Comparative Pharmacology
Head-to-head clinical analysis: BOSUTINIB MONOHYDRATE versus GILOTRIF.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BOSUTINIB MONOHYDRATE versus GILOTRIF.
BOSUTINIB MONOHYDRATE vs GILOTRIF
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Bosutinib is a dual Src/Abl tyrosine kinase inhibitor. It inhibits the BCR-ABL kinase, which is constitutively active in chronic myeloid leukemia (CML), and also inhibits Src family kinases. It has minimal inhibitory activity against c-KIT and PDGFR.
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.
400 mg orally once daily with 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
22.5 hours; supports once-daily dosing, with steady-state achieved by day 8.
Terminal elimination half-life is approximately 41 hours, supporting once-daily dosing. Steady-state is reached within 8 days.
Primarily fecal (91%, as unchanged drug and metabolites) with renal excretion accounting for <3%.
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