Initial US Approval

  • 20131

Indications

Metastatic mEGFR NSCLC (1L):

  • 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 (1.1) Limitations of Use: Safety and efficacy of GILOTRIF were not established in patients whose tumors have resistant EGFR mutations.1

Metastatic Squamous NSCLC (2L):

  • Treatment of patients with metastatic, squamous NSCLC progressing after platinum-based chemotherapy.1

Recommended Dose/Route

Afatinib 40 mg orally once daily at least 1 hour before or 2 hours after a meal until disease progression or no longer tolerated.1

Dose Reductions for Adverse Reactions

  • If afatinib is withheld and resumed when the adverse reaction fully resolves, returns to baseline or improves to Grade 1, reinstitute at a reduced dose, ie, 10 mg per day less than the dose at which the adverse reaction occurred.1

Pivotal Studies

LUX-Lung 3 (NCT00949650)2

  • Key Inclusion Criteria: Previously untreated patients with EGFR mutation-positive, metastatic [Stage IV and Stage IIIb with pleural and/or pericardial effusion as classified by the American Joint Commission on Cancer (AJCC, 6th edition)] NSCLC.1,2
  • Treatment: Afatinib 40 mg orally once daily or intravenous Pemetrexed (500 mg/m2) plus cisplatin (75 mg/m2) once every 21 days for up to 6 cycles.1,2

LUX-Lung 8 (NCT01523587)3

  • Key Inclusion Criteria: Patients With Advanced Squamous Cell Carcinoma of the Lung as Second-line Therapy Following First-line Platinum-based Chemotherapy1,3
  • Treatment: Patients in the afatinib arm received oral afatinib 40 mg once daily. The dose could be escalated to 50 mg once daily in the absence of treatment-related adverse events (AEs) of more than grade.1,3
Afatinib: Efficacy Data

Afatinib: Efficacy Data

Safety

LUX-Lung3

  • Common Adverse Reactions (≥20%): The most frequently reported any grade AEs were diarrhea (96%), rash/acneiform dermatitis (90%), stomatitis (71%), paronychia (58%), and pruritus (21%).1,2
  • Common Laboratory Abnormalities (≥20%): The most frequently reported any grade laboratory abnormalities were increased ALT (54%), alkaline phosphate (51%), decreased creatinine clearance (49%), increased AST (46%), decreased lymphocytes (38%), and decreased potassium (30%).1,2
  • Dosage Reduction Due to AEs: 57%1,2
  • Permanent Discontinuation Due to AEs: 14%1,2

LUX-Lung8

  • Common Adverse Reactions (≥20%): The most frequently reported any grade adverse events (AEs) were diarrhea (75%), rash/acneiform dermatitis (70%), stomatitis (30%), decreased appetite (25%), and nausea (21%).1,3
  • Common Laboratory Abnormalities (≥20%): The most frequently reported any grade laboratory abnormalities was increased alkaline phosphate (34%).1,3
  • Dosage Reduction Due to AEs: 27%1,3
  • Permanent Discontinuation Due to AEs: 20%1,3
Afatinib: Most Common Adverse Events of Grade 3 or 4

Afatinib: Most Common Adverse Events of Grade 3 or 4

References

  1. Gilotrif (Afatinib). Prescribing information. Boehringer Ingelheim. 2022. Accessed December 2, 2024. https://content.boehringer-ingelheim.com/DAM/07c11f94-358a-439d-b0c8-af1e011f04c4/gilotrif-us-pi.pdf
  2. Sequist LV, Yang JC, Yamamoto N, et al. Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations. J Clin Oncol. 2013;31(27):3327-34. doi: 10.1200/JCO.44.2806.
  3. Goss GD, Cobo M, Lu S, et al. Afatinib versus erlotinib as second-line treatment of patients with advanced squamous cell carcinoma of the lung: Final analysis of the randomised phase 3 LUX-Lung 8 trial. EClinicalMedicine. 2021;37:100940. doi: 10.1016/j.eclinm.2021.100940.
  4. Edwards RL, Andan C, Lalla RV, Lacouture ME, O'Brien D, Sequist LV. Afatinib therapy: practical management of adverse events with an oral agent for non-small cell lung cancer treatment. Clin J Oncol Nurs. 2018;22(5):542-548. doi: 10.1188/18.CJON.542-548.