Distribution of the novel anticancer drug candidate brequinar sodium (DuP 785, NSC 368390) into normal and tumor tissues of nude mice bearing human colon carcinoma xenografts |
| |
| Authors: | Huey-shin L. Shen Shih-Fong Chen Davette L. Behrens Charles C. Whitney Daniel L. Dexter Martin Forbes |
| |
| Affiliation: | (1) Drug Metabolism Section, E.I. du Pont de Nemours and Co., Inc, 19898 Wilmington, DE, USA;(2) Cancer Chemotherapy, E.I. du Pont de Nemours and Co., Inc, 19898 Wilmington, DE, USA;(3) Analytical R&D, Pharmaceuticals Division, Medical Products Department, E.I. du Pont de Nemours and Co., Inc, 19898 Wilmington, DE, USA;(4) Stine-Haskell Research Center, Du Pont Company, P. O. Box 30, 19714 Newark, DE, USA |
| |
| Abstract: | ![]()
Summary The distribution of the novel anticancer drug candidate Brequinar Sodium (DuP 785, NSC 368390) was studied in control mice and mice implanted subcutaneously with human colon carcinoma xenografts. Mice were given radiolabeled 14C-Brequinar Sodium intravenously. Brequinar concentrations in blood and various tissues were determined at 1, 6, and 24 h after drug administration. Within 1 h Brequinar distributed to the tumor and all other tissues studied. The tumor-to-blood drug concentration ratios ranged from 0.19 to 0.41. Radioactivity in the liver and small intestine at 1 h accounted for 17% and 13%, respectively, of the dose given. Elimination rates of Brequinar from all tissues were approximately equal to that from blood. Comparison of blood concentrations determined by both radioactivity and HPLC methods suggests that the intact drug is probably the only form in the blood. |
| |
| Keywords: | |
| 本文献已被 SpringerLink 等数据库收录！ |
|
