn6C)c(C)c4)c3n2)CC1
  • InChI=1S/C29H29N9O2/c1-4-26(39)34-19-9-11-38(12-10-19)29-30-15-23-27(36-29)28(32-16-31-23)35-20-5-8-25(18(2)13-20)40-21-6-7-24-22(14-21)33-17-37(24)3/h4-8,13-17,19H,1,9-12H2,2-3H3,(H,34,39)(H,31,32,35)
  • Key:YSGNGFPNTLERCR-UHFFFAOYSA-N

Zongertinib, sold under the brand name Hernexeos, is an anti-cancer medication used for the treatment of non-small cell lung cancer.[1][2] Zongertinib is a kinase inhibitor of human epidermal growth factor receptor 2 (HER2).[1][3][4] It is taken by mouth.[1]

Zongertinib was approved for medical use in the United States in August 2025.[5]

Medical uses

Zongertinib is indicated for the treatment of adults with unresectable or metastatic non-squamous non-small cell lung cancer whose tumors have HER2 (ERBB2) tyrosine kinase domain activating mutations, as detected by an FDA-approved test, and who have received prior systemic therapy.[1][5]

Adverse effects

The US Food and Drug Administration prescribing information includes warnings and precautions for hepatotoxicity, left ventricular dysfunction, interstitial lung disease/pneumonitis, and embryo-fetal toxicity.[1][5]

History

Efficacy was evaluated in participants with unresectable or metastatic, non-squamous non-small cell lung cancer with HER2 (ERBB2) TKD mutations who had received prior systemic therapy and received zongertinib in Beamion LUNG-1 (NCT04886804), an open-label, multi-center, multi-cohort trial.[5] The major efficacy outcome measures were objective response rate (ORR) and duration of response (DOR) determined by blinded independent central review per RECIST v1.1.[5]

The US Food and Drug Administration granted the application for zongertinib priority review, breakthrough therapy, and fast track designations.[5]

Society and culture

Zongertinib was approved for medical use in the United States in August 2025.[2][6]

Names

Zongertinib is the international nonproprietary name[7] and the United States Adopted Name.[8]

Zongertinib is sold under the brand name Hernexeos.[2][6]

References

  1. ^ a b c d e f "Hernexeos (zongertinib tablets), for oral use" (PDF). Product Insert. Boehringer Ingelheim Pharmaceuticals, Inc.
  2. ^ a b c "Novel Drug Approvals for 2025". U.S. Food and Drug Administration (FDA). 8 August 2025. Retrieved 10 August 2025. Public Domain This article incorporates text from this source, which is in the public domain.
  3. ^ Trillo Aliaga P, Spitaleri G, Attili I, Corvaja C, Battaiotto E, Angelopoulos PA, et al. (June 2025). "HER2 in Non-Small Cell Lung Cancer (NSCLC): Evolution of the Therapeutic Landscape and Emerging Drugs-A Long Way to the Top". Molecules. 30 (12). Basel, Switzerland: 2645. doi:10.3390/molecules30122645. PMC 12195848. PMID 40572608.
  4. ^ Ismail A, Desai A, Boumber Y (2025). "HER2 alterations in non-small cell lung cancer (NSCLC): from biology and testing to advances in treatment modalities". Frontiers in Oncology. 15 1624124. doi:10.3389/fonc.2025.1624124. PMC 12226463. PMID 40620714.
  5. ^ a b c d e f "FDA grants accelerated approval to zongertinib for non-squamous NSCLC with HER2 TKD activating mutations". U.S. Food and Drug Administration (FDA). 8 August 2025. Retrieved 10 August 2025. Public Domain This article incorporates text from this source, which is in the public domain.
  6. ^ a b "U.S. FDA grants accelerated approval to Boehringer's Hernexeos as first orally administered targeted therapy for previously treated patients with HER2-mutant advanced NSCLC" (Press release). Boehringer Ingelheim. 8 August 2025. Retrieved 10 August 2025 – via GlobeNewswire.
  7. ^ World Health Organization (2023). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 90". WHO Drug Information. 37 (3). hdl:10665/373341.
  8. ^ "Zongertinib". American Medical Association. Retrieved 10 August 2025.


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