Last reviewed 2026-04-20 · How we verify

Gilotrif (afatinib)

Gilotrif works by blocking the epidermal growth factor receptor, a protein that helps cancer cells grow.

Gilotrif (afatinib) is a small molecule kinase inhibitor developed by Boehringer Ingelheim that targets the epidermal growth factor receptor (EGFR). It is a first-line treatment for non-small cell lung cancer (NSCLC) with EGFR expression. Gilotrif was FDA-approved in 2013 and remains a patented product. Key safety considerations include diarrhea, rash, and interstitial lung disease. It has a half-life of 37 hours.

At a glance

Mechanism of action

Afatinib covalently binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) and irreversibly inhibits tyrosine kinase autophosphorylation, resulting in downregulation of ErbB signaling. Certain mutations in EGFR, including non-resistant mutations in its kinase domain, can result in increased autophosphorylation of the receptor, leading to receptor activation, sometimes in the absence of ligand binding, and can support cell proliferation in NSCLC. Non-resistant mutations are defined as those occurring in exons constituting the kinase domain of EGFR that lead to increased receptor activation and where efficacy is predicted by 1) clinically meaningful tumor shrinkage with the recommended dose of afatinib and/or 2) inhibition of cellular proliferation or EGFR tyrosine kinase phosphorylation at concentrations of afatinib sustainable at the recommended dosage according to validated methods. The most commonly found of these mutations are exon 21 L

Approved indications

• Non-small cell lung cancer, positive for epidermal growth factor receptor expression

Common side effects

• Diarrhea
• Stomatitis
• Rash/acneiform dermatitis
• Paronychia
• Dry skin
• Vomiting
• Dyspnea
• Fatigue
• Hypokalemia
• Pulmonary toxicity/ILD-like adverse reactions
• Sepsis
• Pneumonia

Drug interactions

• P-glycoprotein Substrates

Key clinical trials

• BIBW 2992 (Afatinib) Versus Chemotherapy as First Line Treatment in NSCLC With EGFR Mutation (PHASE3)
• LUX Lung 2 Phase II Single Arm BIBW 2992 "Afatinib" in NSCLC With EGFR Activating Mutations (PHASE2)
• BIBW 2992 (Afatinib) vs Gemcitabine-cisplatin in 1st Line Non-small Cell Lung Cancer (NSCLC) (PHASE3)
• LUX-Lung 8: A Phase III Trial of Afatinib (BIBW 2992) Versus Erlotinib for the Treatment of Squamous Cell Lung Cancer After at Least One Prior Platinum Based Chemotherapy (PHASE3)
• Testing Afatinib as Potentially Targeted Treatment in Cancers With EGFR Genetic Changes (MATCH - Subprotocol A) (PHASE2)
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) (PHASE2)
• Safety Study of Afatinib and Postoperative Radiation Therapy to Treat Head and Neck Cancer (PHASE1)
• Study to Evaluate Efficacy and Safety of Firmonertinib Compared With Investigator's Choice of EGFR Inhibitor as First-Line Treatment in Participants Who Have Locally Advanced or Metastatic NSCLC With EGFR P-Loop and Alpha C-Helix Compressing (PACC) Uncommon Mutations (PHASE3)

Patents

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Gilotrif CI brief — competitive landscape report
• Gilotrif updates RSS · CI watch RSS
• Boehringer Ingelheim portfolio CI