Comparative Pharmacology
Head-to-head clinical analysis: CLOFARABINE versus PURINETHOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CLOFARABINE versus PURINETHOL.
CLOFARABINE vs PURINETHOL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Clofarabine is a purine nucleoside antimetabolite that inhibits DNA synthesis by reducing intracellular deoxynucleotide triphosphate pools via inhibition of ribonucleotide reductase, and by terminating DNA chain elongation through incorporation into DNA, leading to apoptosis.
Mercaptopurine is a purine antimetabolite that inhibits purine nucleotide synthesis and metabolism. It is converted intracellularly to 6-thioguanine nucleotides (6-TGNs), which incorporate into DNA and RNA, inhibiting their synthesis and function. It also inhibits de novo purine synthesis via feedback inhibition.
52 mg/m^2 intravenously over 2 hours daily for 5 consecutive days, repeated every 28 days.
1.5-2.5 mg/kg orally once daily. Initial dose typically 50-75 mg/m²/day.
None Documented
None Documented
Clinical Note
moderateClofarabine + Digoxin
"Clofarabine may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateClofarabine + Digitoxin
"Clofarabine may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateClofarabine + Deslanoside
"Clofarabine may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateClofarabine + Acetyldigitoxin
"Clofarabine may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life: 5.2 hours (range 4-6 hours) in adult patients; clinically, this supports a 5-day continuous infusion schedule
The terminal elimination half-life of mercaptopurine is approximately 1.5 hours. However, the active metabolite 6-thioguanine nucleotides have a half-life of 5-7 days, correlating with pharmacological effects.
Renal: 49-60% as unchanged drug; biliary/fecal: minimal (<1%)
Primarily hepatic metabolism; renal excretion of metabolites accounts for approximately 50% of elimination. Biliary excretion contributes to a minor extent (<10%).
Category C
Category C
Antineoplastic Agent
Antineoplastic Agent