Afatinib

GILOTRIF

Open Afatinib in the interactive console ↗

Pronunciation: a-FA-ti-nib (JEE-loe-trif)

Afatinib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Afatinib ballicule

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 molecular structure (skeletal formula) — Molecular structure: Afatinib

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

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

Afatinib (GILOTRIF)

Strength		#/mo	CostPlus
20 mg	tab	30 qd	not offered
30 mg	tab	30 qd	not offered
40 mg	tab	30 qd	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Afatinib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2026

NO BOXED WARNINGS

Principal riskNo FDA boxed warning.

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Open Afatinib in the interactive console ↗