Modelling of ftorafur and 5-fluorouracil pharmacokinetics following oral UFT administration. A population study in 30 patients with advanced breast cancer

Cancer Chemotherapy and Pharmacology

Volumn 52, Issue 2, 2003, Pages 99-107

  Urien, S ^a   Fumoleau, P ^b   Campone, M ^b   Kerbrat, P ^c   Bonneterre, J ^d   Fargeot, P ^e   Deporte Fety, R ^b  

^a CENTRE RENÉ HUGUENIN   (France)

^b CENTRE RENÉ GAUDUCHEAU   (France)

^c CENTRE EUGÈNE MARQUIS   (France)

^d CENTRE OSCAR LAMBRET   (France)

^e Centre George Fra ois Leclerc   (France)

Author keywords

Oral fluoropyrimidine; Population pharmacokinetics; UFT

Indexed keywords

FLUOROURACIL; FOLINIC ACID; NAVELBINE; TEGAFUR; UFT;

ANEMIA; AREA UNDER THE CURVE; ARTICLE; BREAST CANCER; BREAST METASTASIS; CANCER COMBINATION CHEMOTHERAPY; CLINICAL ARTICLE; CLINICAL TRIAL; COMPETITIVE INHIBITION; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOSE TIME EFFECT RELATION; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG METABOLISM; HUMAN; MAXIMUM TOLERATED DOSE; MULTICENTER STUDY; NAUSEA; NEUTROPENIA; POPULATION MODEL; PRACTICE GUIDELINE; PRIORITY JOURNAL; SIDE EFFECT; VOMITING;

ADMINISTRATION, ORAL; ADULT; AGED; ANTINEOPLASTIC AGENTS, PHYTOGENIC; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; BREAST NEOPLASMS; FEMALE; FLUOROURACIL; HUMANS; LEUCOVORIN; MIDDLE AGED; MODELS, BIOLOGICAL; NEOPLASM METASTASIS; TEGAFUR; URACIL; VINBLASTINE;

EID: 0041375581     PISSN: 03445704     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00280-003-0616-x     Document Type: Article

References (31)

