Comparative Pharmacology
Head-to-head clinical analysis: GILOTRIF versus PONATINIB HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GILOTRIF versus PONATINIB HYDROCHLORIDE.
GILOTRIF vs PONATINIB HYDROCHLORIDE
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 potent oral tyrosine kinase inhibitor that inhibits BCR-ABL, including T315I mutant, as well as VEGFR, PDGFR, FGFR, and SRC 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 half-life of approximately 29 hours (range 18–48 h) supporting once-daily dosing; steady-state reached within 7 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.
Primarily hepatobiliary excretion; ~87% of dose recovered in feces (mostly as metabolites), <5% in urine as unchanged drug.
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor