Targeted Therapy / Oncology

Gilotrif (afatinib dimaleate)

Boehringer Ingelheim · Second-Generation EGFR / ErbB Family Inhibitor

FDA Approved 2013 Oral tablet Specialty Medication
Afatinib Dimaleate Gilotrif 40mg tablets, Boehringer Ingelheim, EGFR-positive NSCLC targeted therapy

What is Gilotrif? Gilotrif (afatinib) is a second-generation, irreversible ErbB family inhibitor by Boehringer Ingelheim approved for first-line treatment of metastatic NSCLC with common EGFR mutations (exon 19 deletions or exon 21 L858R substitutions) and squamous NSCLC after platinum chemotherapy.

About Gilotrif

Brand NameGilotrif
Generic / INNafatinib dimaleate
Drug ClassSecond-Generation EGFR / ErbB Family Inhibitor
ManufacturerBoehringer Ingelheim
AdministrationOral tablet
FDA Approval2013
📦 Available in 20 mg, 30 mg, and 40 mg tablets.

FDA-Approved Uses for Gilotrif

Indications are based on FDA approval. Your healthcare provider determines appropriate use based on your specific diagnosis, stage, biomarker status, and overall clinical picture.

  • Metastatic NSCLC — first-line treatment of patients with common EGFR mutations (exon 19 del or L858R)
  • Metastatic squamous cell NSCLC — after platinum-based chemotherapy
Biomarker Note: EGFR exon 19 deletion or L858R substitution must be confirmed by an FDA-approved companion diagnostic before starting afatinib for the first-line NSCLC indication.

How Does Gilotrif Work?

Afatinib irreversibly inhibits all ErbB family kinases — EGFR (ErbB1), HER2 (ErbB2), ErbB3, and ErbB4 — by covalently binding to their intracellular kinase domains. This pan-ErbB inhibition distinguishes afatinib from first-generation reversible EGFR inhibitors (gefitinib, erlotinib).

Dosage & Administration

40 mg orally once daily on an empty stomach (no food 3 hours before or 1 hour after). Dose escalation to 50 mg if 40 mg tolerated. Dose reduction to 30 mg for toxicity. Avoid strong P-gp inhibitors (taken with meals increases absorption significantly).

⚠️ Important

Dosing is individualized by the prescribing clinician. Never adjust your dose without consulting your healthcare provider. This information is educational only and does not replace the official prescribing information.

Warnings, Precautions & Side Effects

General Warning

Diarrhea — can be severe; proactive management required. Dermatologic reactions (rash, acneiform dermatitis, paronychia). ILD/pneumonitis — can be fatal. Hepatic toxicity — monitor LFTs. Keratitis. Embryo-fetal toxicity. Left ventricular dysfunction.

⛔ Serious Warnings & Precautions
  • Severe diarrhea (manage proactively)
  • ILD/pneumonitis
  • Severe dermatologic reactions
  • Keratitis
  • Hepatotoxicity
  • Embryo-fetal toxicity

Common Side Effects

  • Diarrhea (very common)
  • Acneiform rash
  • Paronychia
  • Dry skin
  • Mucositis/stomatitis
  • Nausea
  • Decreased appetite

This is not a complete list. Always report new or worsening symptoms to your healthcare provider promptly.

Storage & Handling

Store below 25°C (77°F). Protect from high humidity and light. Keep in original bottle with desiccant.

BiologicHealthPlus provides temperature-monitored cold-chain specialty delivery for medications requiring refrigeration. Never use a medication if its storage conditions have been compromised.

Insurance Coverage, Prior Authorization & Patient Assistance

🛡️ Commercial Insurance

Gilotrif is covered by most major commercial insurance plans when medically necessary and prior authorized. Coverage tier and cost-sharing vary by plan.

✅ Prior Authorization

Prior authorization is required by virtually all insurance plans for Gilotrif. BiologicHealthPlus handles the complete prior authorization process at no cost to patients or providers.

🏥 Medicare Coverage

Medicare Part D covers this oral specialty medication. Medicaid coverage varies by state.

🆓 Patient Assistance

Manufacturer patient assistance programs may be available for eligible uninsured or underinsured patients. Contact BiologicHealthPlus for a confidential eligibility review.

Prior Authorization Patient Assistance Insurance & Savings Medication Costs

Frequently Asked Questions — Gilotrif

Gilotrif (afatinib) is a second-generation, irreversible pan-ErbB inhibitor approved for EGFR exon 19 del/L858R NSCLC (first-line) and squamous NSCLC after platinum chemotherapy.

Afatinib irreversibly and covalently inhibits all ErbB family members (EGFR, HER2, ErbB3, ErbB4), while gefitinib and erlotinib are reversible EGFR-selective inhibitors. Afatinib shows particular benefit in certain EGFR mutations uncommon in the L858R/exon 19 population.

Diarrhea is the most common and often dose-limiting side effect. Proactive management with loperamide from the onset of loose stools is strongly recommended.

Related Medications

Tagrisso (osimertinib)  ·  Rybrevant (amivantamab)  ·  Brigatinib (Alunbrig — ALK)  ·  Erlotinib (Tarceva)

Related Conditions

EGFR-mutant NSCLC  ·  Squamous cell NSCLC  ·  Non-small cell lung cancer

Comparisons

Rybrevant Brigatinib

Authoritative References

Medical Disclaimer: This page is for general educational purposes only and does not constitute medical advice, diagnosis, or treatment. Always consult your oncologist, hematologist, or licensed healthcare professional before making any treatment decisions. Last reviewed: August 2026 by the BiologicHealthPlus Clinical Team.