Comparative Pharmacology
Head-to-head clinical analysis: ARSENIC TRIOXIDE versus LONSURF.
Head-to-head clinical analysis: ARSENIC TRIOXIDE versus LONSURF.
ARSENIC TRIOXIDE vs LONSURF
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Arsenic trioxide induces apoptosis in acute promyelocytic leukemia (APL) cells through degradation of PML-RARα fusion protein and modulation of mitochondrial pathways.
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.
0.15 mg/kg IV daily until remission, then 0.15 mg/kg IV 5 days per week for 5 weeks (consolidation); dose based on actual body weight.
Adults: 35 mg/m2 orally twice daily on days 1-5 and 8-12 of each 28-day cycle.
None Documented
None Documented
Clinical Note
moderateArsenic trioxide + Digoxin
"Arsenic trioxide may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateArsenic trioxide + Digitoxin
"Arsenic trioxide may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateArsenic trioxide + Deslanoside
"Arsenic trioxide may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateArsenic trioxide + Acetyldigitoxin
Terminal elimination half-life of inorganic arsenic is approximately 10–14 hours for the trivalent form, but for total arsenic (including methylated metabolites) the half-life ranges from 10 to 32 hours. Clinical context: due to extensive tissue distribution and metabolic conversion, the effective half-life for pharmacodynamic effect is prolonged, with repeated dosing leading to accumulation. The terminal half-life is biphasic: an initial distribution phase of about 2 hours and a terminal phase of 10–14 hours.
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.
Primarily renal excretion; after intravenous administration, approximately 15% of the dose is excreted unchanged in urine over 24 hours. Biliary/fecal excretion accounts for less than 5% as unchanged drug; the majority is eliminated as methylated metabolites (monomethylarsonic acid and dimethylarsinic acid) via urine, with total urinary excretion of arsenic species reaching 60-85% of the dose within 14 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.
Category C
Category C
Antineoplastic
Antineoplastic
"Arsenic trioxide may decrease the cardiotoxic activities of Acetyldigitoxin."