Vizimpro

First-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) with EGFR exon 19 deletion or exon 21 L858R substitution mutations as detected by an FDA-approved test.

Recommended dose: 45 mg orally once daily, with or without food. Continue until disease progression or unacceptable toxicity.
Dose reduction: First reduction to 30 mg once daily; second to 15 mg once daily. Discontinue if unable to tolerate 15 mg once daily.

Tablets: 15 mg, 30 mg, 45 mg

None established in prescribing information.

• Interstitial Lung Disease (ILD)/Pneumonitis: Occurred in 2.1% of patients, including fatal cases. Withhold for suspected ILD; permanently discontinue if confirmed.
• Diarrhea: Grade ≥3 diarrhea in 8% of patients. Treat promptly with antidiarrheals; withhold for Grade ≥3.
• Dermatologic Toxicity: Rash (79%) and acneiform dermatitis common. Dermatologic supportive care recommended.
• Stomatitis: Grade ≥3 in 3% of patients. Treat with non-alcohol mouthwash.
• Paronychia: Common; manage with antiseptics and antibiotics as needed.
• Embryo-Fetal Toxicity: Can cause fetal harm. Advise effective contraception.

Diarrhea (87%), Rash (79%), Paronychia (64%), Stomatitis (44%), Dry Skin (33%), Decreased Appetite (31%), Alopecia (23%), Weight Loss (22%)

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

Proton pump inhibitors (PPIs): Reduce dacomitinib exposure; avoid concomitant use. Use antacids and H2-receptor antagonists with separation in dosing time (antacids: ≥6 hours before or 10 hours after; H2-blockers: ≥6 hours before or 10 hours after).
Strong CYP2D6 inhibitors: Increase dacomitinib exposure; reduce dacomitinib dose by 15 mg.

Can cause fetal harm. Advise females of reproductive potential to use effective contraception. Consult the full prescribing information for pregnancy risk details.

Advise women not to breastfeed during treatment and for a period after the last dose. Refer to prescribing information for duration guidance.

Safety and effectiveness in pediatric patients have not been established unless otherwise noted in the full prescribing information.

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

Dacomitinib is a potent, irreversible (covalent) pan-HER inhibitor that covalently binds to the kinase domains of EGFR (HER1), HER2, and HER4. By irreversibly blocking these receptors, it prevents downstream signaling through the MAPK and PI3K/AKT pathways that drive tumor proliferation. Its second-generation irreversible mechanism aims to overcome acquired resistance to reversible first-generation EGFR TKIs.

Tmax: ~6 hours. Protein binding: ~98%. Metabolized by CYP2D6 and CYP3A4 to active metabolite O-desmethyl-dacomitinib. Half-life: ~70 hours. Elimination: feces (~79%), urine (~3%). Steady state: ~14 days.

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

• ARCHER 1050 — Dacomitinib vs gefitinib as first-line treatment in EGFR-mutant advanced NSCLC. Phase III, n=452.
  🔬 NCT01774721 ↗📄 Primary Publication ↗

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