Comparative Pharmacology
Head-to-head clinical analysis: GILOTRIF versus OFEV.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GILOTRIF versus OFEV.
GILOTRIF vs OFEV
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
GILOTRIF (afatinib) is an irreversible inhibitor of the ErbB family of tyrosine kinases, including EGFR (ErbB1), HER2 (ErbB2), ErbB3, and ErbB4. It binds covalently to the ATP-binding pocket of the kinase domain, blocking downstream signaling pathways involved in cell proliferation, survival, and angiogenesis.
Nintedanib is a tyrosine kinase inhibitor that blocks the activity of fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptor (PDGFR), and vascular endothelial growth factor receptor (VEGFR), thereby inhibiting fibroblast proliferation, migration, and transformation, and reducing extracellular matrix deposition.
40 mg orally once daily for first-line treatment of EGFR mutation-positive non-small cell lung cancer; may be increased to 50 mg if tolerated.
150 mg orally twice daily, taken with food.
None Documented
None Documented
Terminal elimination half-life is approximately 41 hours, supporting once-daily dosing. Steady-state is reached within 8 days.
Terminal elimination half-life is approximately 38 hours (range 30–48 hours) at steady state, supporting once-daily dosing.
Approximately 88% of the administered dose is eliminated via feces (with 85% as unchanged parent drug), and 8% via urine (with <5% as unchanged drug). Biliary excretion is the primary route for unchanged drug.
Primarily biliary/fecal (~93.4% of total radioactivity recovered in feces), renal excretion is minor (~0.6% unchanged in urine).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor