Pharmacokinetics of (6S)-leucovorin and 5-methyltetrahydrofolate after 4-hour continuous intravenous infusion followed by repeated oral doses of (6S)-leucovorin in patients with colorectal cancer treated with 5-fluorouracil

Clinical Drug Investigation

Volumn 12, Issue 1, 1996, Pages 39-45

  Vannozzi, Maria O ^a   Nobile, Maria T ^a   Sanguineti, Ornella ^a   Barzacchi, Cristina ^a   Viale, Maurizio ^a   Numico, Gianmauro ^a   Esposito, Mauro ^a  

^a UNIVERSITY OF GENOA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

5 METHYLTETRAHYDROFOLIC ACID; FLUOROPYRIMIDINE; FLUOROURACIL; FOLINIC ACID;

ADULT; AGED; AREA UNDER THE CURVE; ARTICLE; CLINICAL ARTICLE; CLINICAL PROTOCOL; CLINICAL TRIAL; COLORECTAL CANCER; COLORECTAL CARCINOMA; CONTINUOUS INFUSION; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG CYTOTOXICITY; FEMALE; HUMAN; INTRAVENOUS DRUG ADMINISTRATION; MALE; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL;

EID: 0029775078     PISSN: 11732563     EISSN: None     Source Type: Journal    
DOI: 10.2165/00044011-199612010-00005     Document Type: Article

References (23)

1. Arbuck SG. Overview of clinical trials using 5-fluorouracil and leucovorin for the treatment of colorectal cancer. Cancer 1989; 63 Suppl. 6: 1036-44
2. 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 (10): 1407-18
3. Doroshow JH, Multhauf P, Leong L, et al. Prospective randomized comparison of fluorouracil versus fluorouracil and high-dose continuous infusion leucovorin calcium for the treatment of advanced measurable colorectal cancer in patients previously unexposed to chemotherapy. J Clin Oncol 1990; 8 (3): 491-501
4. Lockshin A, Danenberg PV. Biochemical factors affecting the tightness of 5-fluorodeoxyuridylate binding to human thymidy late synthetase. Biochem Pharmacol 1981; 30 (3): 247-57
5. Cohen SS, Flaks JG, Barser HD, et al. The mode of action of 5-fluorouracil and its derivates. Proc Natl Acad Sci USA 1958; 44: 1004-12
6. Zittoun J. Pharmacokinetics and in vitro studies of 1-leucovorin. Comparison with the d and d,1-leucovorin. Ann Oncol 1993; 4 Suppl. 2: 1-5
7. Machover D, Goldschmidt E, Chollet P, et al. Treatment of advanced colorectal and gastric adenocarcinomas with 5-fluorouracil and high-dose folinic acid. J Clin Oncol 1986; 4 (5): 685-96
8. Straw JA, Newman EM, Doroshow JH. Pharmacokinetics of leucovorin (D,L-5-formyltetrahydrofolate) after intravenous injection and constant intravenous infusion. NCI Monogr 1987; 5: 41-5 (NIH Publication No. 87-2901)
9. Voeller DM, Allegra CJ. Intracellular metabolism of 5-methyltetrahydrofolate and 5-formyltetrahydrofolate in a human breast-cancer line. Cancer Chemother Pharmacol 1994; 34 (6): 491-6
10. Evans RM, Laskin JD, Hakala MT. Effect of excess folates and deoxinosine on the activity and site of action of 5-fluorouracil. Cancer Res 1981; 41 (9): 3288-95
11. Keyomarsi K, Moran RG. Folinic acid augmentation of the effects of fluoropyrimidines on murine and human leukemic cells. Cancer Res 1986; 46 (10): 5229-35
12. Chang Y-M, Bertino JR. Enhancement of fluoropyrimidine inhibition of cell growth by leucovorin and deoxynucleosides in a human squamous cell carcinoma cell line. Cancer Invest 1989; 7 (6): 557-63
13. Moran RG, Scanlon KL. Schedule-dependent enhancement of cytotoxicity of fluoropyrimidines to human carcinoma cells in the presence of folic acid. Cancer Res 1991; 51 (17): 4618-23
14. Drake JC, Voeller DM, Allegra CJ, et al. The effect of dose and interval between 5-fluorouracil and leucovorin on the formation of thymidylate synthase ternary complex in human cancer cells. Br J Cancer 1995; 71 (6): 1145-50
15. Newman EM, Akman SA, Harrison JS, et al. Pharmacokinetics and toxicity of continuous infusion (6S)-folinic acid and bolus 5-fluorouracil in patients with advanced cancer. Cancer Res 1992; 52 (9): 2408-12
16. Schilsky RL, Ratain MJ. Clinical pharmacokinetics of high-dose leucovorin calcium after intravenous and oral administration. J Natl Cancer Inst 1990; 82(17): 1411-5
17. Gibaldi M, Perrier D, editors. Pharmacokinetics. 2nd ed. New York: Marcel Dekker, 1982
18. Machover D, Grison X, Goldschmidt E, et al. Flourouracil combined with pure (6S)-stereoisomer of folinic acid in high doses for treatment of patients with advanced colorectal carcinoma: a phase I-II study. J Natl Cancer Inst 1992; 84 (5): 321-7
19. Nixon PF, Bertino JR. Effective absorption and utilization of oral formyltetrahydrofolate in man. N Engl J Med 1972; 286 (4): 175-9
20. Whitehead VM, Pratt R, Viallet A, et al. Intestinal conversion of folinic acid to 5-methyltetrahydrofolate in man. Br J Haematol 1972; 22 (1): 63-72
21. Mini E, Mazzei T, Coronnello M, et al. Effects of 5-methyltetrahydrofolate on the activity of fluoropyrimidines against human leukemia (CCRF-CEM) cells. Biochem Pharmacol 1987; 36 (18): 2905-11
22. Houghton JA, Williams LG, de Graaf SSN, et al. Comparison of the conversion of 5-formyltetrahydrofolate and 5-methyltetrahydrofolate to 5,10-methylenetetrahydrofolates and tetrahydrofolates in human colon tumors. Cancer Comm 1989; 1 (3): 167-74
23. Hougton JA, Williams LG, de Graaf SSN, et al. Relationship between dose rate of [6R,S]leucovorin administration, plasma concentrations of reduced folates, and pools of 5,10-methylene-tetrahydrofolates and tetrahydrofolates in human colon adenocarcinoma xenografts. Cancer Res 1990; 50 (12): 3493-502