Comparative Pharmacology
Head-to-head clinical analysis: IRESSA versus TARCEVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: IRESSA versus TARCEVA.
IRESSA vs TARCEVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Gefitinib is a selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. It binds reversibly to the ATP-binding site of EGFR, blocking downstream signaling pathways involved in cell proliferation and survival.
Erlotinib is a reversible tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR). It binds to the intracellular ATP-binding domain of EGFR, inhibiting autophosphorylation and downstream signaling pathways involved in cell proliferation, survival, and angiogenesis.
250 mg orally once daily.
150 mg orally once daily on an empty stomach (at least 1 hour before or 2 hours after food) for non-small cell lung cancer with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations.
None Documented
None Documented
Approximately 41 hours (range 30-60 hours) in steady state, supporting once-daily dosing
Terminal elimination half-life is about 36 hours in patients; steady-state is achieved within 7-10 days.
Fecal (86%), renal (<4% unchanged drug and <1% as metabolites)
Primarily fecal (approximately 83% of dose) via hepatobiliary elimination; renal excretion accounts for less than 8% after oral administration.
Category C
Category C
EGFR Tyrosine Kinase Inhibitor
EGFR Tyrosine Kinase Inhibitor