Comparative Pharmacology
Head-to-head clinical analysis: CAPECITABINE versus XELODA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CAPECITABINE versus XELODA.
CAPECITABINE vs XELODA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Capecitabine is a prodrug that is enzymatically converted to 5-fluorouracil (5-FU) in the body, which inhibits thymidylate synthase and incorporates into RNA and DNA, leading to cytotoxic effects.
Prodrug of 5-fluorouracil (5-FU), inhibits thymidylate synthase, incorporates into RNA and DNA, leading to cell death.
Oral, 1250 mg/m2 twice daily for 2 weeks followed by a 1-week rest period.
Capecitabine 1250 mg/m2 orally twice daily for 2 weeks followed by a 1-week rest period, administered as 3-week cycles.
None Documented
None Documented
The terminal elimination half-life of capecitabine is approximately 0.75 hours. For its active metabolite 5-fluorouracil, the half-life is about 0.7 hours. Clinically, this short half-life necessitates twice-daily dosing to maintain therapeutic levels.
Clinical Note
moderateCapecitabine + Digoxin
"Capecitabine may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateCapecitabine + Digitoxin
"Capecitabine may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateCapecitabine + Deslanoside
"Capecitabine may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateCapecitabine + Acetyldigitoxin
"Capecitabine may decrease the cardiotoxic activities of Acetyldigitoxin."
Capecitabine: 0.65-0.85 h; 5'-DFCR: 0.9-1.1 h; 5'-DFUR: 0.75-1.0 h; 5-FU: 0.75-1.1 h. Terminal half-life of 5-FU is short, requiring continuous dosing for sustained exposure.
Capecitabine is predominantly eliminated renally. Approximately 95.5% of the administered dose is recovered in urine, with 61% as unchanged capecitabine and its metabolites. Fecal excretion accounts for about 2.6%. Biliary elimination is minimal (<1%).
Renal (95.5% as metabolites; 26.1% as parent drug and metabolites, primarily 5'-DFCR, 5'-DFUR, and FBAL); fecal (< 3%)
Category D/X
Category C
Antimetabolite
Antimetabolite