Capecitabine is a novel oral fluoropyrimidine carbamate. Capecitabine is a prodrug, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. Capecitabine may inhibit cytochrome CYP2C9 enzyme, and therefore increase levels of substrates such as phenytoin and other substrates of CYP2C9. Capecitabine has shown varying degrees of efficacy with acceptable tolerability in numerous cancers including prostate, renal cell, ovarian, and pancreatic, with the largest amount of evidence in metastatic breast and colorectal cancer. After oral administration of 1250 mg/m2, capecitabine is rapidly and extensively absorbed from the gastrointestinal tract [with a time to reach peak concentration (tmax) of 2 hours and peak plasma compound concentration (Cmax) of 3 to 4 mg/L] and has a relatively short elimination half-life (t(1/2)) [0.55 to 0.89 h]. Capecitabine has been reported to increase serum phenytoin levels and the international normalized ratio in patients receiving concomitant phenytoin and warfarin, respectively.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 72 mg/mL
Ethanol 72 mg/mL
Capecitabine: a review.
Walko CM, et al. Clin Ther. 2005 Jan;27(1):23-44. PMID: 15763604.
Clinical pharmacokinetics of capecitabine.
Reigner B, et al. Clin Pharmacokinet. 2001;40(2):85-104. PMID: 11286326.
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Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses.
Uridine is a nucleoside, contains a uracil attached to a ribose ring via a β-N1-glycosidic bond.
Rifampin is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.
Mitomycin C is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers.
Mercaptopurine is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
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