Hernexeos

Adults with unresectable or metastatic nonsquamous NSCLC with HER2 TKD activating mutations who have received prior systemic therapy.

120 mg orally once daily for patients <90 kg; 180 mg for patients >=90 kg.

Tablets: 60 mg, 120 mg

None listed in the prescribing information.

• Hepatotoxicity: Monitor LFTs.
• Left Ventricular Dysfunction: Assess LVEF before and during treatment.
• ILD/Pneumonitis: Monitor and permanently discontinue if confirmed.
• Embryo-Fetal Toxicity: Can cause fetal harm.

Diarrhea (52%), Nausea (34%), Increased ALT (28%), Rash (26%), Fatigue (24%), Increased AST (22%), Decreased Appetite (20%), Vomiting (16%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Strong CYP3A4 Inhibitors: Avoid.
Strong CYP3A4 Inducers: Avoid.
BCRP Substrates: Monitor.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Zongertinib is a highly selective, irreversible HER2 TKI that covalently binds C805 in the HER2 kinase domain, with high selectivity for HER2 over EGFR, reducing EGFR-mediated toxicities.

Tmax: 2-4 hours. Protein binding: >99%. Half-life: ~30 hours. Steady state ~7 days.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• Beamion LUNG-1 — Zongertinib in HER2-mutant NSCLC. Phase Ib, n=71.
  🔬 NCT04886804 ↗

Hernexeos has FDA-approved indications across the following cancer types covered on CancerDrugEvidence: