Comparative Pharmacology
Head-to-head clinical analysis: BOSUTINIB versus NEXAVAR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BOSUTINIB versus NEXAVAR.
BOSUTINIB vs NEXAVAR
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.
Multikinase inhibitor targeting Raf, VEGFR-2, VEGFR-3, PDGFR-β, c-KIT, Flt-3, and RET kinases, inhibiting tumor growth and angiogenesis.
400 mg orally once daily with food.
400 mg (two 200 mg tablets) orally twice daily approximately 12 hours apart on an empty stomach (at least 1 hour before or 2 hours after a meal).
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 half-life 25-48 hours; supports twice-daily dosing with steady state achieved in 7-14 days.
Primarily fecal (approx. 68% as unchanged drug and metabolites) and renal (approx. 25%, with <0.2% as unchanged drug in urine).
Fecal (77% as unchanged drug and metabolites), renal (19% as metabolites, <1% as unchanged drug).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor