Comparative Pharmacology
Head-to-head clinical analysis: GLEOSTINE versus TEMOZOLOMIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GLEOSTINE versus TEMOZOLOMIDE.
GLEOSTINE vs TEMOZOLOMIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
GLEOSTINE (lomustine) is a nitrosourea alkylating agent that crosslinks DNA and RNA, inhibiting DNA synthesis and repair. It is cell cycle phase-nonspecific.
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.
130 mg/m2 orally every 6 weeks as a single dose; alternatively, 75 mg/m2 orally every 3 weeks.
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
16-48 hours (terminal), with an active metabolite half-life of up to 5 days, requiring dose adjustment for 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.
Renal: 60% (as metabolites), Fecal: <5% (unchanged and metabolites), Biliary: minimal
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