Comparative Pharmacology
Head-to-head clinical analysis: LONSURF versus VOYXACT.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LONSURF versus VOYXACT.
LONSURF vs VOYXACT
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.
GABAA receptor positive allosteric modulator; a neuroactive steroid that potentiates GABAergic inhibition.
Adults: 35 mg/m2 orally twice daily on days 1-5 and 8-12 of each 28-day cycle.
Adults: 200 mg orally once daily with food.
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.
Terminal elimination half-life approximately 37 hours (range 24-51 hours), supporting once-daily dosing with steady-state achieved in 5-8 days.
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 hepatic metabolism via CYP3A4, with 53% of the dose excreted in feces (mainly as metabolites) and 27% in urine (mostly as metabolites); less than 1% excreted unchanged in urine.
Category C
Category C
Antineoplastic
Antineoplastic