Comparative Pharmacology
Head-to-head clinical analysis: GILOTRIF versus INLYTA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GILOTRIF versus INLYTA.
GILOTRIF vs INLYTA
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.
Axitinib is a tyrosine kinase inhibitor that selectively inhibits vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3), which are involved in pathologic angiogenesis, tumor growth, and metastatic progression of cancer.
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.
5 mg orally twice daily, approximately 12 hours apart, with or without 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 13–17 hours in patients, supporting twice-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 hepatic metabolism via CYP3A4 and subsequent biliary-fecal elimination (approximately 61% of dose recovered in feces, 23% in urine as metabolites; <10% excreted unchanged in urine or feces).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor