Comparative Pharmacology
Head-to-head clinical analysis: LENVATINIB versus TASIGNA.
Head-to-head clinical analysis: LENVATINIB versus TASIGNA.
LENVATINIB vs TASIGNA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lenvatinib is a kinase inhibitor that inhibits the receptor tyrosine kinases (RTKs) including VEGFR1 (FLT1), VEGFR2 (KDR), VEGFR3 (FLT4), FGFR1, FGFR2, FGFR3, FGFR4, PDGFRα, KIT, and RET. It also inhibits the kinase activities of other RTKs involved in tumor angiogenesis and tumor growth.
Nilotinib is a tyrosine kinase inhibitor that binds to and inhibits the activity of BCR-ABL, the constitutively activated fusion protein responsible for chronic myeloid leukemia (CML). It also inhibits other kinases including KIT, PDGFR, and DDR1.
24 mg orally once daily for differentiated thyroid carcinoma; 8 mg twice daily or 12 mg once daily in combination with everolimus for renal cell carcinoma; 12 mg once daily in combination with pembrolizumab for advanced endometrial carcinoma.
400 mg orally twice daily approximately every 12 hours. Administer on an empty stomach (no food for at least 2 hours before and 1 hour after dose). Swallow whole with water; do not crush or chew.
None Documented
None Documented
Clinical Note
moderateLenvatinib + Digoxin
"Lenvatinib may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateLenvatinib + Digitoxin
"Lenvatinib may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateLenvatinib + Deslanoside
"Lenvatinib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateLenvatinib + Acetyldigitoxin
"Lenvatinib may decrease the cardiotoxic activities of Acetyldigitoxin."
Approximately 28 hours (range 22-35 hours); supports once-daily dosing with steady-state achieved in ~5-7 days.
Terminal elimination half-life is approximately 90-120 hours, supporting once-daily dosing.
Fecal (approximately 64% of dose) and renal (approximately 25% of dose, with <2% as unchanged drug).
Primarily fecal (approximately 66-93% of the dose) as unchanged drug and metabolites; renal excretion is minimal (<5% of the dose).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor