Comparative Pharmacology
Head-to-head clinical analysis: GLEEVEC versus INLYTA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GLEEVEC versus INLYTA.
GLEEVEC vs INLYTA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
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 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.
5 mg orally twice daily, approximately 12 hours apart, with or without food.
None Documented
None Documented
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.
Terminal elimination half-life is approximately 13–17 hours in patients, supporting twice-daily dosing.
Primarily fecal (68% of dose) as metabolites; renal excretion accounts for approximately 13% of dose (predominantly as metabolites). Unchanged imatinib in urine is <10%.
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