Comparative Pharmacology
Head-to-head clinical analysis: EXKIVITY versus GILOTRIF.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXKIVITY versus GILOTRIF.
EXKIVITY vs GILOTRIF
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Irreversible tyrosine kinase inhibitor that selectively targets epidermal growth factor receptor (EGFR) exon 19 deletion or exon 21 L858R substitution mutations, and specifically inhibits EGFR T790M and C797S resistance mutations, with less activity against wild-type EGFR.
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.
150 mg orally once daily with or without food.
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.
None Documented
None Documented
Terminal elimination half-life is approximately 48 hours, supporting once-daily dosing for systemic exposure.
Terminal elimination half-life is approximately 41 hours, supporting once-daily dosing. Steady-state is reached within 8 days.
Primarily hepatic metabolism with biliary excretion; 91% of total recovered in feces (30% as unchanged drug), <1% in urine.
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.
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor