Comparative Pharmacology
Head-to-head clinical analysis: LENVATINIB versus QINLOCK.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LENVATINIB versus QINLOCK.
LENVATINIB vs QINLOCK
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.
Ripretinib is a switch-control tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and platelet-derived growth factor receptor alpha (PDGFRA) kinase signaling. It binds to both the switch pocket and the activation loop of KIT and PDGFRA, preventing kinase activation and inhibiting downstream signaling pathways involved in tumor cell proliferation and survival.
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.
150 mg orally once daily with food, until disease progression or unacceptable toxicity.
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 15 hours (range 11–20 hours) in patients with advanced GIST. This supports twice-daily dosing.
Fecal (approximately 64% of dose) and renal (approximately 25% of dose, with <2% as unchanged drug).
Primarily hepatic metabolism, with <1% excreted unchanged in urine. Fecal excretion accounts for approximately 80% of the administered dose, with renal excretion of unchanged drug being minimal (<1%).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor