Comparative Pharmacology
Head-to-head clinical analysis: LONSURF versus LYSODREN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LONSURF versus LYSODREN.
LONSURF vs LYSODREN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
LONSURF (trifluridine and tipiracil) is a combination of the thymidine-based nucleoside analogue trifluridine and the thymidine phosphorylase inhibitor tipiracil. Trifluridine incorporates into DNA and inhibits cell proliferation, while tipiracil increases trifluridine exposure by inhibiting its degradation by thymidine phosphorylase.
Adrenocorticolytic agent; causes adrenal cortical necrosis and suppresses adrenal steroidogenesis, especially glucocorticoids and mineralocorticoids.
Adults: 35 mg/m2 orally twice daily on days 1-5 and 8-12 of each 28-day cycle.
Oral, initial dose 2-6 g/day divided in 3-4 doses, increase gradually to 8-10 g/day. Maximum dose 18 g/day.
None Documented
None Documented
Trifluridine: terminal half-life approximately 1.4-2.1 hours; tipiracil: terminal half-life approximately 2-3 hours. Clinical context: short half-lives necessitate twice-daily dosing on Days 1-5 and 8-12 of a 28-day cycle.
18-159 days; clinical context: during chronic therapy, steady-state may not be reached for 3-6 months.
Primarily renal: tipiracil is excreted unchanged in urine (approximately 50% of dose); trifluridine is eliminated via metabolism and renal excretion (as metabolites and unchanged drug). Fecal elimination accounts for <3% of total clearance.
Primarily renal excretion of metabolites; about 10% as unchanged drug. Biliary/fecal excretion accounts for <5%.
Category C
Category C
Antineoplastic
Antineoplastic