Comparative Pharmacology
Head-to-head clinical analysis: HEXALEN versus TEMOZOLOMIDE.
Head-to-head clinical analysis: HEXALEN versus TEMOZOLOMIDE.
HEXALEN vs TEMOZOLOMIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Alkylating agent that crosslinks DNA, inhibiting DNA replication and transcription, and inducing apoptosis in rapidly dividing cells.
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.
260 mg/m2/day orally in 4 divided doses for 14 or 21 days of a 28-day cycle.
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.
None Documented
None Documented
Terminal elimination half-life is 12-13 hours; prolonged to 24 hours in renal impairment.
Clinical Note
moderateTemozolomide + Digoxin
"Temozolomide may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateTemozolomide + Digitoxin
"Temozolomide may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateTemozolomide + Deslanoside
"Temozolomide may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateTemozolomide + Acetyldigitoxin
"Temozolomide may decrease the cardiotoxic activities of Acetyldigitoxin."
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.
Primarily renal and hepatic metabolism; 60-70% excreted in urine as unchanged drug and metabolites; 15-20% eliminated in feces via biliary secretion.
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.
Category C
Category D/X
Alkylating Agent
Alkylating Agent