Comparative Pharmacology
Head-to-head clinical analysis: GILOTRIF versus NEXAVAR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GILOTRIF versus NEXAVAR.
GILOTRIF vs NEXAVAR
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.
Multikinase inhibitor targeting Raf, VEGFR-2, VEGFR-3, PDGFR-β, c-KIT, Flt-3, and RET kinases, inhibiting tumor growth and angiogenesis.
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.
400 mg (two 200 mg tablets) orally twice daily approximately 12 hours apart on an empty stomach (at least 1 hour before or 2 hours after a meal).
None Documented
None Documented
Terminal elimination half-life is approximately 41 hours, supporting once-daily dosing. Steady-state is reached within 8 days.
Terminal half-life 25-48 hours; supports twice-daily dosing with steady state achieved in 7-14 days.
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.
Fecal (77% as unchanged drug and metabolites), renal (19% as metabolites, <1% as unchanged drug).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor