Afatinib

(Gilotrif®)

Gilotrif®

Drug updated on 11/1/2024

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

Indication

  • 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.

Latest News

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Summary
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  • This summary is based on the review of 17 systematic review(s)/meta-analysis(es). [1-17]
  • Obinutuzumab combined with acalabrutinib (O-acala) demonstrated the best progression-free survival (PFS) ranking in chronic lymphocytic leukemia (CLL), particularly in patients with del17/P53mut mutations, with SUCRA scores of 93.5% for aCD20-ibrutinib and 91% for O-acala; acalabrutinib plus obinutuzumab improved PFS compared to ibrutinib-obinutuzumab and venetoclax-obinutuzumab, with relative risks (RRs) of 0.43 and 0.29, respectively.
  • In patients with follicular lymphoma, the combination of obinutuzumab, bendamustine, and maintenance obinutuzumab (G-Benda-G) resulted in the best PFS, achieving a hazard ratio (HR) of 0.41 compared to rituximab-bendamustine (R-Benda), with a SUCRA of 0.97 and a probability of being the best treatment (PbBT) of 72%.
  • Patients with high-risk genetic features in CLL, such as TP53 aberrations and IGHV unmutated status, showed similar PFS across different targeted agents. However, those with unmutated IGHV status had better PFS with acalabrutinib plus obinutuzumab compared to venetoclax plus obinutuzumab.
  • Afatinib was noted for its effectiveness in patients with uncommon EGFR (epidermal growth factor receptor) mutations, demonstrating a higher objective response rate (ORR) of 60.6% compared to osimertinib at 50.3%, although this difference was not statistically significant. Afatinib also showed significantly superior PFS (11.0 months vs. 7.0 months) in these patients.
  • Afatinib demonstrated a lower risk for hepatotoxicity compared to gefitinib and erlotinib, with gefitinib and erlotinib associated with a higher incidence of all-grade and high-grade ALT and AST elevations.
  • Afatinib had a greater overall toxicity profile compared to icotinib but was less toxic than dacomitinib. Gefitinib, erlotinib, and icotinib showed higher incidences of rash and diarrhea.
  • In the treatment of severe adverse events, afatinib was associated with rare occurrences of interstitial lung disease, dyspnea, and pneumonia. However, a reduced dose of 30 mg resulted in a lower incidence of severe diarrhea and rash while maintaining similar efficacy in patients without brain metastasis.
  • East Asian patients with advanced NSCLC demonstrated superior progression-free survival (PFS) and overall survival (OS) with afatinib compared to other EGFR-TKIs, particularly in patients with brain metastasis, where afatinib outperformed gefitinib.
  • Elderly patients (aged >65 years) receiving afatinib showed longer PFS compared to those treated with gefitinib and erlotinib, specifically among those with an ECOG performance status of 0-1.
  • Patients with uncommon EGFR mutations experienced superior PFS with afatinib versus osimertinib, particularly in those with non-ex20ins single uncommon mutations, highlighting the efficacy of afatinib in this subgroup.
  • Patients with T2DM benefited more from MET-EGFR-TKIs in terms of OS compared to non-diabetic patients, indicating a potentially enhanced treatment response in this population.

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 NSCLC-A Systematic Review2024Journal of Thoracic Oncology : Official Publication of The international
Do patient characteristics affect EGFR tyrosine kinase inhibitor treatment outcomes? A network meta-analysis of real-world survival outcomes of East Asian patients with advanced non-small cell lung cancer treated with first-line EGFR-TKIs2023Thoracic Cancer
Survival outcomes of east Asian patients with advanced non-small cell lung cancer treated with first-line EGFR tyrosine kinase inhibitors: A network meta-analysis of real-world evidence2023Thoracic Cancer
Front-line therapy for brain metastases and non-brain metastases in advanced epidermal growth factor receptor-mutated non-small cell lung cancer: a network meta-analysis2023Chinese Medical Journal
Clinical Outcomes of Afatinib Versus Osimertinib in Patients With Non-Small Cell Lung Cancer With Uncommon EGFR Mutations: A Pooled Analysis2023The Oncologist
The Anticancer Effect of Metformin Combined with Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-small Cell Lung Cancer Patients with or Without Type 2 Diabetes Mellitus: A Systematic Review and Meta-analysis2022Oncology and Therapy
Uncommon EGFR Compound Mutations in Non-Small Cell Lung Cancer (NSCLC): A Systematic Review of Available Evidence2022Current Oncology (Toronto, Ont.)
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-Analysis2022Cancers
Overall Survival Benefits of First-Line Treatments for Asian Patients With Advanced EGFR-Mutated NSCLC Harboring L858R Mutation: A Systematic Review and Network Meta-Analysis2022Jto Clinical and Research Reports
Resistance mechanisms of epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer patients: A meta-analysis2021Thoracic Cancer
Hepatotoxicity with epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer patients: A network meta-analysis2021Journal of Clinical Pharmacy and Therapeutics
Toxicity profile of epidermal growth factor receptor tyrosine kinase inhibitors for patients with lung cancer: A systematic review and network meta-analysis2021Critical Reviews in Oncology/Hematology
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer2021The 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-Analysis2021Cancers
Impact of Dose Reduction of Afatinib Used in Patients With Non-Small Cell Lung Cancer: A Systematic Review and Meta-Analysis2021Frontiers in Pharmacology
Comparative analysis of first-line treatment regimens for advanced EGFR-mutant non-small cell lung cancer patients with stable brain metastases2020Annals of Palliative Medicine
Cost-effectiveness analysis of the first-line EGFR-TKIs in patients with non-small cell lung cancer harbouring EGFR mutations2020The European Journal of Health Economics : Hepac : Health Economics in Prevention

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