Overview

No overview information available.

Indication

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Associated Conditions

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Research Report

Published: Sep 29, 2025

Zongertinib (Hernexeos): A Comprehensive Monograph on a Novel HER2-Selective Tyrosine Kinase Inhibitor for Non-Small Cell Lung Cancer

I. Executive Summary & Regulatory Context

Overview of Zongertinib

Zongertinib, marketed under the brand name Hernexeos, is a first-in-class, orally administered, irreversible tyrosine kinase inhibitor (TKI) developed by Boehringer Ingelheim.[1] It represents a pivotal advancement in the field of precision oncology, specifically targeting a molecularly defined subset of non-small cell lung cancer (NSCLC).[3] As a highly selective antineoplastic agent, Zongertinib is designed to interfere with the growth of cancer cells by potently blocking the human epidermal growth factor receptor 2 (HER2), also known as ERBB2.[4]

Primary Indication

Zongertinib is indicated for the treatment of adult patients with unresectable (cannot be removed by surgery) or metastatic (has spread to other parts of the body) non-squamous NSCLC.[4] A critical requirement for its use is the presence of activating mutations within the tyrosine kinase domain (TKD) of the HER2 gene in the patient's tumor, which must be detected by a U.S. Food and Drug Administration (FDA)-approved test.[1] The current approval is for patients who have received prior systemic therapy, positioning Zongertinib as a crucial second-line or later treatment option.[7] This indication addresses a significant unmet medical need for a patient population that has historically faced a poor prognosis and had limited effective therapeutic options.[8]

Synopsis of Efficacy and Safety

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Clinical Trials

Title	Posted	Study ID	Phase	Status	Sponsor
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	2025/09/29	NCT07195695	Not Applicable	Not yet recruiting	Boehringer Ingelheim
Beamion PANTUMOR-1: A Study to Test Whether Zongertinib Helps People With Advanced Cancers With HER2 Alterations	2024/09/03	NCT06581432	Phase 2	Recruiting	Boehringer Ingelheim
A Study in Healthy Men to Test Whether Zongertinib Influences the Amount of 4 Other Medicines (Dabigatran, Rosuvastatin, Metformin, and Furosemide) in the Blood	2024/07/17	NCT06504862	Phase 1	Completed	Boehringer Ingelheim
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	2024/07/10	NCT06494761	Phase 1	Completed	Boehringer Ingelheim
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	2024/03/21	NCT06324357	Phase 1	Recruiting	Boehringer Ingelheim
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	2023/11/30	NCT06151574	Phase 3	Recruiting	Boehringer Ingelheim
A Study in Healthy Men to Test How Zongertinib is Taken up in the Body When Taken With or Without Food	2023/10/10	NCT06075277	Phase 1	Completed	Boehringer Ingelheim
A Study in Healthy Men to Test Whether Carbamazepine Influences the Amount of BI 1810631 in the Blood	2023/09/08	NCT06028464	Phase 1	Completed	Boehringer Ingelheim
A Study in Healthy Men to Test How Zongertinib (BI 1810631) is Taken up and Processed by the Body	2023/05/30	NCT05879991	Phase 1	Completed	Boehringer Ingelheim
A Study in Healthy Men to Test How Itraconazole Influences the Amount of Zongertinib (BI 1810631) in the Blood	2023/04/27	NCT05833139	Phase 1	Completed	Boehringer Ingelheim

FDA Drug Approvals

Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
HERNEXEOS	Boehringer Ingelheim Pharmaceuticals, Inc.	0597-9257	ORAL	60 mg in 1 1	8/8/2025

EMA Drug Approvals

Approved Product	Authorization Holder	Status	Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product	Manufacturer	Approval Number	Dosage Form	Strength	Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

Approved Product	Company	Approval Number	Drug Type	Dosage Form	Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product	Registration No.	Company	Licence No.	Strength	Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product	ARTG ID	Sponsor	Registration Type	Status	Registration Date
No TGA approvals found for this drug.

Health Canada Drug Approvals

Approved Product	Company	DIN	Dosage Form	Strength	Market Date
No Health Canada approvals found for this drug.

CIMA AEMPS Drug Approvals

Approved Product	Company	Registration Number	Pharmaceutical Form	Prescription Type	Status
No CIMA AEMPS (Spain) approvals found for this drug.

Philippines FDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product	Company	Registration Number	Dosage Form	Strength	Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name	MA Holder	MA Number	Pharmaceutical Form	Active Ingredient	Authorization Date
No UK EMC drug information found for this drug.

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