Comparative Pharmacology
Head-to-head clinical analysis: TEMOZOLOMIDE versus VALCHLOR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: TEMOZOLOMIDE versus VALCHLOR.
TEMOZOLOMIDE vs VALCHLOR
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.
Valchlor (mechlorethamine) is a nitrogen mustard alkylating agent that forms cross-links between DNA strands, leading to inhibition of DNA replication and transcription, and inducing apoptosis in rapidly dividing 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.
Topical: Apply 0.016% mechlorethamine gel to affected areas once daily.
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.
The terminal elimination half-life is approximately 24 hours after topical application, supporting daily dosing. Systemic half-life may be prolonged in patients with hepatic 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.
Following topical application, VALCHLOR (mechlorethamine) is systemically absorbed; approximately <10% is excreted unchanged in urine. The majority of the dose is eliminated via metabolism and biliary/fecal routes, with ~50% of a systemic dose recovered in feces as metabolites.
Category D/X
Category C
Alkylating Agent
Alkylating Agent