Comparative Pharmacology
Head-to-head clinical analysis: BOSUTINIB versus INLYTA.
Head-to-head clinical analysis: BOSUTINIB versus INLYTA.
BOSUTINIB vs INLYTA
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.
Axitinib is a tyrosine kinase inhibitor that selectively inhibits vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3), which are involved in pathologic angiogenesis, tumor growth, and metastatic progression of cancer.
400 mg orally once daily with food.
5 mg orally twice daily, approximately 12 hours apart, with or without food.
None Documented
None Documented
Terminal elimination half-life approximately 33 hours (range 22-60 hr) after oral administration, supporting once-daily dosing.
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 is approximately 13–17 hours in patients, supporting twice-daily dosing.
Primarily fecal (approx. 68% as unchanged drug and metabolites) and renal (approx. 25%, with <0.2% as unchanged drug in urine).
Primarily hepatic metabolism via CYP3A4 and subsequent biliary-fecal elimination (approximately 61% of dose recovered in feces, 23% in urine as metabolites; <10% excreted unchanged in urine or feces).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor