Comparative Pharmacology
Head-to-head clinical analysis: LAPATINIB DITOSYLATE versus LENVATINIB.
Head-to-head clinical analysis: LAPATINIB DITOSYLATE versus LENVATINIB.
LAPATINIB DITOSYLATE vs LENVATINIB
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Reversible tyrosine kinase inhibitor that inhibits ErbB-1 (EGFR) and ErbB-2 (HER2) by binding to the ATP-binding pocket, preventing receptor autophosphorylation and downstream signaling.
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.
Lapatinib ditosylate 1250 mg orally once daily on days 1-21 continuously, plus capecitabine 2000 mg/m2 orally once daily in 2 divided doses on days 1-14 of a 21-day cycle. Alternatively, 1500 mg orally once daily with letrozole 2.5 mg orally once daily continuously.
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.
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."
Terminal elimination half-life is 14–24 hours; after repeated dosing, effective half-life is ~24 hours clinically.
Approximately 28 hours (range 22-35 hours); supports once-daily dosing with steady-state achieved in ~5-7 days.
Fecal (approximately 87% as metabolites, with 3% as parent drug); renal (approximately 3% as metabolites).
Fecal (approximately 64% of dose) and renal (approximately 25% of dose, with <2% as unchanged drug).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor