The pharmacokinetics and metabolism of N-desmethyl-N-formyl-leurosine (F-leurosine) in the rat.
Absorption, tissue distribution, excretion, protein binding, and the metabolism of 14C labelled F-leurosine were studied in the rat. A triphasic curve for the disappearance of the drug from blood was found. The bile was the major route of excretion: 80% of radioactivity was recovered in the bile during the first 28 h after i.v. administration. 54% of the F-leurosine binds, in the concentration range of 0.1 mumol/1-0.5 mmol/l to plasma proteins. The TLC and HPLC data suggested that the bile of rats administered [14C]-F-leurosine contained either none or only small amount of metabolic products, which were most probably due to chemical decomposition rather then metabolism. Rat liver homogenates did not metabolize [14C] F-leurosine to any detectable extent.
D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D011485:Protein Binding; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution; D014748:Vinca Alkaloids / Q000097:blood / Q000378:metabolism*
D001798:Blood Proteins; D014748:Vinca Alkaloids; C016463:formyl-leurosine