Comparative Pharmacology
Head-to-head clinical analysis: NILOTINIB versus PEMAZYRE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NILOTINIB versus PEMAZYRE.
NILOTINIB vs PEMAZYRE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Tyrosine kinase inhibitor targeting BCR-ABL, c-KIT, and PDGFR. Binds to inactive conformation of ABL kinase, preventing ATP binding and substrate phosphorylation.
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.
300 mg orally twice daily for newly diagnosed chronic phase CML; 400 mg orally twice daily for resistant or intolerant CML. Take on an empty stomach (no food for 2 hours before and 1 hour after).
13.5 mg orally once daily continuously until disease progression or unacceptable toxicity.
None Documented
None Documented
Clinical Note
moderateNilotinib + Digoxin
"Nilotinib may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateNilotinib + Digitoxin
"Nilotinib may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateNilotinib + Deslanoside
"Nilotinib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateNilotinib + Acetyldigitoxin
"Nilotinib may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life approximately 17 hours (range 14-20 hours), supporting twice-daily dosing.
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 (93% of absorbed dose) via biliary excretion; renal excretion accounts for <1% of unchanged drug.
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