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Chemical Compound Review

Capiibine     pentylN-[1-[(2R,3R,4S,5R)- 3,4-dihydroxy-5...

Synonyms: Caxeta, Xabine, Xeloda, Capecitabin, CAPECITABINE, ...
 Bolaños,  Celio, Manuel Hidalgo,  Johnson,  Leek,  deJonge,  Schmid,  Griffiths,  Sanderink,  Catena,  Strychor,  French,  Yoshizumi,  Russo,  Troy, Patricia Martins,  von Gerstenberg-Helldorf,  Husseinzadeh,  Chen,  Stubbs, Robert Pelley,  Fiveash,  Nishimura,  Fakih,  Mariani,  Schwarz,  Eskens,  Judson,  Buzzoni,  Takino,  Lenauer,  Lopez-Gómez,  Yubero,  Gattinoni,  Carter,  Blessing,  Semiond,  Lang,  Saif, Wells Messersmith, Richat Abbas,  ter Steeg,  Zamboni,  Ohta,  Szatrowski,  Hoff, Antonio Jimeno,  Samid,  Hofheinz,  Fushida,  Chung,  Bertucci,  Blanquicett,  Vicent,  Cohn,  Kornek,  Ramnath,  Pazdur,  Thornton,  Fujimura,  Zamboni,  Zilembo,  Schulz,  Ratain, Charles Erlichman,  Gnad,  Kindler,  van Oosterom,  Abbruzzese,  Depisch,  Longarini,  Miller,  Carpenter,  Lassere,  Schilsky,  Llosa,  Feliu,  Morita,  Cartwright,  Vogelzang,  Lopez,  Mannel,  Varkey,  Gómez-Reina, Gary Croghan,  Miwa,  Cox,  Deery, Joseph Boni,  Ninomiya, Michelle Rudek,  Dumez, Charles Zacharchuk,  Ricotta,  Verweij,  Javle,  Selleslach,  Kraus-Tiefenbacher,  Darcy,  Sparreboom,  Della Torre,  Sanz-Lacalle,  Bajetta,  Schüll,  Assadourian,  Creaven,  Kovats,  Leach,  Steg,  Procopio,  Willeke,  González-Baron,  Casado,  Post,  Wenz, Ronald Bukowski,  Escudero,  Soepenberg,  Garcia,  Eloubeidi,  Hochhaus,  Lenz,  Harris,  Schneeweiss,  Hehlmann,  Diasio,  Terada,  Scheithauer,  Polito,  Raderer,  Trump,  Faithfull,  Müldner, Ross Donehower,  Nagai, Dan Laheru,  Repinski,  
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Disease relevance of Xeloda

  • Multicenter phase II study of capecitabine in paclitaxel-refractory metastatic breast cancer [1].
  • The objectives of this study were to assess the safety and efficacy of capecitabine in patients with metastatic colorectal carcinoma who progressed despite previous FU therapy [2].
  • No association between TP:DPD ratio and efficacy of capecitabine or severity of toxicities was identified [3].
  • PATIENTS AND METHODS: Nineteen patients with rectal cancer clinical stage T3-4, Nx received weekly irinotecan 50 mg/m(2) (days 1, 8, 15, 22, 29) and two doses of capecitabine (days 1 through 38; dose level [DL] I, 500 mg/m(2) bid; DL II, 625 mg/m(2) bid) according to phase I methodology [4].
  • Phase II study of oral capecitabine in patients with advanced or metastatic pancreatic cancer [5].

Psychiatry related information on Xeloda


High impact information on Xeloda


Chemical compound and disease context of Xeloda


Biological context of Xeloda


Anatomical context of Xeloda


Associations of Xeloda with other chemical compounds


Gene context of Xeloda


Analytical, diagnostic and therapeutic context of Xeloda

  • CONCLUSION: The recommended dose for phase II evaluation is capecitabine 825 mg/m(2) bid, administered without break during a conventional radiotherapy period of about 6 weeks [33].
  • The present study investigated whether the efficacy of capecitabine and its intermediate metabolite 5'-dFUrd correlates with levels of these enzymes in various human cancer xenograft models [24].
  • PATIENTS AND METHODS: Fifty-one patients with advanced CRC who were >/= 70 years and considered ineligible for combination chemotherapy received oral capecitabine 1,250 mg/m(2) twice daily on days 1 to 14 every 3 weeks [9].
  • These results together with its generally tolerable safety profile and the added advantage of oral administration provide the basis for further evaluating capecitabine as a single agent or in combination with other treatment modalities in this patient population [5].
  • The dose-intensified bimonthly capecitabine arm, however, seems to be more effective in increasing both response rate and progression-free survival time [11].


  1. Multicenter phase II study of capecitabine in paclitaxel-refractory metastatic breast cancer. Blum, J.L., Jones, S.E., Buzdar, A.U., LoRusso, P.M., Kuter, I., Vogel, C., Osterwalder, B., Burger, H.U., Brown, C.S., Griffin, T. J. Clin. Oncol. (1999) [Pubmed]
  2. Phase II study of capecitabine in patients with fluorouracil-resistant metastatic colorectal carcinoma. Hoff, P.M., Pazdur, R., Lassere, Y., Carter, S., Samid, D., Polito, D., Abbruzzese, J.L. J. Clin. Oncol. (2004) [Pubmed]
  3. Phase I study of capecitabine with concomitant radiotherapy for patients with locally advanced pancreatic cancer: expression analysis of genes related to outcome. Saif, M.W., Eloubeidi, M.A., Russo, S., Steg, A., Thornton, J., Fiveash, J., Carpenter, M., Blanquicett, C., Diasio, R.B., Johnson, M.R. J. Clin. Oncol. (2005) [Pubmed]
  4. Phase I trial of capecitabine and weekly irinotecan in combination with radiotherapy for neoadjuvant therapy of rectal cancer. Hofheinz, R.D., von Gerstenberg-Helldorf, B., Wenz, F., Gnad, U., Kraus-Tiefenbacher, U., Müldner, A., Hehlmann, R., Post, S., Hochhaus, A., Willeke, F. J. Clin. Oncol. (2005) [Pubmed]
  5. Phase II study of oral capecitabine in patients with advanced or metastatic pancreatic cancer. Cartwright, T.H., Cohn, A., Varkey, J.A., Chen, Y.M., Szatrowski, T.P., Cox, J.V., Schulz, J.J. J. Clin. Oncol. (2002) [Pubmed]
  6. Implementation of capecitabine (Xeloda) into a cancer centre: UK experience. Faithfull, S., Deery, P. European journal of oncology nursing : the official journal of European Oncology Nursing Society. (2004) [Pubmed]
  7. Clinical picture: leopard-like vitiligo with capecitabine. Schmid-Wendtner, M.H., Wendtner, C.M., Volkenandt, M., Heinemann, V. Lancet (2001) [Pubmed]
  8. Safety and efficacy of two different doses of capecitabine in the treatment of advanced breast cancer in older women. Bajetta, E., Procopio, G., Celio, L., Gattinoni, L., Della Torre, S., Mariani, L., Catena, L., Ricotta, R., Longarini, R., Zilembo, N., Buzzoni, R. J. Clin. Oncol. (2005) [Pubmed]
  9. Capecitabine as first-line treatment for patients older than 70 years with metastatic colorectal cancer: an oncopaz cooperative group study. Feliu, J., Escudero, P., Llosa, F., Bolaños, M., Vicent, J.M., Yubero, A., Sanz-Lacalle, J.J., Lopez, R., Lopez-Gómez, L., Casado, E., Gómez-Reina, M.J., González-Baron, M. J. Clin. Oncol. (2005) [Pubmed]
  10. Phase I and pharmacokinetic study of oral irinotecan given once daily for 5 days every 3 weeks in combination with capecitabine in patients with solid tumors. Soepenberg, O., Dumez, H., Verweij, J., Semiond, D., deJonge, M.J., Eskens, F.A., ter Steeg, J., Selleslach, J., Assadourian, S., Sanderink, G.J., Sparreboom, A., van Oosterom, A.T. J. Clin. Oncol. (2005) [Pubmed]
  11. Randomized multicenter phase II trial of two different schedules of capecitabine plus oxaliplatin as first-line treatment in advanced colorectal cancer. Scheithauer, W., Kornek, G.V., Raderer, M., Schüll, B., Schmid, K., Kovats, E., Schneeweiss, B., Lang, F., Lenauer, A., Depisch, D. J. Clin. Oncol. (2003) [Pubmed]
