Initial US Approval:
2025
Key Clinical Studies:
Beamion LUNG-1 (NCT04886804)
Drug Class/Description:
Kinase inhibitor
Indications and Usage:
HERNEXEOS is a kinase inhibitor indicated for the treatment of adult patients 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.
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.
Dosage and Administration:
- Select patients for treatment with HERNEXEOS based on the presence of HER2 (ERBB2) tyrosine kinase domain activating mutations.
- The recommended dosage of HERNEXEOS is based on body weight:
- < 90 kg: 120 mg
- ≥ 90 kg: 180 mg
- Take HERNEXEOS orally once daily with or without food until disease progression or unacceptable toxicity.
Dosage Forms and Strengths:
Tablets: 60 mg
Contraindications:
None.
Warnings and Precautions:
- Hepatotoxicity: Monitor liver function tests including ALT, AST, and total bilirubin at baseline prior to administration, every 2 weeks during the first 12 weeks, and then monthly thereafter as clinically indicated, with more frequent testing in patients who develop transaminase elevations. Interrupt, reduce the dose, or permanently discontinue HERNEXEOS based on severity.
- Left Ventricular Dysfunction: Before initiating, evaluate LVEF and monitor at regular intervals during treatment and as clinically indicated. Interrupt, reduce the dose, or permanently discontinue HERNEXEOS based on severity.
- Interstitial Lung Disease/Pneumonitis: Monitor for new or worsening symptoms indicative of ILD/pneumonitis (e.g., dyspnea, cough, fever). Interrupt, reduce the dose, or permanently discontinue HERNEXEOS based on severity.
- Embryo-Fetal Toxicity: Can cause fetal harm. Advise patients of the potential risk to a fetus and to use effective contraception.
Adverse Reactions
Most common adverse reactions (≥ 20%) are diarrhea, hepatotoxicity, rash, fatigue, and nausea.
The most common (≥ 2%) Grade 3 or 4 laboratory abnormalities were decreased lymphocytes, increased alanine aminotransferase, increased aspartate aminotransferase, decreased potassium, and increased gamma glutamyl transferase.
Drug Interactions:
- Strong CYP3A Inducers: Avoid concomitant use with strong CYP3A inducers. If concomitant use cannot be avoided, increase HERNEXEOS dose.
- BCRP Substrates: Avoid concomitant use with certain BCRP substrates where minimal concentration increase may lead to serious adverse reactions and consider alternative therapies. If concomitant use cannot be avoided, monitor patients closely for adverse reactions and follow recommendations provided in the BCRP substrate approved product labeling. For other BCRP substrates, monitor for increased adverse reactions and adjust the dosages of those substrates as clinically appropriate.
Use in Specific Populations:
- Lactation: Advise not to breastfeed.
Adapted From:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/219042s000lbl.pdf
Every health-care provider should make their own determination regarding specific safe and appropriate patient care practices, including drug dosages and indications. The provider should always consult the most recent prescribing/product information. FDA Focus information is not guaranteed to be accurate, complete, or current. JADPRO and its editors, authors, reviewers, and commentators cannot be held responsible for any liability incurred as a consequence of the application of any of the information listed within.
