Dose dependent retention and polyglutamation of N10-propargyl-5,8-dideazafolic acid (CB 3717) in the tumour-bearing mouse.
The antifolate drug, CB 3717, when given to the tumour-bearing mouse, was retained in its liver and kidneys and to a smaller extent (50-200 fold) in EAC-cells. The amount of the drug retained in the tumour cells, but not in the host organs, depended on the route of its administration, being distinctly higher after i.p. than after s.c. injection. The extensive polyglutamation of CB 3717 occurred in the liver only after administration of the drug at 20 but not at 100 mg per kg. CB 3717 polyglutamation in the kidneys was low and in EAC-cells negligible.
Manteuffel-Cymborowska
M
M
Department of Cellular Biochemistry, Nencki Institute of Experimental Biology, Warsaw, Poland.
Kaminska
B
B
Grzelakowska-Sztabert
B
B
D000818:Animals; D000970:Antineoplastic Agents / Q000493:pharmacokinetics*; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism*; D005260:Female; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics; D005493:Folic Acid Antagonists / Q000493:pharmacokinetics*; D007668:Kidney / Q000378:metabolism; D007700:Kinetics; D008099:Liver / Q000378:metabolism; D051379:Mice; D011799:Quinazolines / Q000378:metabolism / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D000970:Antineoplastic Agents; D005493:Folic Acid Antagonists; D011799:Quinazolines; C031662:CB 3717; D005492:Folic Acid