Comparative Pharmacology
Head-to-head clinical analysis: BUSULFAN versus HEXALEN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BUSULFAN versus HEXALEN.
BUSULFAN vs HEXALEN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Busulfan is a bifunctional alkylating agent that crosslinks DNA, primarily at guanine N7 positions, leading to DNA strand breaks and inhibition of DNA replication and transcription. It is cell cycle phase-nonspecific.
Alkylating agent that crosslinks DNA, inhibiting DNA replication and transcription, and inducing apoptosis in rapidly dividing cells.
1-4 mg/day orally for remission induction in CML; 0.8-1 mg/kg every 6 hours orally for 4 days as part of myeloablative conditioning with cyclophosphamide.
260 mg/m2/day orally in 4 divided doses for 14 or 21 days of a 28-day cycle.
None Documented
None Documented
Terminal elimination half-life is 2.5 to 4 hours (mean ~2.6 hours) after oral administration; prolonged to 3-5 hours with high-dose regimens. Half-life may increase with hepatic impairment.
Clinical Note
moderateBusulfan + Digoxin
"Busulfan may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateBusulfan + Digitoxin
"Busulfan may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateBusulfan + Deslanoside
"Busulfan may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateBusulfan + Acetyldigitoxin
"Busulfan may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life is 12-13 hours; prolonged to 24 hours in renal impairment.
Renal (10-50% unchanged), hepatic metabolism (primarily via glutathione S-transferases) with metabolites excreted in bile and urine. Fecal excretion minimal (<5%).
Primarily renal and hepatic metabolism; 60-70% excreted in urine as unchanged drug and metabolites; 15-20% eliminated in feces via biliary secretion.
Category C
Category C
Alkylating Agent
Alkylating Agent