Comparative Pharmacology
Head-to-head clinical analysis: CAPRELSA versus GEFITINIB.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CAPRELSA versus GEFITINIB.
CAPRELSA vs GEFITINIB
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Inhibits multiple receptor tyrosine kinases involved in tumor angiogenesis and oncogenesis, including VEGFR2, EGFR, and RET.
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor; inhibits EGFR autophosphorylation and downstream signaling, leading to cell cycle arrest and apoptosis in EGFR-overexpressing tumors.
300 mg orally once daily, with or without food.
250 mg orally once daily
None Documented
None Documented
Terminal half-life approximately 90 hours (range 30–150 hours), supporting once-daily dosing; steady-state achieved by day 15.
Clinical Note
moderateGefitinib + Digoxin
"Gefitinib may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateGefitinib + Digitoxin
"Gefitinib may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateGefitinib + Deslanoside
"Gefitinib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateGefitinib + Acetyldigitoxin
"Gefitinib may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal half-life 48 hours (range 24-85 hr); supports once-daily dosing, steady state achieved by day 7-10
Primarily fecal (approximately 75% of administered dose, mainly as unchanged drug and metabolites); renal excretion accounts for about 25% (less than 1% unchanged).
Primarily fecal (86% unchanged + metabolites), renal excretion <5%
Category C
Category D/X
Kinase Inhibitor
Kinase Inhibitor