Comparative Pharmacology
Head-to-head clinical analysis: TEMOZOLOMIDE versus TREANDA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: TEMOZOLOMIDE versus TREANDA.
TEMOZOLOMIDE vs TREANDA
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.
Bendamustine is a bifunctional mechlorethamine derivative that forms electrophilic alkyl groups which covalently bond to DNA bases, resulting in interstrand DNA crosslinks, DNA single- and double-strand breaks, and ultimately apoptosis. It also inhibits several mitotic checkpoints and induces both apoptosis and necrosis in cancer cells.
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.
120 mg/m2 IV over 60 minutes on Days 1 and 2 of a 21-day cycle.
None Documented
None Documented
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.
Terminal elimination half-life: ~36-40 minutes (active metabolite M3: ~3 hours). Short half-life supports multi-day dosing regimens; clinical effect duration is longer due to DNA alkylation.
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.
Renal: ~50% as unchanged drug and metabolites; additional biliary/fecal elimination (non-renal clearance accounts for ~50% in humans, but specific biliary/fecal percentages not routinely quantified in clinical studies).
Category D/X
Category C
Alkylating Agent
Alkylating Agent