Comparative Pharmacology
Head-to-head clinical analysis: TEMOZOLOMIDE versus URACIL MUSTARD.
Peer-Reviewed Evidence
Head-to-head clinical analysis: TEMOZOLOMIDE versus URACIL MUSTARD.
TEMOZOLOMIDE vs URACIL MUSTARD
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Temozolomide is an alkylating agent that causes DNA methylation at O6 and N7 positions of guanine, leading to DNA damage and apoptosis. It is converted to the active metabolite MTIC under physiological conditions.
Uracil mustard is a nitrogen mustard alkylating agent that crosslinks DNA, inhibiting DNA replication and transcription, leading to cell death.
150 mg/m2 orally once daily for 5 consecutive days of a 28-day cycle; for first cycle, then increase to 200 mg/m2/day if tolerated.
1 mg orally daily for 3 weeks, then 1 mg daily every 4 weeks, or 0.15 mg/kg orally once weekly.
None Documented
None Documented
1.8 hours (range 1.3–2.5 hours) for temozolomide; the active monomethyl triazeno imidazole carboxamide (MTIC) metabolite has a half-life of approximately 2.0 hours.
Clinical Note
moderateTemozolomide + Digoxin
"Temozolomide may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateUracil mustard + Digoxin
"Uracil mustard may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateTemozolomide + Digitoxin
"Temozolomide may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateUracil mustard + Digitoxin
"Uracil mustard may decrease the cardiotoxic activities of Digitoxin."
Terminal half-life approximately 6–8 hours in patients with normal renal function; may be prolonged with renal impairment
Approximately 38% of total radioactivity is excreted in urine over 7 days (5.6% as unchanged temozolomide, 12% as AIC metabolite, 21% as other polar metabolites), and less than 1% is excreted in feces.
Primarily renal (56-80% as unchanged drug and metabolites); minor fecal (10%)
Category D/X
Category C
Alkylating Agent
Alkylating Agent