  12. Dose-escalating study of capecitabine plus gemcitabine combination therapy in patients with advanced cancer. Schilsky, R.L., Bertucci, D., Vogelzang, N.J., Kindler, H.L., Ratain, M.J. J. Clin. Oncol. (2002) [Pubmed]
  13. Effect of hepatic dysfunction due to liver metastases on the pharmacokinetics of capecitabine and its metabolites. Twelves, C., Glynne-Jones, R., Cassidy, J., Schüller, J., Goggin, T., Roos, B., Banken, L., Utoh, M., Weidekamm, E., Reigner, B. Clin. Cancer Res. (1999) [Pubmed]
  14. Antitumor efficacy of capecitabine and celecoxib in irradiated and lead-shielded, contralateral human BxPC-3 pancreatic cancer xenografts: clinical implications of abscopal effects. Blanquicett, C., Saif, M.W., Buchsbaum, D.J., Eloubeidi, M., Vickers, S.M., Chhieng, D.C., Carpenter, M.D., Sellers, J.C., Russo, S., Diasio, R.B., Johnson, M.R. Clin. Cancer Res. (2005) [Pubmed]
  15. Significant effect of capecitabine on the pharmacokinetics and pharmacodynamics of warfarin in patients with cancer. Camidge, R., Reigner, B., Cassidy, J., Grange, S., Abt, M., Weidekamm, E., Jodrell, D. J. Clin. Oncol. (2005) [Pubmed]
  16. Pharmacobiologically based scheduling of capecitabine and docetaxel results in antitumor activity in resistant human malignancies. Nadella, P., Shapiro, C., Otterson, G.A., Hauger, M., Erdal, S., Kraut, E., Clinton, S., Shah, M., Stanek, M., Monk, P., Villalona-Calero, M.A. J. Clin. Oncol. (2002) [Pubmed]
  17. Effect of food on the pharmacokinetics of capecitabine and its metabolites following oral administration in cancer patients. Reigner, B., Verweij, J., Dirix, L., Cassidy, J., Twelves, C., Allman, D., Weidekamm, E., Roos, B., Banken, L., Utoh, M., Osterwalder, B. Clin. Cancer Res. (1998) [Pubmed]
  18. UGT1A7 and UGT1A9 polymorphisms predict response and toxicity in colorectal cancer patients treated with capecitabine/irinotecan. Carlini, L.E., Meropol, N.J., Bever, J., Andria, M.L., Hill, T., Gold, P., Rogatko, A., Wang, H., Blanchard, R.L. Clin. Cancer Res. (2005) [Pubmed]
  19. Capecitabine-induced abnormalities in thyroid function tests. Narula, H.S., Carlson, H.E. Am. J. Med. (2004) [Pubmed]
  20. Role of the human concentrative nucleoside transporter (hCNT1) in the cytotoxic action of 5[Prime]-deoxy-5-fluorouridine, an active intermediate metabolite of capecitabine, a novel oral anticancer drug. Mata, J.F., García-Manteiga, J.M., Lostao, M.P., Fernández-Veledo, S., Guillén-Gómez, E., Larrayoz, I.M., Lloberas, J., Casado, F.J., Pastor-Anglada, M. Mol. Pharmacol. (2001) [Pubmed]
  21. Clinical pharmacokinetics of capecitabine. Reigner, B., Blesch, K., Weidekamm, E. Clinical pharmacokinetics. (2001) [Pubmed]
  22. Anti-metastatic effect of capecitabine on human colon cancer xenografts in nude mouse rectum. Ninomiya, I., Terada, I., Yoshizumi, T., Takino, T., Nagai, N., Morita, A., Fushida, S., Nishimura, G., Fujimura, T., Ohta, T., Miwa, K. Int. J. Cancer (2004) [Pubmed]
  23. Augmentation of the antitumor activity of capecitabine by a tumor selective dihydropyrimidine dehydrogenase inhibitor, RO0094889. Endo, M., Miwa, M., Eda, H., Ura, M., Tanimura, H., Ishikawa, T., Miyazaki-Nose, T., Hattori, K., Shimma, N., Yamada-Okabe, H., Ishitsuka, H. Int. J. Cancer (2003) [Pubmed]
  24. Positive correlation between the efficacy of capecitabine and doxifluridine and the ratio of thymidine phosphorylase to dihydropyrimidine dehydrogenase activities in tumors in human cancer xenografts. Ishikawa, T., Sekiguchi, F., Fukase, Y., Sawada, N., Ishitsuka, H. Cancer Res. (1998) [Pubmed]
  25. Phase I and pharmacokinetic study of weekly docetaxel, cisplatin, and daily capecitabine in patients with advanced solid tumors. Fakih, M.G., Creaven, P.J., Ramnath, N., Trump, D., Javle, M., Strychor, S., Repinski, T.V., Zamboni, B.A., Schwarz, J.K., French, R.A., Zamboni, W.C. Clin. Cancer Res. (2005) [Pubmed]
  26. Noninvasive measurements of capecitabine metabolism in bladder tumors overexpressing thymidine phosphorylase by fluorine-19 magnetic resonance spectroscopy. Chung, Y.L., Troy, H., Judson, I.R., Leek, R., Leach, M.O., Stubbs, M., Harris, A.L., Griffiths, J.R. Clin. Cancer Res. (2004) [Pubmed]
  27. A phase I study of EKB-569 in combination with capecitabine in patients with advanced colorectal cancer. Laheru, D., Croghan, G., Bukowski, R., Rudek, M., Messersmith, W., Erlichman, C., Pelley, R., Jimeno, A., Donehower, R., Boni, J., Abbas, R., Martins, P., Zacharchuk, C., Hidalgo, M. Clin. Cancer Res. (2008) [Pubmed]
  28. Rationally designed pharmacogenomic treatment using concurrent capecitabine and radiotherapy for glioblastoma; gene expression profiles associated with outcome. Grunda, J.M., Fiveash, J., Palmer, C.A., Cantor, A., Fathallah-Shaykh, H.M., Nabors, L.B., Johnson, M.R. Clin. Cancer Res. (2010) [Pubmed]
  29. Enzyme expression profiles suggest the novel tumor-activated fluoropyrimidine carbamate capecitabine (Xeloda) might be effective against papillary thyroid cancers of children and young adults. Patel, A., Pluim, T., Helms, A., Bauer, A., Tuttle, R.M., Francis, G.L. Cancer Chemother. Pharmacol. (2004) [Pubmed]
  30. Phase II clinical trial of capecitabine in ovarian carcinoma recurrent 6-12 months after completion of primary chemotherapy, with exploratory TS, DPD, and TP correlates: a Gynecologic Oncology Group study. Garcia, A.A., Blessing, J.A., Lenz, H.J., Darcy, K.M., Mannel, R.S., Miller, D.S., Husseinzadeh, N. Gynecol. Oncol. (2005) [Pubmed]
  31. Hydrolysis of capecitabine to 5'-deoxy-5-fluorocytidine by human carboxylesterases and inhibition by loperamide. Quinney, S.K., Sanghani, S.P., Davis, W.I., Hurley, T.D., Sun, Z., Murry, D.J., Bosron, W.F. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  32. Relationship between single nucleotide polymorphisms and haplotypes in DPYD and toxicity and efficacy of capecitabine in advanced colorectal cancer. Deenen, M.J., Tol, J., Burylo, A.M., Doodeman, V.D., de Boer, A., Vincent, A., Guchelaar, H.J., Smits, P.H., Beijnen, J.H., Punt, C.J., Schellens, J.H., Cats, A. Clin. Cancer Res. (2011) [Pubmed]
  33. Phase I trial evaluating the concurrent combination of radiotherapy and capecitabine in rectal cancer. Dunst, J., Reese, T., Sutter, T., Zühlke, H., Hinke, A., Kölling-Schlebusch, K., Frings, S. J. Clin. Oncol. (2002) [Pubmed]
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