The pharmacokinetics of 1954U89, 1,3-diamino-7-(1-ethylpropyl)-8- methyl-7H-pyrrolo-(3, 2-f)quinazoline, in dogs and rats after intravenous and oral administration

Biopharmaceutics and Drug Disposition

Volumn 18, Issue 5, 1997, Pages 433-442

  Studenberg, S D ^a   Woolley, J L ^a   Deangelis, D V ^a   Wargin, W A ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

Bioavailability; Dihydrofolate reductase; Enzyme inhibition; Pharmacokinetics

Indexed keywords

1,3 DIAMINO 7 (1 ETHYLPROPYL) 8 METHYL 7H PYRROLO (3,2 F) QUINAZOLINE; 1954 U89; DIHYDROFOLATE REDUCTASE INHIBITOR; FOLINATE CALCIUM; UNCLASSIFIED DRUG;

ARTICLE; CANCER CHEMOTHERAPY; DOG; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; ENZYME INHIBITION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; ORAL DRUG ADMINISTRATION; RAT;

ADMINISTRATION, ORAL; ANIMALS; ANTIDOTES; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DOGS; FOLIC ACID ANTAGONISTS; HALF-LIFE; INFUSIONS, INTRAVENOUS; LEUCOVORIN; MALE; PYRROLES; QUINAZOLINES; RATS; RATS, INBRED STRAINS; SPECIES SPECIFICITY;

EID: 0030792337     PISSN: 01422782     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1099-081X(199707)18:5<433::AID-BDD32>3.0.CO;2-P     Document Type: Article

References (11)

1. L. F. Kuyper, D. P. Baccanari, M. L. Jones, R. N. Hunter, R. L. Tansik, S. S. Joyner, C. M. Boytos, S. K. Rudolph, V. Knick, H. R. Wilson, J. M. Caddell, H. S. Friedman, J. C. W. Comley and J. N. Stables, High affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1, 3-diaminopyrrolo[3, 2-f]quinazolines with small molecular size. J. Med. Chem, 39, 892-903 (1996).
2. E. M. Berman and L. M. Werbel, The renewed potential for folate antagonists in contemporary cancer chemotherapy. J. Med. Chem., 34, 479-485 (1991).
3. R. A. Upton, Simple and reliable method for serial sampling of blood from rats. J. Pharm. Sci., 64, 112-114 (1975).
4. S. D. Studenberg, D. V. DeAngelis and J. L. Woolley, High performance liquid chromatographic assay with fluorescence detection for the analysis of 1954U89, 1, 3-diamino-7-(1-ethylpropyl)-8-methyl-7H-pyrrolo-(3, 2-f)quinazoline, in plasma. J. Liq. Chromatogr., 19, 823-836 (1996).
5. M. Gibaldi and D. Perrier, Pharmacokinetics, 2nd edn, Dekker, New York, 1982.
6. B. Davies and T. Morris, Physiological parameters in laboratory animals and humans. Pharm. Res., 10, 1093-1095 (1993).
7. E. C. Weir, A. R. Cashmore, R. N. Dreyer, M. Graham, N. Hsiao, B. A. Moroson, W. L. Sawicki and J. R. Bertino, Pharmacology and toxicity of a potent 'nonclassical' 2,4-diamino quinazoline folate antagonist, trimetrexate, in normal dogs. Cancer Res., 42, 1696-1702 (1982).
8. 14C]piritrexim in dogs and oral adminstration. Drug Metab. Disposit., 19, 1139-1146 (1991).
9. Y. He, Y. Tanigawara, M. Yasuhara and R. Hori, Effect of folinic acid on tissue residence and excretion of methotrexate in rats. Drug Metab. Disposit., 19, 729-734 (1991).
10. B. K. Wong, T. F. Woolf, T. Chang and L. R. Whitfield, Metabolic disposition of trimetrexate, a nonclassical dihydrofolate reductase inhibitor, in rat and dog. Drug Metab. Disposit., 18, 980-986 (1990).
11. 14C]piritrexim in rats after intravenous and oral administration. Drug Metab. Disposit., 19, 600-608 (1991).