Comparative Pharmacology
Head-to-head clinical analysis: BOSUTINIB versus GLEEVEC.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BOSUTINIB versus GLEEVEC.
BOSUTINIB vs GLEEVEC
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.
Imatinib mesylate is a tyrosine kinase inhibitor that selectively inhibits BCR-ABL, c-KIT, PDGFR, and other kinases, blocking proliferation and inducing apoptosis in cells expressing these targets.
400 mg orally once daily with food.
400 mg orally once daily with a meal and a large glass of water. For advanced GIST, 400 mg daily; for CML in chronic phase, 400 mg daily; for accelerated phase or blast crisis, 600 mg daily. Dose may be increased to 600 mg or 800 mg daily in patients with disease progression.
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 18 hours (range 13–20 hours) in healthy subjects; for the active N-desmethyl metabolite, half-life is about 40 hours (range 30–50 hours). Clinical context: Steady-state is achieved within 1–2 weeks; once-daily dosing maintains therapeutic concentrations.
Primarily fecal (approx. 68% as unchanged drug and metabolites) and renal (approx. 25%, with <0.2% as unchanged drug in urine).
Primarily fecal (68% of dose) as metabolites; renal excretion accounts for approximately 13% of dose (predominantly as metabolites). Unchanged imatinib in urine is <10%.
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor