Comparative Pharmacology
Head-to-head clinical analysis: GILOTRIF versus ICLUSIG.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GILOTRIF versus ICLUSIG.
GILOTRIF vs ICLUSIG
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.
Ponatinib is a multi-targeted tyrosine kinase inhibitor that inhibits BCR-ABL, including T315I mutant form, and also inhibits VEGFR, PDGFR, FGFR, EPH receptors, and SRC family kinases.
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.
45 mg orally once daily 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 7.5 hours in healthy subjects, 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 fecal (91%) as unchanged drug and metabolites; renal elimination accounts for less than 4% of the dose.
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor