Comparative Pharmacology
Head-to-head clinical analysis: NINTEDANIB ESYLATE versus STIVARGA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NINTEDANIB ESYLATE versus STIVARGA.
NINTEDANIB ESYLATE vs STIVARGA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Nintedanib esylate is a tyrosine kinase inhibitor that binds competitively to the ATP-binding pocket of vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3), platelet-derived growth factor receptors (PDGFR-α, PDGFR-β), and fibroblast growth factor receptors (FGFR-1, FGFR-2, FGFR-3). This inhibition blocks downstream signaling pathways involved in angiogenesis and fibrosis.
Multikinase inhibitor that inhibits VEGFR-1, -2, -3, PDGFR-α, PDGFR-β, FGFR-1, -2, TIE2, KIT, RET, RAF-1, and B-RAF.
150 mg orally twice daily, 12 hours apart, taken with 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 10 hours in patients with IPF; steady state reached within 7 days.
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.
Biliary/fecal: >90% (unchanged and metabolites); Renal: <1%
Approximately 51% fecal (as unchanged drug and metabolites), 19% renal (as metabolites, <1% unchanged).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor