Comparative Pharmacology
Head-to-head clinical analysis: BOSUTINIB versus BOSUTINIB MONOHYDRATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BOSUTINIB versus BOSUTINIB MONOHYDRATE.
BOSUTINIB vs BOSUTINIB MONOHYDRATE
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.
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.
400 mg orally once daily with food.
400 mg orally once daily with 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."
22.5 hours; supports once-daily dosing, with steady-state achieved by day 8.
Primarily fecal (approx. 68% as unchanged drug and metabolites) and renal (approx. 25%, with <0.2% as unchanged drug in urine).
Primarily fecal (91%, as unchanged drug and metabolites) with renal excretion accounting for <3%.
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor