Drug lookup
Drug reference

Afatinib

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplasticATC null
CDSCO approved
EXCRETION
not curated
INTERACTIONS
7 major
SEVERE in our sources
PREGNANCY
X
FDA category + note
Top interactionssee all 8
  • Aminolevulinic AcidSevereDatabaseDDInter
  • LeflunomideSevereDatabaseDDInter
  • LomitapideSevereDatabaseDDInter
  • MipomersenSevereDatabaseDDInter

Mechanism

Afatinib is a protein kinase inhibitor that specifically inhibits the kinase domains of Epidermal Growth Factor Receptor (EGFR), Human Epidermal Growth Factor Receptor 2 (HER2), and HER4. This inhibition leads to the suppression of downstream ErbB signaling pathways.

Indications

Treatment of locally advanced or metastatic non-small cell lung cancer with activating epidermal growth factor receptor (EGFR) mutations, in patients who have not previously been treated with EGFR tyrosine kinase inhibitorlung NSCLC (EGFR deletion of exon 19 or L858R mutation)first-line treatment of patients with metastatic NSCLC with EGFR mutationsmetastatic squamous NSCLC that has progressed subsequent to platinum-based chemotherapy

Dosing

Adult
Oral: 40 mg once daily; increased if tolerated to up to 50 mg once daily, dose increase may be considered after 3 weeks at initial dose.
Renal adjustment
In patients with severe renal impairment, a dose reduction is recommended.
Max dose
50 mg once daily

Pharmacokinetics

Half-life
37 h (after repeat dosing)

Contraindications

  • Cardiac risk factors
  • Conditions which may affect left ventricular ejection fraction
  • Diarrhoea
  • Exposure to sun (protect skin from exposure to sun)
  • History of keratitis
  • New pulmonary symptoms (including dyspnoea, cough, fever)
  • Severe dry eyes
  • Signs and symptoms of keratitis
  • Signs and symptoms of skin reaction

Side effects

Common
DiarrheaSkin rashAnorexiaDry eyesacneiform dermatitisstomatitishand-foot skin reactionsnail changes
Serious
  • Interstitial lung disease
  • Hepatotoxicity
  • Keratitis
  • Stevens-Johnson syndrome
  • New pulmonary symptoms (dyspnoea, cough, fever)
  • liver function abnormalities
  • left ventricular dysfunction
  • gastrointestinal perforation (0.2% of patients)

Pregnancy & lactation

Pregnancy

X

Drug interactions

Aminolevulinic Acid
Severe
Database

Clinical effect not specified

Source: DDInter

Leflunomide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Lomitapide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Mipomersen
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Ozanimod
Severe
Database

Drug interaction classified as: others

Source: DDInter

Pexidartinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Teriflunomide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Pgp Modulating Drugs
Moderate
Textbook

Altered afatinib concentrations.

Source: G&G 14e · p1385

4 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.

Related guidelines

Other Tyrosine Kinase Inhibitor drugs

Ask House about Afatinib

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-10 · House clinical team