Afatinib
Afatinib is an irreversible tyrosine kinase inhibitor that targets and blocks EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) receptors by covalently binding to their kinase domains. It is primarily used to treat metastatic non-small cell lung cancer (NSCLC) with certain EGFR mutations, as it effectively downregulates ErbB signaling pathways that drive tumor growth.
Afatinib is an irreversible ErbB family blocker used to treat EGFR-mutation positive non-small cell lung cancer.
Key facts at a glance
- ATC
- L01EB03
- RxNorm
- 1430438
- Generic
- Afatinib
- Class
- atc-l01
- Brands
- Gilotrif
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 40mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- not established
- Maximum
- consult physician
- Frequency
- not applicable
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 40mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
8 groupspregnancy
first trimesteravoid use
Afatinib should not be used during pregnancy due to potential harm to the fetus. Women of childbearing potential should use effective contraception during treatment and for at least 2 weeks after discontinuation.
regular fetal monitoring via ultrasound
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second third trimesteravoid use
Continue to avoid use. If pregnancy occurs during treatment, discontinue therapy immediately and consult physician.
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
breastfeedingdiscontinue breastfeeding
Breastfeeding should be avoided during afatinib treatment and for at least 2 weeks after the last dose due to potential infant exposure
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
pediatric_age
children adolescentsnot indicated
Afatinib is not approved for use in pediatric patients. Safety and efficacy have not been established in patients under 18 years of age.
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
elderly over 65no specific dose adjustment required
No overall differences in safety or efficacy observed between elderly and younger patients. Monitor for increased susceptibility to adverse effects including diarrhea and skin reactions.
monitor renal function and for adverse reactions
Use with caution and monitor for adverse effects.
renal_impairment
severereduce starting dose to 20mg once daily
In patients with severe renal impairment (creatinine clearance <30 mL/min), a dose reduction is recommended. Monitor renal function during treatment.
regular monitoring of renal function (creatinine clearance)
Use with caution and monitor for adverse effects.
renal_impairment
moderateconsider dose reduction to 30mg
Monitor patients with moderate renal impairment (creatinine clearance 30-60 mL/min) closely. Consider dose reduction if adverse effects occur.
monitor renal function periodically
Use with caution and monitor for adverse effects.
hepatic_impairment
moderate severeno specific recommendation - use with caution
Afatinib is primarily metabolized in the liver. Use with caution in patients with moderate to severe hepatic impairment. No formal dosing recommendations exist.
monitor liver function tests periodically
Use with caution and monitor for adverse effects.
Statistics and clinical data
FDA approval year
Initial FDA approval for Afatinib
Drug class
ATC classification as L01EB02
Primary indication
First-line treatment for metastatic NSCLC with EGFR exon 19 deletions or L858R mutations
Mechanism of action
Covalently binds to EGFR, HER2, and HER4 receptors blocking signal transduction
Metastatic non-small cell lung cancer (NSCLC) with EGFR exon 19 deletions or L858R mutations; approved for first-line treatment in these patients
Covalently binds irreversibly to the kinase domains of EGFR, HER2, and HER4, inhibiting tyrosine kinase autophosphorylation and blocking downstream ErbB signaling pathways that promote cancer cell growth and survival
Can cause severe diarrhea requiring prompt management; may cause skin toxicity, interstitial lung disease (rare but serious), hepatotoxicity, and embryo-fetal toxicity; avoid pregnancy during treatment; drug interactions with P-gp inducers and inhibitors should be considered
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy