Comparative Pharmacology
Head-to-head clinical analysis: NINTEDANIB versus NINTEDANIB ESYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NINTEDANIB versus NINTEDANIB ESYLATE.
NINTEDANIB vs NINTEDANIB ESYLATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Nintedanib is a small molecule tyrosine kinase inhibitor that inhibits multiple receptor tyrosine kinases, including 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). It also inhibits RET, FLT3, and Src family kinases. These receptors are involved in angiogenesis, proliferation, and fibrosis.
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.
150 mg orally twice daily approximately 12 hours apart, taken with food.
150 mg orally twice daily, 12 hours apart, taken with food.
None Documented
None Documented
Clinical Note
moderateNintedanib + Digoxin
"Nintedanib may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateNintedanib + Digitoxin
"Nintedanib may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateNintedanib + Deslanoside
"Nintedanib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateNintedanib + Acetyldigitoxin
"Nintedanib may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal half-life: 9.5 hours (range 6-14 hours) in patients with IPF; supports twice-daily dosing.
Terminal elimination half-life is approximately 10 hours in patients with IPF; steady state reached within 7 days.
Primarily fecal (85%) as unchanged drug; renal excretion accounts for <1%.
Biliary/fecal: >90% (unchanged and metabolites); Renal: <1%
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor