Comparative Pharmacology
Head-to-head clinical analysis: INLYTA versus STIVARGA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INLYTA versus STIVARGA.
INLYTA vs STIVARGA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Axitinib is a tyrosine kinase inhibitor that selectively inhibits vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3), which are involved in pathologic angiogenesis, tumor growth, and metastatic progression of cancer.
Multikinase inhibitor that inhibits VEGFR-1, -2, -3, PDGFR-α, PDGFR-β, FGFR-1, -2, TIE2, KIT, RET, RAF-1, and B-RAF.
5 mg orally twice daily, approximately 12 hours apart, with or without food.
160 mg orally once daily for 3 weeks, followed by 1 week off (28-day cycle).
None Documented
None Documented
Terminal elimination half-life is approximately 13–17 hours in patients, supporting twice-daily dosing.
Terminal elimination half-life is approximately 30 hours (range 15-42 h) for regorafenib and 25-60 h for its active metabolites M-2 and M-5. Steady-state is reached within 2-3 weeks.
Primarily hepatic metabolism via CYP3A4 and subsequent biliary-fecal elimination (approximately 61% of dose recovered in feces, 23% in urine as metabolites; <10% excreted unchanged in urine or feces).
Approximately 51% fecal (as unchanged drug and metabolites), 19% renal (as metabolites, <1% unchanged).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor