Clinical pharmacokinetics of 5-fluorouracil with consideration of chronopharmacokinetics

REFERENCES

• Heidelberger C., Chandhuari N.K., Danenberg P. Fluorinated Pyrimidines: A New Class of Tumor Inhibitor Compounds. Nature 1957; 79: 663–666
   Google Scholar
• Rutman R.J., Cantarow A., Paschkis D.I. Studies on 2-Acetylaminofluorene Carcinogenesis: III. The Utilization of Uracil-2-C14 by Pre-Neoplastic Rat Liver. Cancer Res. 1954; 14: 119–126
   PubMed Web of Science ®Google Scholar
• Grem J.L. Fluorinated Pyrimidine. Cancer Chemotherapy: Principles and Practice, B.A. Chabner, J.M. Collins. JB Lippincott Co., Philadelphia 1990; 149–212
   Google Scholar
• Diasio R.B., Harris B.E. Clinical Pharmacology of 5-Fluorouracil. Clin. Pharmacokinet. 1989; 16: 215–237
   PubMed Web of Science ®Google Scholar
• Parker W.B., Cheng Y.C. Metabolism and Mechanism of Action 5-Fluorouracil. Pharm. Ther. 1990; 48: 381–395
   PubMed Web of Science ®Google Scholar
• Reichard P., Sköld O., Klein G. Studies on Resistance Against 5-Fluorouracil. Enzymes of the Uracil Pathway During Development of Resistance. Cancer Res. 1962; 22: 235–243
   PubMedGoogle Scholar
• Ardalan B., Cooney D.A., Jayaram H.N., Carrico C.K., Glazer R.I., Macdonald J., Schein P.S. Mechanism of Sensitivity and Resistance of Murine Tumors to 5-Fluorouracil. Cancer Res. 1980; 40: 1431–1437
   PubMedGoogle Scholar
• Houghton J.A., Maroda S.J., Phillips J.O., Houghton P.J. Biochemical Determinants of Responsiveness to 5-Fluorouracil and Its Derivatives in Xenografts of Human Colorectal Adenocarcinoma in Mice. Cancer Res. 1981; 41: 144–149
   PubMed Web of Science ®Google Scholar
• Mulkins M.A., Heidelberg C. Biochemical Characterization of Fluoropyrimidine-Resistant Murine Leukemic Cell Lines. Cancer Res. 1982; 42: 965–972
   PubMed Web of Science ®Google Scholar
• Wang F.S., Aschele C., Sobrero A., Chang Y.M., Bertino J.R. Decreased Folylpolyglutamate Synthetase Expression: A Novel Mechanism of Fluorouracil Resistance. Cancer Res. 1993; 53: 3677–3680
   PubMedGoogle Scholar
• Clark J.L., Berger S.H., Mittelman A., Berger F.G. Thymidylate Synthase Gene Amplification in a Colon Tumor Resistant to Fluoropyrimidine Chemotherapy. Cancer Treat. Rep. 1987; 71: 261–265
   PubMedGoogle Scholar
• Johnston P.G., Fischer E., Rockette H.E. Thymidylate Synthase Expression is an Independent Predictor of Survival/Disease Free Survival in Patients with Rectal Cancer. Proc. Am. Soc. Clin. Oncol. 1993; 202: 599
   Google Scholar
• Johnston P.G., Lenz H.J., Leichman C.G., Florentine B., Johnston P.G., Groshen S., Zhou L., Xiong Y.P., Danenberg P.V., Leichman P.L. Thymidylate Synthase Gene and Protein Expression Correlate and Are Associated with Response to 5-Fluorouracil in Human Colorectal and Gastric Tumors. Cancer Res. 1995; 55: 1407–1412
   PubMed Web of Science ®Google Scholar
• Aschele C., Debernardis D., Casazza S., Antonelli G., Tunesi G., Baldo C., Lionetto R., Maley F., Sobrero A. Immunohistochemical Quantification of Thymidylate Synthase Expression in Colorectal Cancer Metastases Predicts for Clinical Outcome to Fluorouracil-Based Chemotherapy. J. Clin. Oncol. 1999; 17: 1760–1770
   PubMed Web of Science ®Google Scholar
• Peters G.J., Laurensse E., Leyva A., Lankelma J., Pinedo H.M. Sensitivity of Human, Murine, and Rats Cells to 5-Fluorouracil and 5′-Deoxy-5-fluorouridine in Relation to Drug-Metabolizing Enzymes. Cancer Res. 1986; 46: 20–28
   PubMed Web of Science ®Google Scholar
• Aiba K., Allegra C., Park J. Multifactorial Resistance of 5-Fluorouracil in Human Colon Cancer Cell Lines. Proc. AACR 1990; 31: 424
   Google Scholar
• Aschele C., Sobrero A., Faderan M.A., Bertino J.R. Novel Mechanism (s) of Resistance to 5-Fluorouracil in Human Colon Cancer (HCT-8) Sublines Following Exposure to Two Different Clinically Relevant Dose Schedules. Cancer Res. 1992; 52: 1855–1864
   PubMed Web of Science ®Google Scholar
• Naguib F.N.M., El Kouni A.M., Cha S. Enzymes of Uracil Catabolism in Normal and Neoplastic Human Tissues. Cancer Res. 1985; 45: 5404–5412
   Google Scholar
• Beck A., Etienne M.C., Chéradame S., Fischel J.L., Formento P., Renée N., Milano G. A Role of Dihydropyrimidine Dehydrogenase and Thymidylate Synthase in Tumor Sensitivity to Fluorouracil. Eur. J. Cancer 1994; 30: 1517–1522
   Google Scholar
• Poon M.A., O'Connell M.J., Weiland H.S., Krook J.E., Gerstner J.B., Tschetter L.K., Levitt R., Kardinal C.G., Mailliard J.A. Biochemical Modulation of Fluorouracil with Leucovorin. Confirmatory Evidence of Improved Therapeutic Efficacy in Advanced Colorectal Cancer. J. Clin. Oncol. 1991; 9: 1967–1972
   PubMed Web of Science ®Google Scholar
• Douillard J.Y., Cunningham D., Roth A.D., Navarro M., James R.D., Karasek P., Jandik P., Iveson T., Carmichael J., Alakl M., Gruia G., Awad L., Rougier P. Irinotecan Combined with Fluorouracil Compared with Fluorouracil Alone as First-Line Treatment for Metastatic Colorectal Cancer: a Multicenter Randomised Trial. Lancet 2000; 355: 1041–1047
   PubMed Web of Science ®Google Scholar
• Giacchetti S., Perpoint B., Zidani R., Le Bail N., Faggiuolo R., Focan C., Chollet P., Llory J.F., Letourneau Y., Coudert B., Bertheaut-Cvitkovic F., Larregain-Fournier D., Le Rol A., Walter S., Adam R., Misset J.L., Levi F. Phase III Multicenter Randomized Trial of Oxaliplatin Added to Chronomodulated Fluorouracil–Leucovorin as First-Line Treatment of Metastatic Colorectal Cancer. J. Clin. Oncol. 2000; 18: 136–147
   PubMed Web of Science ®Google Scholar
• Fraile R.J., Baker L.H., Buroker T.R., Horwitz J., Vaitkevicius V.K. Pharmacokinetics of 5-Fluorouracil Administered Orally, by Rapid Intravenous and by Slow Infusion. Cancer Res. 1980; 40: 2223–2228
   PubMed Web of Science ®Google Scholar
• Almersjo C.E., Gustavsson B.G., Regardh C.G., Wahlen P. Pharmacokinetics Studies of 5-Fluorouracil After Oral and Intravenous Administration in Man. Acta Pharmacol. Toxicol. 1980; 46: 329–336
   PubMedGoogle Scholar
• Borner M.M., Kneer J., Crevoisier C., Brunner K.W., Cerny T. Bioavailability and Feasibility of Subcutaneous 5-Fluorouracil. Br. J. Cancer 1993; 68: 537–539
   PubMedGoogle Scholar
• Erlanger M., Martz G., Ott F., Storck H., Rieder J., Kessler S. Cutaneous Absorption and Urinary Excretion of 6-14C-5-Fluorouracil Ointment Applied to Healthy and Diseased Human Skin. Dermatology 1970; 140((suppl. 1))7–14
   Google Scholar
• Drewinko B., Yang L.Y. Cellular Basis for the Inefficacy of 5-FU in Human Colon Carcinoma. Cancer Treat. Rep. 1985; 69: 1391–1398
   PubMedGoogle Scholar
• Hansen R.M., Ryan L., Anderson T., Krzywda B., Quebbeman E., Benson A., 3rd, Haller D.G., Tormey D.C. Phase III Study of Bolus Versus Infusion Fluorouracil with or without Cisplatin in Advanced Colorectal Cancer. J. Natl Cancer Inst. 1996; 88: 668–674
   PubMed Web of Science ®Google Scholar
• Efficacy of Intravenous Continuous Infusion of Fluorouracil Compared with Bolus Administration in Advanced Colorectal Cancer. J. Clin. Oncol. 1998; 16: 301–308
   PubMed Web of Science ®Google Scholar
• Van Groeningen C.J., Pinedo H.M., Heddes J., Kok R.M., de Jong A.P., Wattel E., Peters G.J., Lankelma J. Pharmacokinetics of 5-Fluorouracil Assessed with a Sensitive Mass Spectrometric Method in Patients on a Dose Escalation Schedule. Cancer Res. 1988; 48: 6956–6961
   PubMed Web of Science ®Google Scholar
• Spicer D.V., Ardalan B., Daniels J.R., Silberman H., Johnson K. Reevaluation of the Maximum Tolerated Dose of Continuous Venous Infusion of 5-Fluorouracil with Pharmacokinetics. Cancer Res. 1988; 48: 459–461
   PubMed Web of Science ®Google Scholar
• Erlichman C., Fine S., Elhakim T. Plasma Pharmacokinetics of 5-FU Given by Continuous Infusion with Allopurinol. Cancer Treat. Rep. 1986; 70: 903–904
   PubMedGoogle Scholar
• Fleming R.A., Milano G., Etienne M.C., Renee N., Thyss A., Schneider M., Demard F. No Effect of Dose, Hepatic Function or Nutritional Status on 5-FU Clearance Following Continuous (5-day) 5-FU Infusion. Br. J. Cancer 1992; 66: 668–672
   PubMed Web of Science ®Google Scholar
• Ratain M.J., Shilsky R.L., Conley B.A., Egorin M.J. Pharmacodynamics in Cancer Therapy. J. Clin. Oncol. 1990; 8: 1739–1753
   PubMed Web of Science ®Google Scholar
• Au J.L.S., Rustum Y.M., Lederma E.J., Mittelman A., Creaven P.J. Clinical Pharmacological Studies of Concurrent Infusion of 5-Fluorouracil and Thymidine in the Treatment of Colorectal Carcinoma. Cancer Res. 1982; 42: 2930–2937
   PubMedGoogle Scholar
• Thyss A., Milano G., Renée N., Vallicioni J., Schneider M., Demard F. Clinical Pharmacokinetic Study of 5-FU in Continuous 5-day Infusions for Head and Neck Cancer. Cancer Chemother. Pharmacol. 1986; 16: 64–66
   PubMed Web of Science ®Google Scholar
• Vokes E.E., Mick R., Kies M.S., Dolan M.E., Malone D., Athanasiadis I., Haraf D.J., Kozloff M., Weichselbaum R.R., Ratain M.J. Pharmacodynamics of Fluorouracil-Based Induction Chemotherapy in Advanced Head and Neck Cancer. J. Clin. Oncol. 1996; 14: 1663–1671
   PubMed Web of Science ®Google Scholar
• Yoshida T., Araki E., Ligo M., Fujii T., Yoshino M., Shimada Y., Saito D., Tajiri H., Yamaguchi H., Yoshida S., 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
   PubMed Web of Science ®Google Scholar
• Trump D.L., Egorin M.J., Forrest A., Willson J.K., Remick S., Tutsch K.D. Pharmacokinetics and Pharmacodynamics Analysis of Fluorouracil During 72-Hour Continuous Infusion with and without Dipyridamole. J. Clin. Oncol. 1991; 9: 2027–2035
   PubMedGoogle Scholar
• Hillcoat B.L., Mc Culloch P.B., Figueredo A.T., Ehsan M.H., Rosenfeld J.M. Clinical Response and Plasma Levels of 5-Fluorouracil in Patients with Colonic Cancer Treated by Drug Infusion. Br. J. Cancer 1978; 38: 719–724
   PubMed Web of Science ®Google Scholar
