Afatinib
GILOTRIF
Pronunciation: a-FA-ti-nib (JEE-loe-trif)
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.
Afatinib prescription history
Animated chart of estimated U.S. prescriptions per year, Tyrosine kinase inhibitors (2001–2026). Afatinib enters in 2013 (estimated).
Principal riskNo FDA boxed warning.
Classes and tags
Clinical profile
FDA label
Read the full label on DailyMed ↗
NO BOXED WARNINGS
| 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
Available strengths
- tab 20, 30, 40 mg
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)
Cost
| Strength | #/mo | generic $/mo | CostPlus | |
|---|---|---|---|---|
| 20 mg | tab | 30 qd | not offered | |
| 30 mg | tab | 30 qd | not offered | |
| 40 mg | tab | 30 qd | not offered |
Generic entry2026
Open Afatinib in the interactive console ↗
Self-check
- Which EGFR mutations can afatinib cover beyond first-generation reversible inhibitors?
Certain uncommon mutations. - Which two common toxicities often force afatinib reduction or discontinuation?
Diarrhea and acneiform rash.