Comparative Pharmacology
Head-to-head clinical analysis: CABOZANTINIB versus GILOTRIF.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CABOZANTINIB versus GILOTRIF.
CABOZANTINIB vs GILOTRIF
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.
GILOTRIF (afatinib) is an irreversible inhibitor of the ErbB family of tyrosine kinases, including EGFR (ErbB1), HER2 (ErbB2), ErbB3, and ErbB4. It binds covalently to the ATP-binding pocket of the kinase domain, blocking downstream signaling pathways involved in cell proliferation, survival, and angiogenesis.
60 mg orally once daily, taken without food (at least 1 hour before or 2 hours after eating).
40 mg orally once daily for first-line treatment of EGFR mutation-positive non-small cell lung cancer; may be increased to 50 mg if tolerated.
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 41 hours, supporting once-daily dosing. Steady-state is reached within 8 days.
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%.
Approximately 88% of the administered dose is eliminated via feces (with 85% as unchanged parent drug), and 8% via urine (with <5% as unchanged drug). Biliary excretion is the primary route for unchanged drug.
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor