Comparative Pharmacology
Head-to-head clinical analysis: GEFITINIB versus PEMAZYRE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GEFITINIB versus PEMAZYRE.
GEFITINIB vs PEMAZYRE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Selective inhibitor of fibroblast growth factor receptor (FGFR) 1, 2, 3, and 4; binds to and inhibits FGFR kinase activity, leading to decreased tumor cell proliferation and angiogenesis.
250 mg orally once daily
13.5 mg orally once daily continuously until disease progression or unacceptable toxicity.
None Documented
None Documented
Terminal half-life 48 hours (range 24-85 hr); supports once-daily dosing, steady state achieved by day 7-10
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 elimination half-life is approximately 20 hours (range 14–32 h), supporting once-daily dosing with steady-state reached within 8 days.
Primarily fecal (86% unchanged + metabolites), renal excretion <5%
Primarily hepatobiliary excretion: 72% of the dose recovered in feces (mainly as unchanged drug and metabolites); renal excretion accounts for approximately 17% (less than 1% unchanged).
Category D/X
Category C
Kinase Inhibitor
Kinase Inhibitor