Highlights from: 5-Fluorouracil drug management pharmacokinetics and pharmacogenomics workshop: Orlando, Florida; January 2007 - 5-Fluorouracil drug management: Pharmacokinetics and pharmacogenomics workshop meeting summary

Clinical Colorectal Cancer

Volumn 6, Issue 6, 2007, Pages 407-422

  Bertino, Joseph ^a   Gamelin, Erick ^b   Milano, Gérard ^c  

^a RUTGERS CANCER INSTITUTE OF NEW JERSEY   (United States)

^b CENTRE PAUL PAPIN   (France)

^c CENTRE ANTOINE LACASSAGNE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

BEVACIZUMAB; CAPECITABINE; CISPLATIN; DIHYDROFLUOROURACIL; DIHYDROPYRIMIDINE DEHYDROGENASE; DIHYDROURACIL; FLUOROPYRIMIDINE DERIVATIVE; FLUOROURACIL; FOLINIC ACID; LEVAMISOLE; METHOTREXATE; MONOCLONAL ANTIBODY; OXALIPLATIN; SPARFOSIC ACID; TRIMETREXATE; URACIL;

ADJUVANT THERAPY; ADVANCED CANCER; ALOPECIA; AREA UNDER THE CURVE; BLOOD TOXICITY; BONE MARROW SUPPRESSION; BREAST CARCINOMA; CLINICAL TRIAL; COLON ADENOCARCINOMA; COLON CANCER; COLORECTAL CANCER; COMBINATION CHEMOTHERAPY; CONFERENCE PAPER; CONTINUOUS INFUSION; CONTROLLED CLINICAL TRIAL; CORRELATION ANALYSIS; DIARRHEA; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DETERMINATION; DRUG MEGADOSE; DRUG MONITORING; DRUG STABILITY; ENZYME ACTIVITY; ENZYME DEFICIENCY; GASTROINTESTINAL TOXICITY; GENOTYPE; HAND FOOT SYNDROME; HEAD AND NECK CANCER; HUMAN; IMMUNOASSAY; LEUKOPENIA; LIQUID CHROMATOGRAPHY; LOW DRUG DOSE; META ANALYSIS; MONOTHERAPY; MUCOSA INFLAMMATION; NAUSEA; NAUSEA AND VOMITING; NEUTROPENIA; OVERALL SURVIVAL; PHARMACOGENOMICS; PHARMACOLOGICAL PARAMETERS; PLASMA HALF LIFE; RANDOMIZED CONTROLLED TRIAL; RECTUM CANCER; RECTUM CARCINOMA; STOMACH CANCER; STOMATITIS; SURVIVAL RATE; SYSTEMATIC REVIEW; TANDEM MASS SPECTROMETRY; TREATMENT RESPONSE; TUMOR GROWTH; UNSPECIFIED SIDE EFFECT;

EID: 34247543930     PISSN: 15330028     EISSN: None     Source Type: Journal    
DOI: 10.1016/s1533-0028(11)70480-7     Document Type: Conference Paper

References (91)

1. Midgley R, Kerr D. Colorectal cancer. Lancet 1999; 353:391-399.
2. Meyerhardt JA, Mayer RJ. Systemic therapy for colorectal cancer. N Engl J Med 2005; 352:476-487.
3. Poon MA, O'Connell MJ, Moertel CG, et al. Biochemical modulation of fluorouracil: evidence of significant improvement of survival and quality of life in patients with advanced colorectal carcinoma. J Clin Oncol 1989; 7:1407-1418.
4. Hoff P, Pazdur R. Progress in the development of novel treatments for colorectal cancer. Oncology 2004; 18:705-708.
5. The Meta-Analysis Group in Cancer. Modulation of fluorouracil by leucovorin in patients with advanced colorectal cancer: an updated meta-analysis. J Clin Oncol 2004; 22:3766-3775.
6. Buroker TR, O'Connell MJ, Wieland HS, et al. Randomized comparison of two schedules of fluorouracil and leucovorin in the treatment of advanced colorectal cancer. J Clin Oncol 1994; 12:14-20.
7. de Gramont A, Bosset JF, Milan C, et al. Randomized trial comparing monthly low-dose leucovorin and fluorouracil bolus with bimonthly high-dose leucovorin and fluorouracil bolus plus continuous infusion for advanced colorectal cancer: a French Intergroup study. J Clin Oncol 1997; 15:808-815.
8. The Meta-Analysis Group in Cancer. Efficacy of intravenous continuous infusion of fluorouracil compared with bolus administration in advanced colorectal cancer. J Clin Oncol 1998; 16:301-308.
9. The Meta-Analysis Group in Cancer. Toxicity of fluorouracil in patients with advanced colorectal cancer: effect of administration schedule and prognostic factors. J Clin Oncol 1998; 16:3537-3541.
10. Chu E, Eng C, Abbruzzese J, et al. Efficacy and safety of capecitabine for colorectal cancer. Am J Oncol Rev 2003; 2(suppl 3):1-28.
11. Hoff PM, Ansari R, Batist G, et al. Comparison of oral capecitabine versus intravenous fluorouracil plus leucovorin as first-time treatment in 605 patients with metastatic colorectal cancer: results of a randomized phase III study. J Clin Oncol 2001; 19:2282-2292.
12. van Cutsem E, Twelves C, Cassidy J, et al. Oral capecitabine compared with intravenous fluorouracil plus leucovorin in patients with metastatic colorectal cancer: results of a large phase III study. J Clin Oncol 2001; 19:4097-4106.
13. Twelves C, for the Xeloda Colorectal Cancer Group. Capecitabine as first-line treatment in colorectal cancer: pooled data from two large, phase III trials. Eur J Cancer 2002; 38(suppl 2):S15-S20.
14. Saif MW. Capecitabine versus continuous-infusion 5-fluorouracil for colorectal cancer: a retrospective efficacy and safety comparison. Clin Colorectal Cancer 2005; 5:89-100.
15. Gray RG, Barnell J, Hills R, et al. QUASAR: a randomized study of adjuvant chemotherapy (CT) vs observation including 3238 colorectal cancer patients. Proc Am Soc Clin Oncol 2004; 23:246 (Abstract #3501).
16. Twelves C, Wong A, Nowacki MP, et al. Capecitabine as adjuvant treatment for stage III colon cancer. N Engl J Med 2005; 352:2696-2704.
17. Arbuck SG. Overview of clinical trials using 5-fluorouracil and leucovorin for the treatment of colorectal cancer. Cancer 1989; 63:1036-1044.
18. Au JL, Rustum YM, Ledesma EJ, et al. Clinical pharmacological studies of concurrent infusion of 5-fluorouracil and thymidine in the treatment of colorectal carcinoma. Cancer Res 1982; 42:2930-2937.
19. Brohee D. 5-Fluorouracil with or without folinic acid in human colorectal cancer: multivariate meta-analysis of the literature. Med Oncol Tumor Pharmacother 1991; 8:271-280.
20. Gamelin E, Boisdron-Celle M. Dose monitoring of 5-fluorouracil in patients with colorectal or head and neck cancer. Status of the art. Crit Rev Oncol Hematol 1999; 30:71-79.
21. Gamelin E, Boisdron-Celle M, Delva R, et al. Long-term weekly treatment of colorectal metastatic cancer with fluorouracil and leucovorin: results of a multicentric prospective trial of fluorouracil dosage optimization by pharmacokinetic monitoring in 152 patients. J Clin Oncol 1998; 16:1470-1478.
22. Gamelin E, Boisdron-Celle M, Guérin-Meyer V, et al. Correlation between uracil and dihydrouracil plasma ratio, and 5-fluorouracil pharmacokinetic parameters and tolerance in patients with advanced colorectal cancer. A potential interest for predicting 5-FU toxicity and for determining optimal 5-FU dosage. J Clin Oncol 1999; 17:1105-1110.
23. Gamelin EC, Danquechin-Dorval EM, Dumesnil R, et al. Relationship between 5-fluorouracil dose-intensity and therapeutic response in patients with advanced colorectal cancer receiving 5-FU containing infusional therapy. Cancer 1996; 77:441-451.
24. Thyss A, Milano G, Renee N, et al. Clinical pharmacokinetic study of 5-FU in continuous 5-day infusions for head and neck cancer. Cancer Chemother Pharmacol 1986; 16:64-66.
25. Trump DL, Egorin MJ, Forrest A, et al. Pharmacokinetic and pharmacodynamic analysis of fluorouracil during 72-hour continuous infusion with and without dipyridamole. J Clin Oncol 1991; 9:2027-2035.
26. Van Groeningen CJ, Pinedo HM, Heddes J, et al. Pharmacokinetics of 5-fluorouracil assessed with a sensitive mass spectrometric method in patients on a dose escalation schedule. Cancer Res 1988; 48:6956-6961.
27. Vokes EE, Mick R, Kies MS, et al. Pharmacodynamics of fluorouracil-based induction chemotherapy in advanced head and neck cancer. J Clin Oncol 1996; 14:1663-1671.
28. Ychou M, Duffour J, Kramar A, et al. Individual 5-FU dose adaptation in metastatic colorectal cancer: results of a phase II study using a bimonthly pharmacokinetically intensified LV5FU2 regimen. Cancer Chemother Pharmacol 2003; 52:282-290.
29. Yoshida T, Araki E, Ligo M, et al. Clinical significance of monitoring serum levels of 5-fluorouracil by continuous infusion in patients with advanced colonic cancer. Cancer Chemother Pharmacol 1990; 26:352-354.
30. Milano G, Etienne MC, Renee N, et al. Relationship between fluorouracil systemic exposure and tumor response and patient survival. J Clin Oncol 1994; 12:1291-1295.
31. Santini J, Milano G, Thyss A, et al. 5-FU therapeutic monitoring with dose adjustment leads to an improved therapeutic index in head and neck cancer. Br J Cancer 1989; 59:287-290.
32. Hillcoat BL, McCulloch PB, Figueredo AT, et al. Clinical response and plasma levels of 5-fluorouracil in patients with colonic cancer treated by drug infusion. Br J Cancer 1978; 38:719-724.
33. Hryniuk WM, Figueredo A, Goodyear M. Applications of dose intensity to problems in chemotherapy of breast and colorectal cancer. Semin Oncol 1987; 4:3-11.
34. Milano G, Roman P, Khater P, et al. Dose versus pharmacokinetics for predicting tolerance to 5-day continuous infusion of 5-FU. Int J Cancer 1988; 41:537-541.
35. Schneider M, Etienne MC, Milano G, et al. Phase II trial of cisplatin, fluorouracil and pure folinic acid for locally advanced head and neck cancer: a pharmacokinetic and clinical survey. J Clin Oncol 1995; 3:1656-1662.
36. Seitz JF, Cano JP, Rigault JP, et al. Chimiothérapie des cancers digestifs étendus par le 5-fluorouracile: relations entre la réponse clinique et la clairance plasmatique du médicament [in French]. Gastroenterol Clin Biol 1983; 7:374-380.
37. Sheiner LB. Population pharmacokinetics/pharmacodynamics. Ann Rev Pharmacol Toxicol 1993; 32:185-200.
38. Spicer DV, Ardalan B, Daniels JR, et al. Reevaluation of the maximum tolerated dose of continuous venous infusion of 5-fluorouracil with pharmacokinetics. Cancer Res 1988; 48:459-461.
