Comparative Pharmacology
Head-to-head clinical analysis: BOSUTINIB versus GILOTRIF.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BOSUTINIB versus GILOTRIF.
BOSUTINIB vs GILOTRIF
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Bosutinib is a tyrosine kinase inhibitor that inhibits the BCR-ABL kinase, including many imatinib-resistant mutations, and Src family kinases.
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
Clinical Note
moderateBosutinib + Digoxin
"The serum concentration of Digoxin can be increased when it is combined with Bosutinib."
Clinical Note
moderateBosutinib + Digitoxin
"Bosutinib may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateBosutinib + Deslanoside
"Bosutinib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateBosutinib + Acetyldigitoxin
"Bosutinib may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life approximately 33 hours (range 22-60 hr) after oral administration, supporting once-daily dosing.
Terminal elimination half-life is approximately 41 hours, supporting once-daily dosing. Steady-state is reached within 8 days.
Primarily fecal (approx. 68% as unchanged drug and metabolites) and renal (approx. 25%, with <0.2% as unchanged drug 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