Pharmacokinetics and bioequivalence of a combined oral formulation of eniluracil, an inactivator of dihydropyrimidine dehydrogenase, and 5-fluorouracil in patients with advanced solid malignancies

Annals of Oncology

Volumn 11, Issue 10, 2000, Pages 1313-1322

  Ochoa, L ^a   Hurwitz, H I ^b   Wilding, G ^c   Cohen, D ^b   Thomas, J P ^c   Schwartz, G ^d   Monroe, P ^a   Petros, W P ^b   Ertel, V Ph ^e   Hsieh, A ^e   Hoffman, C ^e   Drengler, R ^a   Magnum, S ^e   Rowinsky, E K ^a  

^a CTRC Institute for Drug Development   (United States)

^b DUKE UNIVERSITY MEDICAL CENTER   (United States)

^c University of Wisconsin   (United States)

^d BROOKE ARMY MEDICAL CENTER   (United States)

^e GLAXOSMITHKLINE   (United States)

Author keywords

5 Fluorouracil; 776C85; Bioequivalence; Dihydropyrimidine dehydrogenase inhibitor; Eniluracil; Pharmacokinetics

Indexed keywords

5 ETHYNYLURACIL; ALPHA FLUORO BETA ALANINE; DIHYDROPYRIMIDINE DEHYDROGENASE; ENZYME INHIBITOR; FLUOROURACIL; URACIL;

ADULT; ADVANCED CANCER; AGED; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CLINICAL ARTICLE; CLINICAL TRIAL; CONSTIPATION; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DISTRIBUTION VOLUME; DRUG CLEARANCE; DRUG FORMULATION; DRUG HALF LIFE; DRUG TOLERABILITY; DYSPNEA; FEMALE; HUMAN; MALAISE; MALE; MUCOSA INFLAMMATION; NAUSEA; NEUTROPENIA; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SOLID TUMOR; URINARY EXCRETION; VOMITING;

EID: 0033758470     PISSN: 09237534     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1008379802642     Document Type: Article

References (26)

1. Fluorouracil in colorectal cancer - A tale of two drugs: Implications for biochemical modulation
2. Hepatic arterial chemotherapy for metastatic colorectal carcinoma
3. Clinical pharmacology of 5-fluorouracil
4. Phase II study of fluorouracil and its modulation in advanced colorectal cancer: A Southwest Oncology Group study
5. Meta-analysis of all trials comparing intraveous bolus administration to continuous infusion of 5-fluorouracil in patients will advanced colorectal cancer
6. Dihydropyrimidine dehydrogenase activity in cancer patients
7. Population study of dihydropyrimidine dehydrogenase in cancer patients
8. Biochemical basis for circadian-dependent metabolism of fluoropyrimidines
9. Human polymorphism in drug metabolism: Mutation in the dihydropyrimidine dehydrogenase gene results in exon skipping and thymine uracilurea
10. Response to fluorouracil therapy in cancer patients: The role of tumoral dihydropyrimidine dehydrogenase activity
11. Experimental neurotoxicity of 5-fluorouracil and its derivatives is due to poisoning by the monofluorinated organic metabolites, monofluoroacetic acid and alpha-fluoro-beta-alanine
12. Pharmacokinetics and tissue distribution of 2-fluoro-beta-alanine in rats. Potential relevance to toxicity pattern of 5-fluorouracil
13. Attenuation of the antitumor activity of 5-fluorouracil by (R)-5-fluoro-5,6-dihydrouracil
14. Mechanism-based inactivation of dihydropyrimidine dehydrogenase by 5-ethynyluracil
15. 5-Ethynyluracil (776C85): Inactivation of dihydropyrimidine dehydrogenase in vivo
16. Eniluracil treatment completely inactivates dihydropyrimidine dehydrogenase in colorectal tumors
17. Improving fluorouracil chemotherapy with a novel orally administered fluoropyrimidines
18. 5-Ethynyluracil (776C85): A potent modulator of the pharmacokinetics and antitumor activity of 5-FU
19. Phase I clinical and pharmacologic study of eniluracil plus fluorouracil in patients with advanced cancer
20. Pharmacokinetic, oral bioavailability, and safety study of fluorouracil in patients treated with 776C85, an inactivator of dihydropyrimidine dehydrogenase
21. Phase I and pharmacologic study of oral fluorouracil on a chronic daily schedule in combination with the dihydropyrimidine dehydrogenase inactivator eniluracil
22. Prediction of creatinine clearance from serum creatinine
23. Dihydropyrimidine dehydrogenase activity in human peripheral blood mononuclear cells and liver: Population characteristics, newly identified deficient patients, and clinical implication in 5-fluorouracil chemotherapy
24. Decreased dihydropyrimidine dehydrogenase activity in a population of patients with breast cancer: Implication for 5-fluorouracil-based chemotherapy
25. Severe neurotoxicity following 5-fluorouracil-based chemotherapy in a patient with dihydropyrimidine dehydrogenase deficiency
26. S-ethynylurail (776C85), a modulator of the therapeutic activity of 5-fluorouracil