1. Borner MM, Castiglione M, Bacchi M, Weber W, Herrmann R, Fey MF, Pagani O, Leyvraz S, Morant R, Pestalozzi B, Hanselmann S, Goldhirsch A (1998) The impact of adding low-dose leucovorin to monthly 5-fluorouracil in advanced colorectal carcinoma: results of a phase III trial. Swiss Group for Clinical Cancer Research (SAKK). Ann Oncol 9:535
2. Borner MM, Schöffski P, de Wit R, Caponigro F, Comella G, Sulkes A, Greim G, Peters GJ, van der Born K, Wanders J, de Boer RF, Martin C, Fumoleau P (2002) Patient preference and pharmacokinetics of oral modulated UFT versus intravenous fluorouracil and leucovorin: a randomised crossover trial in advanced colorectal cancer. Eur J Cancer 38:349
3. Bressole F, Joulia JM, Pinguet F, Ychou M, Astre C, Duffour J, Gomeni R (1999) Circadian rhythm of 5-fluorouracil population pharmacokinetics in patients with metastatic colorectal cancer. Cancer Chemother Pharmacol 44:295
4. Chatelut E, Boddy AV, Peng B, Rubie H, Lavit M, Dezeuze A, Pearson AD, Roche H, Robert A, Newell DR, Canal P (1996) Population pharmacokinetics of carboplatin in children. Clin Pharmacol Ther 59:436
5. Christophidis N, Mihaly G, Vadja F, Louis W (1979) Comparison of liquid and gas-liquid chromatographic assays of 5 fluorouracil in plasma. Clin Chem 25:83
6. Creaven PJ, Rustum YM, Petrelli NJ, Meropol NJ, Raghavan D, Rodriguez-Bigas M, Levine EG, Frank C, Udvary-Nagy S, Proefrock A (1994) Phase I and pharmacokinetic evaluation of floxuridine/leucovorin given on the Roswell Park weekly regimen. Cancer Chemother Pharmacol 34:261
7. Damle B, Ravandi F, Kaul S, Sonnichsen D, Ferreira I, Brooks D, Stewart D, Alberts D, Pazdur R (2001) Effect of food on the oral bioavailability of UFT and leucovorin in cancer patients. Clin Cancer Res 7:517
8. Deporte-Fety R, Urien S, Milano G, Kerbrat P, Bonneterre J, Fargeot P, Fumoleau P (2001) A phase I pharmacokinetic (PK) and pharmacodynamic (PD) analysis of UFT/leucovorin (LV) in combination with vinorelbine (V). Proc Am Soc Clin Oncol 20:90a
9. Diasio RB, Harris BE (1989) Clinical pharmacology of 5-fluorouracil. Clin Pharmacokinet 16:215
10. Freyer G, Tranchand B, Ligneau B, Ardiet C, Souquet PJ, Court-Fortune I, Riou R, Rebattu P, Boissel JP, Trillet-Lenoir V, Girard P (2000) Population pharmacokinetics of doxorubicin, etoposide and ifosfamide in small cell lung cancer patients: results of a multicentre study. Br J Clin Pharmacol 50:315
11. Fujii S, Ikenaka K, Fukushima M, Shirasaka T (1978) Effect of uracil and its derivatives on antitumor activity of 5-fluorouracil and 1-(tetrahydro-2-furyl)-5-fluorouracil. Gann 69:763
12. Fumoleau P, Delozier T, Extra JM, Canobbio L, Delgado FM, Hurteloup P (1995) Vinorelbine (Navelbine) in the treatment of breast cancer: the European experience. Semin Oncol 22:22
13. Harris BE, Song R, Soong SJ, Diasio RB (1990) Relationship between dihydropyrimidine dehydrogenase activity and plasma 5-fluorouracil levels with evidence for circadian variation of enzyme activity and plasma drug levels in cancer patients receiving 5-fluorouracil by protracted continuous infusion. Cancer Res 50:197
14. Ho DH, Covington W, Brown N, Lin SN, Pazdur R, Huo YY, Creaven PJ, Rustum YM, Meropol NJ, Lassere Y, Kuritani J, Hayakawa T (2000) Oral uracil and ftorafur plus leucovorin: pharmacokinetics and toxicity in patients with metastatic cancer. Cancer Chemother Pharmacol 46:351
15. Ikeda K, Yoshisue K, Matsushima E, Nagayama S, Kobayashi K, Tyson CA, Chiba K, Kawaguchi Y (2000) Bioactivation of tegafur to 5-fluorouracil is catalyzed by cytochrome P-450 2A6 in human liver microsomes in vitro. Clin Cancer Res 6:4409
16. Komatsu T, Yamazaki H, Shimada N, Nagayama S, Kawaguchi Y, Nakajima M, Yokoi T (2001) Involvement of microsomal cytochrome P450 and cytosolic thymidine phosphorylase in 5-fluorouracil formation from tegafur in human liver. Clin Cancer Res 7:675
17. Meropol N, Rustum Y, Petrelli N, Rodriguez-Bigas M, Frank C, Ho DH, Kurowski M, Creaven PJ (1996) A phase I and pharmacokinetic study of oral uracil, ftorafur, and leucovorin in patients with advanced cancer. Cancer Chemother Pharmacol 37:581
18. Meropol NJ, Sonnichsen DS, Birkhofer M, Ferreira I, Noel D (1999) Bioavailability and phase II study of oral UFT plus leucovorin in patients with relapsed or refractory colorectal cancer. Cancer Chemother Pharmacol 43:221
19. Milano G, McLeod HL (2000) Can dihydropyrimidine dehydrogenase impact 5-fluorouracil-based treatment? Eur J Cancer 36:37
20. Mori K, Hasegawa M, Nishida M, Toma H, Fukuda M, Kubota T, Nagasue N, Yamana H, Hirakawa-YS Chung K, Ikeda T, Takasaki K, Oka M, Kameyama M, Toi M, Fujii H, Kitamura M, Murai M, Sasaki H, Ozono S, Makuuchi H, Shimada Y, Onishi Y, Aoyagi S, Mizutani K, Ogawa M, Nakao A, Kinoshita H, Tono T, Imamoto H, Nakashima Y, Manabe T (2000) Expression levels of thymidine phosphorylase and dihydropyrimidine dehydrogenase in various human tumor tissues. Int J Oncol 17:33
21. Muggia FM, Wu X, Spicer D, Groshen S, Jeffers S, Gail Leichman C, Leichman L, Chan KK (1996) Phase I and pharmacokinetic study of oral UFT, a combination of 5-fluorouracil prodrug tegafur and uracil. Clin Cancer Res 2:1461
22. Ota K, Taguchi T, Kimura K (1988) Report on nationwide pooled data and cohort investigation in UFT phase II study. Cancer Chemother Pharmacol 22:333
23. Pelkonen O, Rautio A, Raunio H, Pasanen M (2000) CYP2A6: a human coumarin 7-hydroxylase. Toxicology 144:139
24. Pinedo HM, Peters GF (1988) Fluorouracil: biochemistry and pharmacology. J Clin Oncol 6:1653
25. Poon MA, O'Connell J, Moertel CG, Wieand HS, Cullinan SA, Everson LK, Krook JE, Mailliard JA, Laurie JA, Tschetter LK, Weisenfeld M (1989) Biochemical modulation of fluorouracil: evidence of significant improvement of survival and quality of life in patients with advanced colorectal carcinoma. J Clin Oncol 10:1407
26. Ratain MJ (1998) Body-surface area as a basis for dosing of anticancer agents: science, myth, or habit? J Clin Oncol 16:2297
27. Shoemaker RC, Cohen AF(1996) Estimating impossible curves using NONMEM. Br J Clin Pharmacol 42:283
28. Thomas JP, Arzoomanian R, Alberti D, Feierabend C, Binger K, Tutsch KD, Steele T, Marnocha R, Smith C, Smith S, MacDonald J, Wilding G, Bailey H (2001) Phase I clinical and pharmacokinetic trial of UFT. Cancer Chemother Pharmacol 48:467
29. Urien S (1997) MP2 (V 2.0) - a Windows application for population pharmacokinetics. In: Aarons L, et al (eds) The population approach: measuring and managing variability in response, concentration. Eur-OP, Brussels, p 419
30. Wijnand HP (1988) Pharmacokinetic model equations for the one- and two-compartment models with the first-order processes in which the absorption and exponential elimination or distribution rate constants are equal. J Pharmacokinet Biopharm 16:109
31. Yamazaki H, Komatsu T, Takemoto K, Shimada N, Nakajima M, Yokoi T (2001) Rat cytochrome P450 1a and 3a enzymes involved in bioactivation of tegafur to 5-fluorouracil and autoinduced by tegafur in liver microsomes. Drug Metab Dispos 29:794