Pharmacokinetics of capecitabine (Xeloda) in Japanese and Caucasian patients with breast cancer

Reigner, Bruno; Watanabe, Tôru; Schüller, J.; Lucraft, Helen; Sasaki, Yasutsuna; Bridgewater, John; Sendo, Toshiaki; McAleer, J. J.; Kuranami, Masaru; Poole, Christopher; Kimura, M; Monkhouse, Jayne; Yorulmaz, Cahit; Weidekamm, E.; Grange, Susan

doi:10.1007/s00280-003-0642-8

Cited by 43 publications

(41 citation statements)

References 28 publications

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“…Following doses of 1250 to 1255 mg/m 2 , the mean area under the curve of 5Ј-DFCR ranged from 6.51 to 14.1 mg/h/l with a coefficient of variation up to 77% (Reigner et al, 2003). According to our data, 5Ј-DFCR is equally well formed by CES1A1 and CES2.…”

Section: Discussionsupporting

confidence: 51%

“…This three-step targeted prodrug approach was developed to increase the bioavailability of 5-fluorouracil by reducing the catabolism of 5-fluorouracil in the liver by dihydropyrimidine dehydrogenases and targeting 5-fluorouracil formation to the tumor. Pharmacokinetic analyses indicate high interpatient variability in the exposure to capecitabine and its metabolites in plasma (Reigner et al, 2003).…”

mentioning

confidence: 99%

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Hydrolysis of Capecitabine to 5′-Deoxy-5-fluorocytidine by Human Carboxylesterases and Inhibition by Loperamide

Quinney

Sanghani

Davis

et al. 2005

J Pharmacol Exp Ther

166

117

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Capecitabine is an oral prodrug of 5-fluorouracil that is indicated for the treatment of breast and colorectal cancers. A three-step in vivo-targeted activation process requiring carboxylesterases, cytidine deaminase, and thymidine phosphorylase converts capecitabine to 5-fluorouracil. Carboxylesterases hydrolyze capecitabine's carbamate side chain to form 5Ј-deoxy-5-fluorocytidine (5Ј-DFCR). This study examines the steady-state kinetics of recombinant human carboxylesterase isozymes carboxylesterase (CES) 1A1, CES2, and CES3 for hydrolysis of capecitabine with a liquid chromatography/mass spectroscopy assay. Additionally, a spectrophotometric screening assay was utilized to identify drugs that may inhibit carboxylesterase activation of capecitabine. CES1A1 and CES2 hydrolyze capecitabine to a similar extent, with catalytic efficiencies of 14.7 and 12.9 min Ϫ1 mM Ϫ1

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Section: Discussionsupporting

confidence: 51%

mentioning

confidence: 99%

Hydrolysis of Capecitabine to 5′-Deoxy-5-fluorocytidine by Human Carboxylesterases and Inhibition by Loperamide

Quinney

Sanghani

Davis

et al. 2005

J Pharmacol Exp Ther

166

117

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show abstract

“…Considering the fact that, capecitabine exhibits linear increases in C max and AUC 0-¥ when dosage increases, 4 it is possible to normalize the previously reported pharmacokinetic data to a dose of 1500 mg. Therefore, it can be concluded that the pharmacokinetic parameters obtained in this study were similar to the published pharmacokinetic studies 26,28 and it seems that there are no racial differences in capecitabine pharmacokinetics.…”

Section: Application Of the Methodssupporting

confidence: 72%

Development and validation of an ecofriendly HPLC-UV method for determination of capecitabine in human plasma: Application to pharmacokinetic studies

Hassanlou¹,

Rajabi²,

Shahrasbi³

et al. 2016

S.Afr.j.chem.

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A simple, rapid, cost-effective and green high-performance liquid chromatographic assay for determination of capecitabine in human plasma using a C 18 reversed-phase analytical column was developed and validated. within-day variability was less than 15 % and the bias was within ±15 %. This validated method was successfully applied to a pharmacokinetic study enrolling seven Iranian cancer patients after administration of a morning oral dose of 1500 mg.

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“…13 There is no evidence of drug accumulation across a range of doses, and pharmacokinetics were found to be similar between Caucasian and Japanese patient populations. 14,15 The half-life of capecitabine is between 0.49 and 0.89 hours, while the half-life of the metabolite (5-FU) extends from 0.67 to 1.15 hours. 13,14,16 Of additional interest, capecitabine is supposed to be dosed within 30 minutes of food.…”

Section: Mode Of Action and Pharmacokineticsmentioning

confidence: 99%

Capecitabine in the management of colorectal cancer

Zafar¹,

Hirsch²

2011

CMAR

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5-Fluorouracil has been a mainstay in the treatment of colorectal cancer for nearly five decades; however, the use of oral formulations of the medication has been gaining increasing traction since capecitabine was approved for use in adjuvant settings by the US Food and Drug Administration in 2005. The use of capecitabine has since spread to a number of off-label indications, including the treatment of advanced or metastatic colorectal cancer and the neoadjuvant treatment of rectal cancer. In light of increasing utilization, it is critical that clinicians have a firm understanding of the literature supporting capecitabine across various settings as well as the attributes of the drug, such as its dosing recommendations, side-effect profile, and use in the elderly. The purpose of this review is to synthesize the literature in a fashion that can be used to help guide decisions. In a setting of increasing focus on cost, the pharmacoeconomic literature is also briefly reviewed.

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Pharmacokinetics of capecitabine (Xeloda) in Japanese and Caucasian patients with breast cancer

Cited by 43 publications

References 28 publications

Hydrolysis of Capecitabine to 5′-Deoxy-5-fluorocytidine by Human Carboxylesterases and Inhibition by Loperamide

Hydrolysis of Capecitabine to 5′-Deoxy-5-fluorocytidine by Human Carboxylesterases and Inhibition by Loperamide

Development and validation of an ecofriendly HPLC-UV method for determination of capecitabine in human plasma: Application to pharmacokinetic studies

Capecitabine in the management of colorectal cancer

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