Comparative Pharmacology
Head-to-head clinical analysis: BOSUTINIB MONOHYDRATE versus ICLUSIG.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BOSUTINIB MONOHYDRATE versus ICLUSIG.
BOSUTINIB MONOHYDRATE vs ICLUSIG
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Ponatinib is a multi-targeted tyrosine kinase inhibitor that inhibits BCR-ABL, including T315I mutant form, and also inhibits VEGFR, PDGFR, FGFR, EPH receptors, and SRC family kinases.
400 mg orally once daily with food.
45 mg orally once daily with or without food.
None Documented
None Documented
22.5 hours; supports once-daily dosing, with steady-state achieved by day 8.
Terminal elimination half-life is approximately 7.5 hours in healthy subjects, supporting twice-daily dosing.
Primarily fecal (91%, as unchanged drug and metabolites) with renal excretion accounting for <3%.
Primarily fecal (91%) as unchanged drug and metabolites; renal elimination accounts for less than 4% of the dose.
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor