Thymidylate synthase inhibition after administration of fluorouracil with or without leucovorin in colon cancer patients: Implications for treatment with fluorouracil

Journal of Clinical Oncology

Volumn 12, Issue 10, 1994, Pages 2035-2042

  Peters, G J ^a   Van Der Wilt, C L ^a   Van Groeningen, C J ^a   Smid, K ^a   Meijer, S ^a   Pinedo, H M ^a  

^a VU UNIVERSITY MEDICAL CENTER   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

DEOXYURIDINE PHOSPHATE; FLOXURIDINE PHOSPHATE; FLUOROURACIL; FOLINIC ACID; METHYLENETETRAHYDROFOLIC ACID; TETRAHYDROFOLIC ACID; THYMIDYLATE SYNTHASE;

ADULT; ADVANCED CANCER; AGED; ARTICLE; CANCER ADJUVANT THERAPY; COLON CANCER; CONTROLLED STUDY; DRUG RESPONSE; ENZYME ACTIVITY; ENZYME INHIBITION; FEMALE; HEPATIC ARTERY; HUMAN; HUMAN TISSUE; INTRAARTERIAL DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; LAPAROTOMY; LIVER METASTASIS; MAJOR CLINICAL STUDY; MALE; PRIORITY JOURNAL; REGIONAL PERFUSION; TUMOR BIOPSY;

EID: 0028019880     PISSN: 0732183X     EISSN: None     Source Type: Journal    
DOI: 10.1200/JCO.1994.12.10.2035     Document Type: Article

References (38)

1. Peters GJ, Van Groeningen CJ: Clinical relevance of biochemical modulation of 5-fluorouracil. Ann Oncol 2:469-480, 1991
2. Pinedo HM, Peters GJ: 5-Fluorouracil: Biochemistry and pharmacology. J Clin Oncol 6:1653-1664, 1988
3. Danenberg PV: Thymidylate synthetase - A target enzyme in cancer chemotherapy. Biochim Biophys Acta 473:73-92, 1977
4. Bapat AR, Zarov C, Danenberg PV: Human leukemic cells resistant to 5-fluoro-2′deoxyuridine contain a thymidylate synthase with lower affinity for nucleotides. J Biol Chem 258:4130-4136, 1983
5. Radparvar S, Houghton PJ, Houghton JA: Characteristics of thymidylate synthase purified from a human adenocarcinoma. Arch Biochem Biophys 260:342-350, 1988
6. Houghton JA, Williams LG, Radparvar S, et al: Characterization of the pools of 5,10-methylenetetrahydrofolales and tetrahydrofolates in xenografts of human colon adenocarcinoma. Cancer Res 48:3062-3069, 1988
7. Yin MB, Zakrzewski SF, Hakala MT: Relationship of cellular folate cofactor pools to the activity of 5-fluorouracil. Mol Pharmacol 23:190-197, 1983
8. Spears CP, Gustavsson BG, Berne M, et al: Mechanisms of innate resistance to thymidylate synthase inhibition after 5-fluorouracil. Cancer Res 48:5894-5900, 1988
9. Priest DG, Ledford SE, Doig MT: Increased thymidylate synthetase in 5-fluorodeoxyuridine resistant cultured hepatoma cells. Biochem Pharmacol 29:1549-1553, 1980
10. Berger SH, Barbour KW, Berger FG: A naturally occurring variation in thymidylate synthase structure is associated with a reduced response to 5-fluoro-2′-deoxyuridine in a human colon tumor cell line. Mol Pharmacol 34:480-484, 1988
11. Berger SH, Jenh CH, Johnson LF, et al: Thymidylate synthase overproduction and gene amplification in fluorodeoxyuridine-resistant human cells. Mol Pharmacol 28:461-467, 1985
12. Jenh CH, Geyer PK, Baskin F, et al: Thymidylate synthase gene amplification in fluorodeoxyuridine-resistant mouse cell lines. Mol Pharmacol 28:80-85, 1985
13. Van der Wilt CL, Pinedo HM, Smid K, et al: Elevation of thymidylate synthase following 5-fluorouracil treatment is prevented by addition of leucovorin in murine colon tumors. Cancer Res 52:4922-4928, 1992
14. Clark JL, Berger SH, Mittelman A, et al: Thymidylate synthase overproduction gene amplification in a colon tumor resistant to fluoropyrimidine chemotherapy. Cancer Treat Rep 71:261-265, 1987
15. Swain SM, Lippman ME, Egan EF, et al: Fluorouracil and high-dose leucovorin in previously treated patients with metastatic breast cancer. J Clin Oncol 7:890-899, 1989
16. Martin DS: Biochemical modulation: perspectives and objectives, in Harrap K, Connors T (eds): New Avenues in Developmental Cancer Chemotherapy. London, England, Academic, 1987, pp 113-161
17. Nord LD, Stolfi RL, Martin DS: Biochemical modulation of 5-fluorouracil with leucovorin or delayed uridine rescue. Biochem Pharmacol 44:2543-2549, 1993
18. Aschele C, Sobrero A, Faderan MA, et al: 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 52:1855-1864, 1992
19. Sobrero AF, Aschele C, Guglielmi AP, et al: Synergism and lack of cross-resistance between short-term and continuous exposure to fluorouracil in human colon adenocarcinoma cells. J Natl Cancer Inst 85:1937-1944, 1993
20. Peters GJ, Laurensse E, Leyva A, et al: Sensitivity of human, murine and rat cells to 5-fluorouracil and 5′-deoxy-5-fluorouridine in relation to drug-metabolizing enzymes. Cancer Res 46:20-28, 1986
21. Peters GJ, Lankelma J, Kok RM, et al: Long retention of high concentrations of 5-fluorouracil in human and murine tumors compared to plasma. Cancer Chemother Pharmacol 31:269-276, 1993
22. Spears CP, Gustavsson BG, Mitchell MS, et al: Thymidylate synthase inhibition in malignant tumors and normal liver of patients given intravenous 5-fluorouracil. Cancer Res 44:4144-4150, 1984
23. Trave F, Rustum YM, Petrelli NJ, et al: Plasma and tumor tissue pharmacology of high-dose intravenous leucovorin calcium in combination with fluorouracil in patients with advanced colorectal carcinoma. J Clin Oncol 6:1184-1191, 1988
24. Peters GJ, Van Groeningen CJ, Laurensse EJ, et al: Thymidylate synthase from untreated human colorectal cancer and colonic mucosa; Enzyme activity and inhibition by 5-fluoro-2′-deoxyuridine-5′-monophosphate. Eur J Cancer 27:263-267, 1991
25. Peters GJ, Laurensse E, Leyva A, et al: Tissue homogenization using a microdismembrator for the measurement of enzyme activities. Clin Chim Acta 158:193-198, 1986
26. Spears CP, Shahinian AH, Moran RG, et al: In vivo kinetics of thymidylate synthase inhibition in 5-fluorouracil-sensitive and -resistant murine colon adenocarcinomas. Cancer Res 42:450-456, 1982
27. Houghton JA, Radparvar S, Torrance PM, et al: Determination of thymidylate synthase activity in colon tumor tissues after treatment with 5-fluorouracil. Biochem Pharmacol 36:1285-1289, 1987
28. Fernandes DJ, Cranford SK: A method for the determination of total, free and 5-fluorouridylate-bound thymidylate synthase in cell extracts. Anal Biochem 142:378-385, 1984
29. Van Groeningen CJ. New technical developments in antineoplastic drug delivery and their role in cancer treatment, in Domellöf L (ed): Drug Delivery in Cancer Treatment. ESO Monographs. Berlin, Germany, Springer Verlag, 1987, pp 39-45
30. Chu E, Koeller DM, Johnston PG, et al: Regulation of thymidylate synthase in human colon cancer cells treated with 5-fluorouracil and interferon-γ. Mol Pharmacol 43:527-533, 1993
31. Spears CP, Gustavsson G, Frosing R: Folinic acid modulation of 5-fluorouracil kinetics at bolus administration. Invest New Drugs 7:27-36, 1989
32. Mini E, Trave F, Rustum YM, et al: Enhancement of the antitumor effects of 5-fluorouracil by folinic acid. Pharmacol Ther 47:1-19, 1990
33. Nadal JC, Van Groeningen CJ, Pinedo HM, et al: Schedule-dependency of in vivo modulation of 5-fluorouracil by leucovorin and uridine in murine colon carcinoma. Invest New Drugs 7:163-172, 1989
34. Peters GJ, Codacci-Pisanelli G, Van der Wilt CL, et al: Comparison of continuous infusions and bolus injections of 5-fluorouracil with or without leucovorin; Implications for inhibition of thymidylate synthase, in Rustum YM (ed): Novel Approaches to Selective Treatments of Human Solid Tumors: Laboratory and Clinical Correlation. New York, NY, Plenum, 1993, pp 9-20
35. Freemantle SJ, Aherne GW, Hardcastle A, et al: Increases in thymidylate synthase protein levels measured using newly developed antibodies. Proc Am Assoc Cancer Res 32:360, 1991 (abstr 2138)
36. Johnston PG, Fisher E, Rockette HE, et al: Thymidylate synthase expression is an independent predictor of survival/disease free survival in patients with rectal cancer. Proc Am Soc Clin Oncol 12:202, 1993 (abstr 599)
37. Horikoshi T, Danenberg KD, Stadlbauer THW, et al: Quantitation of thymidylate synthase, dihydrofolate reductase, and DT-diaphorase gene expression in human tumors using the polymerase chain reaction (PCR). Cancer Res 52:108-116, 1991
38. Lenz HJ, Leichman C, Danenberg P, et al: Thymidylate synthase (TS) gene expression predicts response of primary gastric cancer (GC) to 5-fluorouracil (5FU)-leucovorin (LV)-cisplatin (DDP). Proc Am Soc Clin Oncol 12:199, 1993 (abstr 585)