Afatinib
GILOTRIF
What it isOral irreversible EGFR tyrosine-kinase inhibitor; metastatic EGFR-mutant non-small-cell lung cancer.
Why this oneCovalent binding covers certain uncommon EGFR mutations that first-generation reversible inhibitors may miss.
What limits itDiarrhea and acneiform rash often force reduction or discontinuation; pneumonitis, hepatotoxicity, and GI perforation can occur.
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Metastatic NSCLC with non-resistant EGFR mutations (first-line; select by FDA-approved test) | Adults | 40 mg QD | 40 mg QD until progression or no longer tolerated | 40 mg QD |
| Metastatic squamous NSCLC progressing after platinum-based chemotherapy | Adults | 40 mg QD | 40 mg QD until progression or no longer tolerated | 40 mg QD |
Renal Mild-moderate (eGFR 30-89): no starting-dose adjustment. Severe (eGFR 15-29): 30 mg QD. Not studied at eGFR <15 or on dialysis
Hepatic Mild-moderate (Child-Pugh A/B): no adjustment. Severe (C): not studied — monitor closely, adjust if not tolerated
Dose reductions in 10 mg decrements; discontinue if severe/intolerable AE occurs at 20 mg/day
Instructions
- Take at least 1 h before or 2 h after a meal
- Missed dose: do not take within 12 h of next dose
- Hold for Grade >=3 reactions, persistent Grade 2 diarrhea (>=2 days on antidiarrheals), or prolonged/intolerable Grade 2 cutaneous reactions; resume at 10 mg/day lower once recovered to <=Grade 1/baseline
- Permanently discontinue for: life-threatening bullous/blistering/exfoliating skin lesions, confirmed ILD, severe drug-induced hepatic impairment, GI perforation, persistent ulcerative keratitis, symptomatic LV dysfunction, or severe/intolerable AE at 20 mg/day
- With P-gp inhibitor (if not tolerated): reduce daily dose by 10 mg; with chronic P-gp inducer: increase by 10 mg as tolerated
Cautions
- Diarrhea — can be severe with dehydration/renal impairment; treat promptly, hold for persistent Grade 2 or Grade >=3
- Bullous, blistering, and exfoliative skin disorders (incl. fatal); Grade 3 cutaneous reactions
- Interstitial lung disease — discontinue if confirmed
- Hepatic toxicity — obtain periodic LFTs; discontinue for severe hepatic impairment
- GI perforation (incl. fatal)
- Keratitis — discontinue if persistent ulcerative keratitis
- Embryo-fetal toxicity — effective contraception during and >=2 weeks after treatment
Adverse reactions
- Diarrhea
- Rash/acneiform dermatitis
- Stomatitis
- Paronychia
- Dry skin
- Decreased appetite
- Nausea
- Vomiting
- Pruritus
Pregnancy Can cause fetal harm (animal embryotoxicity/abortions at sub-clinical exposures); advise of fetal risk; effective contraception during and for >=2 weeks after last dose
Lactation Advise not to breastfeed during treatment and for 2 weeks after final dose (present in rat milk at 80-150x plasma)
NO BOXED WARNINGS
Principal riskNo FDA boxed warning.
Generic entry2026
Classes and tags
Clinical profile
Mechanism of action: Afatinib ballicule