39. Fety R, Rolland F, Barberi-Heyob M, et al. Clinical impact of pharmacokinetically-guided dose adaptation of 5-fluorouracil: results from a multicentric randomized trial in patients with locally advanced head and neck carcinomas. Clin Cancer Res 1998; 4:2039-2045.
40. Gamelin E, Jacob J, Danquechin-Dorval E, et al. Multicentric randomized trial comparing in weekly treatment of advanced colorectal cancer (CRC) intensified 5-fluorouracil and folinic acid (FA) with pharmacokinetic monitoring to a constant dose calculated with body surface area. J Clin Oncol 1998; 24(18 suppl):145s (Abstract #1039).
41. Diasio RB, Beavers TL, Carpenter JT. Familial deficiency of dihydropyrimidine dehydrogenase (biochemical basis for familial pyrimidinemia and severe 5-fluorouracil-induced toxicity). J Clin Invest 1988; 81:47-51.
42. Diasio RB, Johnson MR. Dihydropyrimidine dehydrogenase: its role in 5-fluorouracil clinical toxicity and tumor resistance. Clin Cancer Res 1999; 5:2672-2673.
43. Lu Z, Zhang R, Diasio RB. Dihydropyrimidine dehydrogenase activity in human peripheral blood mononuclear cells and liver: population characteristics, newly identified deficient patients, and clinical implication in 5-fluorouracil chemotherapy. Cancer Res 1993; 53:5433-5438.
44. Etienne MC, Lagrange JL, Dassonville O, et al. Population study of dihydropyrimidine dehydrogenase in cancer patients. J Clin Oncol 1994; 12:2248-2253.
45. Tuchman M, Stoeckeler JS, Kiang DT, et al. Familial pyrimidinemia and pyrimidinuria associated with severe fluorouracil toxicity. N Engl J Med 1985; 313:245-249.
46. Ezzeldin H, Diasio R. Dihydropyrimidine dehydrogenase deficiency, a pharmacogenetic syndrome associated with potentially life-threatening toxicity following 5-fluorouracil administration. Clin Colorectal Cancer 2004; 4:181-189.
47. Van Kuilenburg AB, Haasjes J, Richel DJ, et al. Clinical implication of dihydropyrimidine dehydrogenase (DPD) deficiency in patients with severe 5-fluorouracil-associated toxicity: identification of new mutations in the DPD gene. Clin Cancer Res 2000; 6:4705-4712.
48. Fleming R, Milano G, Thyss A, et al. Correlation between dihydropyrimidine dehydrogenase activity in peripheral mononuclear cells and systemic clearance of fluorouracil in cancer patients. Cancer Res 1992; 52:2899-2902.
49. Johnson MR, Yan J, Shao L, et al. Semi-automated radioassay for determination of dihydropyrimidine dehydrogenase (DPD) activity screening cancer patients for DPD deficiency, a condition associated with 5-fluorouracil toxicity. J Chromatogr B Analyt Technol Biomed Life Sci 1997; 696:183-191.
50. Boisdron-Celle M, Remaud G, Traore S, et al. 5-Fluorouracil-related severe toxicity: a comparison of different methods for the pretherapeutic detection of dihydropyrimidine dehydrogenase deficiency. Cancer Lett 2006. [Epub ahead of print].
51. Van Kuilenburg AB, Abreu R, Van Gennip A. Pharmacogenetic and clinical aspects of dihydropyrimidine dehydrogenase deficiency. Ann Clin Biochem 2003; 40:41-45.
52. McLeod HL, Collie-Duguid ESR, Vrecken P, et al. Nomenclature for human DPYD alleles. Pharmacogenetics 1998; 8:455-459.
53. Morel A, Boisdron-Celle M, Fey L, et al. Identification of a novel mutation in the dihydropyrimidine dehydrogenase gene in a patient with lethal outcome after 5-fluorouracil administration and determination of its frequency in a population of 500 patients with colorectal carcinoma. Clin Biochem 2007; 40:11-17.
54. Morel A, Boisdron-Celle M, Fey L, et al. Clinical relevance of different dihydropyrimidine dehydrogenase gene single nucleotide polymorphisms (SNP) upon 5-fluorouracil tolerance in a prospective clinical study in a French Caucasian population. Mol Cancer Ther 2006; 5:2895-2904.
55. Collie-Duguid ESR, Etienne MC, Milano G, et al. Known variant DPYD alleles do not explain DPD deficiency in cancer patients. Pharmacogenetics 2000; 10:217-223.
56. Gamelin E, Boisdron-Celle M, Turcant A, et al. Rapid and sensitive HPLC analysis of halogenopyrimidines in plasma. J Chromatogr B 1997; 695:409-416.
57. Remaud G, Boisdron-Celle M, Hameline C, et al. An accurate dihydrouracil/uracil determination using improved high performance liquid chromatography method for preventing fluoropyrimidines-related toxicity in clinical practice. J Chromatogr B 2005; 823:98-107.
58. Largillier R, Etienne-Grimaldi MC, Formento JL, et al. Pharmacogenetics of capecitabine in advanced breast cancer patients. Clin Cancer Res 2006; 12:5496-5502.
59. Bensadoun RJ, Etienne MC, Dassonville O, et al. Concomitant B.I.D. radiotherapy and chemotherapy with cisplatin and 5-fluorouracil in unresectable squamous-cell carcinoma of the pharynx: clinical and pharmacological data of a French multicenter phase II study. Int J Radiat Oncol 1998, 42:237-245.
60. Etienne MC, Chatelut E, Pivot X, et al. Co-variables influencing 5-fluorouracil clearance during continuous venous infusion. A NONMEM analysis. Eur J Cancer 1998; 34:92-97.
61. Van Kuilenburg AB. Dihydropyrimidine dehydrogenase and the efficacy and toxicity of 5-fluorouracil. Eur J Cancer 2004; 40:939-950.
62. Marsh S. Thymidylate synthase pharmacogenetics. Invest New Drugs 2005; 23:533-537.
63. Van Kuilenburg AB. Screening for dihydropyrimidine dehydrogenase deficiency: to do or not to do, that's the question. Cancer Invest 2006; 24:215-217.
64. Bocci G, Danesi R, Allegrini G, et al. Severe 5-fluorouracil toxicity associated with a marked alteration of pharmacokinetics of 5-fluorouracil and its catabolite 5-fluoro-5,6-dihydrouracil: a case report. Eur J Clin Pharmacol 2002; 58:593-595.
65. Di Paolo A, Danesi R, Falcone A, et al. Relationship between 5-fluorouracil disposition, toxicity and dihydropyrimidine dehydrogenase activity in cancer patients. Ann Oncol 2001; 12:1301-1306.
66. Di Paolo A, Danesi R, Ciofi L, et al. Improved analysis of 5-fluorouracil and 5,6-dihydro-5-fluorouracil by HPLC with diode array detection for determination of cellular dihydropyrimidine dehydrogenase activity and pharmacokinetic profiling. Ther Drug Monit 2005; 27:362-368.
67. Di Paolo A, Ibrahim T, Danesi R, et al. Relationship between plasma concentrations of 5-fluorouracil and 5-fluoro-5,6-dihydrouracil and toxicity of 5-fluorouracil infusions in cancer patients. Ther Drug Monit 2002; 24:588-593.
68. Di Paolo A, Danesi R, Vannozzi F, et al. Limited sampling model for the analysis of 5-fluorouracil pharmacokinetics in adjuvant chemotherapy for colorectal cancer. Clin Pharmacol Ther 2002; 72:627-637.
69. Bocci G, Danesi R, Di Paolo A, et al. Comparative pharmacokinetic analysis of 5-fluorouracil and its major metabolite 5-fluoro-5,6-dihydrouracil after conventional and reduced test dose in cancer patients. Clin Cancer Res 2000; 6:3032-3037.
70. Bocci G, Barbara C, Vannozzi F, et al. A pharmacokinetic-based test to prevent severe 5-fluorouracil toxicity. Clin Pharmacol Ther 2006; 80:384-395.
71. Diasio RB, Schuetz JD, Wallace HJ, et al. Dihydrofluorouracil, a fluorouracil catabolite with antitumor activity in murine and human cells. Cancer Res 1985; 45:4900-4903.
72. Yamashita K, Yada H, Ariyoshi T. Neurotoxic effects of alpha-fluoro-beta-alanine (FBAL) and fluoroacetic acid (FA) on dogs. J Toxicol Sci 2004; 29:155-166.
73. Chazal M, Etienne MC, Renee N, et al. Link between dihydropyrimidine dehydrogenase activity in peripheral blood mononuclear cells and liver. Clin Cancer Res 1996; 2:507-510.
74. Ho DH, Townsend L, Luna MA, et al. Distribution and inhibition of dihydrouracil dehydrogenase activities in human tissues using 5-fluorouracil as a substrate. Anticancer Res 1986; 6:781-784.
75. Van Kuilenburg AB, van Lenthe H, Blom MJ, et al. Profound variation in dihydropyrimidine dehydrogenase activity in human blood cells: major implications for the detection of partly deficient patients. Br J Cancer 1999; 79:620-626.
76. Stephan F, Etienne MC, Wallays C, et al. Depressed hepatic dihydropyrimidine dehydrogenase activity and fluorouracil-related toxicities. Am J Med 1995; 99:685-688.
77. Extermann M, Chen H, Cantor AB, et al. Predictors of tolerance to chemotherapy in older cancer patients: a prospective pilot study. Eur J Cancer 2002; 38:1466-1473.
78. Wallace KJ, Overcash C, Yoder J, et al. Influence of concomitant medications on toxicity from chemotherapy in elderly patients. Focus on cytochrome P-450 inhibition and protein binding effects. J Clin Oncol 2005; 23(16 suppl):735s (Abstract #8025).
79. Yamamoto N, Tamura T, Murakami H, et al. Randomized pharmacokinetic and pharmacodynamic study of docetaxel: dosing based on body-surface area compared with individualized dosing based on cytochrome P450 activity estimated using a urinary metabolite of exogenous cortisol. J Clin Oncol 2005; 23:1061-1069.
80. Voog E, Bienvenu J, Warzocha K, et al. Factors that predict chemotherapy-induced myelosuppression in lymphoma patients: role of the tumor necrosis factor ligand-receptor system. J Clin Oncol 2000; 18:325-331.
81. Intragumtornchai T, Sutheesophon J, Sutcharitchan P, et al. A predictive model for life-threatening neutropenia and febrile neutropenia after the first course of CHOP chemotherapy in patients with aggressive non-Hodgkin's lymphoma. Leuk Lymphoma 2000; 37:351-360.
82. Extermann M, Bonetti M, Sledge GW, et al. MAX2-a convenient index to estimate the average per patient risk for chemotherapy toxicity; validation in ECOG trials. Eur J Cancer 2004; 40:1193-1198.
83. Escoriaza J, Aldaz A, Calvo E, et al. Simple and sensitive determination of 5-fluorouracil in plasma by high-performance liquid chromatography. Application to clinical pharmacokinetic studies. J Chromatogr Biomed 1999; 736:97-102.
84. Beumer JH, Eiseman JL, Parise RA, et al. Pharmacokinetics, metabolism, and oral bioavailability of the DNA methyltransferase inhibitor 5-fluoro-2′-deoxycytidine in mice. Clin Cancer Res 2006; 12:7483-7491.
85. Nishimura M, Naito S. Tissue-specific mRNA expression profiles of human phase I metabolizing enzymes except for cytochrome P450 and phase II metabolizing enzymes. Drug Metab Pharmacokinet 2006; 21:357-374.
86. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER), Center for Veterinary Medicine (CVM). Guidance for Industry- Bioanalytical Method Validation, 2001. Available at: http://www.fda.gov/cder/guidance/ 4252fnl.pdf. Accessed ???
87. Beumer JH, Courtney JB, Stocker D, et al. 5-FU measurement by LC-MS/MS and stability in human blood and plasma. Clin Colorectal Cancer. [In press].
88. Wu R, McNally AJ, Salamone SJ. Synthesis of d-propoxyphene derivatives and the development of a microparticle-based immunoassay for the detection of propoxyphene and nor-propoxyphene. Bioconj Chem 1997; 8:385-390.
89. Li Z, Goc-Szkutnicka K, McNally AJ, et al. New synthesis and characterization of LSD derivatives and the development of a microparticle-based immunoassay for the detection of LSD and its metabolites. J Bioconj Chem 1997; 8:896-905.
90. McNally AJ, Pilcher I, Wu R, et al. Evaluation of the online immunoassay for propoxyphene: comparison to EMIT II and GC-MS. J Anal Toxicol 1996; 20:537-540.
91. Salamone SJ, Courtney JB, Stocker D. 5-Fluorouracil immunoassay. US patent pending, application 20060177884. August 10, 2006.