• Milano G., Etienne M.C., Renée N., Thyss A., Schneider M., Ramaioli A., Demard F. Relationship Between Fluorouracil Systemic Exposure and Tumor Response and Patient Survival. J. Clin. Oncol. 1994; 12: 1291–1295
   PubMed Web of Science ®Google Scholar
• Presant C.A., Wolf W., Waluch V., Wiseman C., Kennedy P., Blayney D., Brechner R.R. Association of Intratumoral Pharmacokinetics of Fluorouracil with Clinical Response. Lancet 1994; 343: 1184–1187
   PubMed Web of Science ®Google Scholar
• Gamelin E., Boisdron-Celle M., Delva R., Regimbeau C., Cailleux P.E., Alleaume C., Maillet M.L., Goudier M.J., Sire M., Person-Joly M.C., Maigre M., Maillart P., Fety R., Burtin P., Lortholary A., Dumesnil Y., Picon L., Geslin J., Gesta P., Danquechin-Dorval E., Larra F., Robert J. Long-Term Weekly Treatment of Colorectal Metastatic Cancer with Fluorouracil and Leucovorin: Results of a Multicentric Prospective Trial with Fluorouracil Dosage Optimization by Pharmacokinetic Monitoring in 152 Patients. J. Clin. Oncol. 1998; 16: 1470–1478
   PubMed Web of Science ®Google Scholar
• Gamelin E., Danquechim-Dorval E.M., Dunesnil Y.F., Maillart P.J., Goudier M.J., Burtin P.C., Delva R.G., Lortholary A.H., Gesta P.H., Larra F.G. Relationship Between 5-Fluorouracil Dose Intensity and Therapeutic Response in Patients with Advanced Colorectal Cancer Receiving Infusional Therapy Containing 5-FU. Cancer 1996; 77: 441–451
   PubMed Web of Science ®Google Scholar
• Ensminger W.D., Rosowsky A., Raso V., Levin D.C., Glode M., Come S., Steele G., Frei E., 3rd. A Clinical–Pharmacological Evaluation of Hepatic Arterial Infusions of 5-Fluoro-2′Deoxyuridine and 5-Fluorouracil. Cancer Res. 1978; 38: 3784–3792
   PubMed Web of Science ®Google Scholar
• Nowakowska-Dulawa E. Circadian Rhythm of 5-Fluorouracil and Pharmacokinetics and Tolerance. Chronobiologia 1990; 17: 27–30
   PubMedGoogle Scholar
• Krishnaswamy K. Drug Metabolism and Pharmacokinetics in Malnutrition. Clin. Pharmacokinet. 1978; 3: 216–221
   PubMed Web of Science ®Google Scholar
• Floyd R.A., Hornbeck C.L., Byfield J.E. Clearance of Continuously Infused 5-Fluorouracil in Adults Having Lung or Gastrointestinal Carcinoma With or Without Hepatic Metastases. Drug Intell. Clin. Pharm. 1982; 16: 665–669
   PubMedGoogle Scholar
• Breimer D.D. Variability in Human Drug Metabolism and Its Implications. Int. J. Clin. Pharmacol. Res. 1983; 3: 399–413
   PubMedGoogle Scholar
• Milano G., Etienne M.C., Cassuto-Viguier E., Thyss A., Santini J., Frenay M., Renee N., Schneider M., Demard F. Influence of Sex and Age on Fluorouracil Clearance. J. Clin. Oncol. 1992; 10: 1171–1175
   PubMed Web of Science ®Google Scholar
• Vokes E.E., Ratain M.J., Mick R., McEvilly J.M., Haraf D., Kozloff M., Hamasaki V., Weichselbaum R.R., Panje W.R., Wenig B. Cisplatin, Fluorouracil and Leucovorin Augmented by Interferon Alfa-2b in Head and Neck Cancer. A Clinical and Pharmacologic Analysis. J. Clin. Oncol. 1993; 11: 360–368
   PubMedGoogle Scholar
• Chazal M., Etienne M.C., Renée N., Bourgeon A., Richelme H., Milano G. Link Between Dihydropyrimidine Dehydrogenase Activity in Peripheral Blood Mononuclear Cells and Liver. Clin. Cancer Res. 1996; 2: 507–510
   PubMed Web of Science ®Google Scholar
• Fleming R.A., Milano G., Thyss A., Etienne M.C., Renee N., Schneider M., Demard F. Correlation Between Dihydropyrimidine Dehydrogenase Activity in Peripheral Mononuclear Cells and Systemic Clearance of Fluorouracil in Cancer Patients. Cancer Res. 1992; 52: 2899–2902
   PubMed Web of Science ®Google Scholar
• Etienne M.C., Lagrange J.L., Dassonville O., Fleming R., Thyss A., Renee N., Schneider M., Demard F., Milano G. Population Study of Dihydropyrimidine Dehydrogenase in Cancer Patients. J. Clin. Oncol. 1994; 12: 2248–2253
   PubMed Web of Science ®Google Scholar
• Etienne M.C., Chatelut E., Pivot X., Lavit M., Pujol A., Canal P., Milano G. Co-variables Influencing 5-Fluorouracil Clearance During Continuous Venous Infusion. A NONNEM analysis. Eur. J. Cancer 1998; 34: 92–97
   PubMed Web of Science ®Google Scholar
• Mc Leod H.L., Sludden J., Hardy S.C., Lock R.E., Hawksworth G.M., Cassidy J. Autoregulation of 5-Fluorouracil Metabolism. Eur. J. Cancer 1998; 34: 1623–1627
   PubMedGoogle Scholar
• Harris B.E., Song R., He Y.J., Soong S.J., Diasio R.B. Circadian Rhythm of Rat Liver Dihydropyrimidine Dehydrogenase. Possible Relevance to Fluoropyrimidine Chemotherapy. Biochem. Pharmacol. 1988; 37: 4759–4762
   PubMed Web of Science ®Google Scholar
• Harris B.E., Song R., Soong S.J., Diasio R.B. 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. 1990; 50: 197–201
   PubMed Web of Science ®Google Scholar
• Petit E., Milano G., Levi F., Thyss A., Bailleul F., Schneider M. Circadian Rhythm-Varying Plasma Concentration of 5-Fluourouracil During a Five-Day Continuous Venous Infusion at a Constant Rate in Cancer Patients. Cancer Res. 1988; 48: 1676–1679
   PubMed Web of Science ®Google Scholar
• Tuchman M., Von Roemeling R., Lanning R.M., Sothern R.B., Hrushesky W.J.M. Sources of Variability of Dihydropyrimidine Dehydrogenase Activity in Human Blood Mononuclear Cells. Annu Rev. Chronopharmacol. 1988; 5: 399–402
   Google Scholar
• Grem J.L., Yee L.K., Venzon D.J., Takimoto C.H., Allegra C.J. Inter- and Intraindividual Variation in Dihydropyrimidine Dehydrogenase Activity in Peripheral Blood Mononuclear Cells. Cancer Chemother. Pharmacol. 1997; 40: 117–125
   PubMed Web of Science ®Google Scholar
• Levi F. Chronopharmacology of Anticancer Agents. Physiology and Pharmacology of Biological Rhythms, P.H. Redfern, B. Lemmer. Springer, Berlin 1997; 300–331
   Google Scholar
• Smaaland R., Lacrum O.D., Sothern R.B., Sletvold O., Bjerknes R., Lote K. Colony-Forming Unit-Granulocyte-Macrophage and DNA Synthesis of Human Bone Marrow are Circadian Stage-Dependent and Show Correlation. Blood 1992; 79: 2281–2287
   PubMed Web of Science ®Google Scholar
• Warnakulasuriya K.A., Mac Donald D.G. Diurnal Variation in Labeling Index in Human Buccal Epithelium. Arch. Oral Biol. 1993; 38: 1107–1111
   PubMed Web of Science ®Google Scholar
• Levi F.A., Zidani R., Vannetzel J.M., Perpoint B., Focan C., Faggiuolo R., Chollet P., Garufi C., Itzhaki M., Dogliotti L. Chronomodulated Versus Fixed-Infusion-Rate Delivery of Ambulatory Chemotherapy with Oxaliplatin, Fluorouracil, and Folinic Acid (Leucovorin) in Patients with Colorectal Cancer Metastases: a Randomized Multi-Institutional Trial. J. Natl Cancer Inst. 1994; 86: 1608–1617
   PubMed Web of Science ®Google Scholar