Comparative Pharmacology
Head-to-head clinical analysis: GILOTRIF versus STIVARGA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GILOTRIF versus STIVARGA.
GILOTRIF vs STIVARGA
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 that inhibits VEGFR-1, -2, -3, PDGFR-α, PDGFR-β, FGFR-1, -2, TIE2, KIT, RET, RAF-1, and B-RAF.
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.
160 mg orally once daily for 3 weeks, followed by 1 week off (28-day cycle).
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 30 hours (range 15-42 h) for regorafenib and 25-60 h for its active metabolites M-2 and M-5. Steady-state is reached within 2-3 weeks.
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.
Approximately 51% fecal (as unchanged drug and metabolites), 19% renal (as metabolites, <1% unchanged).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor