Comparative Pharmacology
Head-to-head clinical analysis: CABOZANTINIB versus GLEEVEC.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CABOZANTINIB versus GLEEVEC.
CABOZANTINIB vs GLEEVEC
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Small molecule tyrosine kinase inhibitor that targets MET, VEGFR2, RET, AXL, KIT, TIE2, FLT3, and TRKB. Inhibits tumor growth, angiogenesis, and metastasis.
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.
60 mg orally once daily, taken without food (at least 1 hour before or 2 hours after eating).
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.
None Documented
None Documented
Clinical Note
moderateCabozantinib + Digoxin
"Cabozantinib may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateCabozantinib + Digitoxin
"Cabozantinib may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateCabozantinib + Deslanoside
"Cabozantinib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateCabozantinib + Acetyldigitoxin
"Cabozantinib may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life is approximately 99 hours (range 68–136 hours) in patients with advanced solid tumors, supporting once-daily dosing.
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.
Primarily fecal (approximately 54% of administered dose as unchanged drug and metabolites), with renal excretion accounting for approximately 27% (largely as metabolites). Mean total recovery in feces and urine is about 81%.
Primarily fecal (68% of dose) as metabolites; renal excretion accounts for approximately 13% of dose (predominantly as metabolites). Unchanged imatinib in urine is <10%.
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor