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Drug updated on 4/24/2024

Dosage FormTablet (oral; 20 mg, 30 mg, 40 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies


  • Indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have non-resistant epidermal growth factor receptor (EGFR) mutations as detected by an FDA-approved test.
  • Indicated for the treatment of patients with metastatic, squamous NSCLC progressing after platinum-based chemotherapy.

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  • Afatinib demonstrated superior response rates in patients with specific uncommon EGFR mutations such as G719X, S768I, E709X, and L747X compared to first or third-generation TKIs. It was particularly effective in compound mutations involving G719X, E709X, or S768I.
  • Fourteen systematic reviews/meta-analyses provided information on the effectiveness and safety of Afatinib in treating various forms of non-small cell lung cancer (NSCLC), including those with different EGFR mutations.
  • Compared to osimertinib, afatinib showed a superior progression-free survival benefit despite a slightly lower objective response rate in patients with NSCLC harboring uncommon EGFR mutations. The safety and efficacy were comparable between both drugs for patients with or without brain metastases.
  • No significant overall survival benefit was observed from using afatinib over conventional chemotherapies among Asian populations who have an L858R mutation or exon 19 deletion.
  • In terms of toxicity profile and dosing strategies, afatinib, along with dacomitinib, had greater toxicity compared to other EGFR-TKIs such as osimertinib, which has a more favorable safety profile. High-dose intermittent strategies reported manageable toxicity levels while increasing maximum plasma concentrations.
  • There is no significant difference between the effectiveness of a 30 mg dose versus a 40 mg dose in treating NSCLC patients using afatinib, but the former dosage level is associated with significantly less severe adverse events like diarrhea and rash.
  • Afatinib monotherapy improved survival rates among NSCLC patient groups, especially if administered as a first-line treatment option, whereas second-line monotherapy showed promise in squamous NSCLC progressing after platinum-based chemotherapy.
  • Afatinib had a significantly lower T790M mutation acquisition rate compared to first-generation TKIs (gefitinib, erlotinib), suggesting a potential advantage in delaying resistance mechanisms.

Product Monograph / Prescribing Information

Document TitleYearSource
Gilotrif (afatinib) Prescribing Information.2022Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT

Systematic Reviews / Meta-Analyses

Document TitleYearSource
Unveiling the Landscape of uncommon EGFR Mutations in non-small cell lung cancer - a systematic review.2024Journal of thoracic oncology
Clinical outcomes of afatinib versus osimertinib in patients with non-small cell lung cancer with uncommon EGFR mutations: A pooled analysis. 2023The Oncologist
Overall survival benefits of first-line treatments for Asian patients with advanced EGFR-Mutated NSCLC harboring L858R mutation: A systematic review and network meta-analysis.2022JTO Clinical and Research Reports
Overall survival benefits of first-line treatments for Asian patients with advanced epidermal growth factor receptor-mutated NSCLC harboring exon 19 deletion: A systematic review and network meta-analysis.2022Cancers
Comparison of T790M acquisition after treatment with first- and second-generation tyrosine-kinase inhibitors: A systematic review and network meta-analysis.2022Frontiers in Oncology
Non-small cell lung cancer with EGFR exon 20 insertion mutation: A systematic literature review and meta-analysis of patient outcomes.2022Current Medical Research and Opinion
First‐line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non‐squamous non‐small cell lung cancer.2021The Cochrane Database of Systematic Reviews
Efficacy of afatinib in the treatment of patients with non-small cell lung cancer and head and neck squamous cell carcinoma: A systematic review and meta-analysis.2021Cancers
Toxicity profile of epidermal growth factor receptor tyrosine kinase inhibitors for patients with lung cancer: A systematic review and network meta-analysis.2021Critical Reviews in Oncology/Hematology
High-dose administration of tyrosine kinase inhibitors to improve clinical benefit: A systematic review.2021Cancer Treatment Reviews
Impact of dose reduction of afatinib used in patients with non–small cell lung cancer: A systematic review and meta-analysis. 2021Frontiers in Pharmacology
Comparative analysis of first-line treatment regimens for advanced EGFR-mutant non-small cell lung cancer patients with stable brain metastases.2020Annals of Palliative Medicine
Efficacy and safety of first line treatments for patients with advanced epidermal growth factor receptor mutated, non-small cell lung cancer: Systematic review and network meta-analysis.2019BMJ
Systematic review and network meta-analysis of first-line therapy for advanced EGFR-positive non-small-cell lung cancer.2019Future Oncology

Clinical Practice Guidelines