Brand Name
Hernexeos
Generic Name
Zongertinib
View Brand Information FDA approval date: August 08, 2025
Form: Tablet
What is Hernexeos (Zongertinib)?
HERNEXEOS is indicated for the treatment of adult patients with unresectable or metastatic non-squamous non-small cell lung cancer whose tumors have HER2 tyrosine kinase domain activating mutations, as detected by an FDA-approved test, and who have received prior systemic therapy [see Dosage and Administration.
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Brand Information
HERNEXEOS (zongertinib)
1INDICATIONS AND USAGE
HERNEXEOS is indicated for the 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, 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
2DOSAGE FORMS AND STRENGTHS
60 mg tablets: yellow, oval, biconvex, film-coated tablets, debossed with "L6" on one side and the Boehringer Ingelheim company symbol on the other side. Each tablet contains 60 mg of zongertinib.
3CONTRAINDICATIONS
None.
4ADVERSE REACTIONS
The following adverse reactions are discussed in greater detail in other sections of the labeling:
- Hepatotoxicity
- Left Ventricular Dysfunction
- Interstitial Lung Disease/Pneumonitis
4.1Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
The pooled safety population described in WARNINGS AND PRECAUTIONS reflects exposure to HERNEXEOS in 260 patients with unresectable or metastatic non-squamous NSCLC with HER2 (ERBB2) mutations who received HERNEXEOS as a single agent at 120 mg orally once daily until disease progression or unacceptable toxicity in Beamion LUNG-1
5OVERDOSAGE
Overdose in one patient who ingested 600 mg of HERNEXEOS resulting in nausea and vomiting.
6DESCRIPTION
HERNEXEOS tablets for oral administration contain zongertinib, a kinase inhibitor. The chemical name of zongertinib is 2-Propenamide,
Zongertinib is a yellow to dark yellow or orange solid. Zongertinib is slightly soluble at pH 1.2, and practically insoluble at pHs 3.6, 4.5, 5.4 and 6.8.
Each film-coated tablet of HERNEXEOS contains 60 mg of zongertinib and the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, hypromellose acetate succinate, mannitol, microcrystalline cellulose, and sodium stearyl fumarate. In addition, the film-coating contains the following inactive ingredients: ferric oxide (yellow), glycerol mono and dicaprylocaprate, polyvinyl alcohol, sodium lauryl sulfate, talc, and titanium dioxide.
7CLINICAL STUDIES
HERNEXEOS was evaluated in Beamion LUNG-1 (NCT04886804), a single arm, open-label, multi-center, multi-cohort trial. Eligible patients were required to have unresectable or metastatic NSCLC with HER2 (ERBB2) mutations. Patients with stable brain metastases were eligible to enroll. The study excluded patients who had a history of non-infectious interstitial lung disease/pneumonitis.
Patients received HERNEXEOS 120 mg orally once daily until disease progression or unacceptable toxicity. The major efficacy outcome measures were objective response rate (ORR) and duration of response (DOR) by Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 as assessed by blinded independent central review (BICR).
The efficacy population included 71 patients with unresectable or metastatic, non-squamous NSCLC with HER2 (ERBB2) tyrosine kinase domain (TKD) mutations based on prospective local testing. Of those, tumor tissue samples from 52% (37/71) of patients were retrospectively tested using Oncomine™ Dx Target Test (Life Technologies Corporation, Tissue-test). While 84% (31/37) of samples were positive for HER2 (ERBB2) TKD mutations, 2.7% (1/37) did not have HER2 (ERBB2) TKD mutations identified, and 13.5% (5/37) were unevaluable.
The baseline demographic and disease characteristics of the efficacy population were: 62 years (range: 30 to 80); 70% female, 55% Asian, 35% White, 0% Black or African American; 10% had unknown race data; 1.4% were of Hispanic or Latino ethnicity; 39% Eastern Cooperative Oncology Group (ECOG) performance status (PS) 0 and 61% ECOG PS 1; 65% never smoked; 100% metastatic disease; and 37% with brain metastases. The median number of prior therapies was 1 (range: 1 to 10); 100% of patients had prior platinum therapy and 78% had prior treatment with anti-PD-1/PD-L1 antibody. No patient had received previous treatment with a HER2-targeted tyrosine kinase inhibitor (TKI) or HER2-targeted antibody-drug conjugate (ADC).
Efficacy results are summarized in Table 5.
Among the 71 patients, 5 patients had measurable CNS metastases at baseline as assessed by BICR and had not received radiation therapy to the brain within 2 months prior to treatment with HERNEXEOS. Based on Response Assessment in Neuro-Oncology Brain Metastases (RANO-BM) criteria per BICR, responses were observed in 3 patients.
HERNEXEOS was also evaluated in 34 patients with unresectable or metastatic HER2 (ERBB2) TKD mutation-positive non-squamous NSCLC who had received previous treatment with platinum-based chemotherapy and a HER2-targeted ADC. Eligibility criteria were otherwise similar to the efficacy population described above. The median age was 58 years (range: 31 to 85); 65% female, 35% Asian, 50% White, 0% Black or African American; 15% had unknown race data; and 2.9% were of Hispanic or Latino ethnicity. Baseline ECOG performance status was 0 (21%) or 1 (79%); 65% never smoked. 100% patients had metastatic disease and 74% had brain metastases. The median number of prior therapies was 3 (range: 1 to 8); 100% of patients had prior platinum therapy and 77% had prior treatment with anti-PD-1/PD-L1 antibody; 2.9% of patients had received previous treatment with a HER2-targeted TKI. Confirmed ORR by RECIST v1.1 based on BICR was 44% (95% CI 29, 61), with 2.9% of patients having a complete response. Median DOR was 5.4 months (95% CI 2.8, not estimable), and 27% of responders had an observed DOR ≥ 6 months.
8HOW SUPPLIED/STORAGE AND HANDLING
60 mg tablets: yellow, oval, biconvex, film-coated, debossed with "L6" on one side and the Boehringer Ingelheim company symbol on the other side. They are packaged in a bottle containing two silica gel desiccants and with a child-resistant closure, available as follows:
9PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Patient Information).
10PRINCIPAL DISPLAY PANEL - 60 mg Tablet Bottle Carton
NDC 0597-9257-86
HERNEXEOS
60 mg
Pharmacist: Store and dispense in the
60 tablets
Rx only
Boehringer
