The pharmacokinetics of N-[ 14C-formyl]-leurosine in humans

• Published in: European journal of cancer Vol. 17; no. 3; pp. 329 - 335
• Main Authors: Erdélyi-Tóth, V., Csetényi, J., Kanyár, B., Kerpel-Fronius, S., Eckhardt, S.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.03.1981
• Subjects: Antineoplastic Agents, Phytogenic - metabolism; Feces - analysis; Female; Humans; Male; Metabolic Clearance Rate; Models, Biological; Neoplasms - metabolism; Vinca Alkaloids - blood; Vinca Alkaloids - metabolism; Vinca Alkaloids - urine
• ISSN: 0014-2964
• DOI: 10.1016/0014-2964(81)90124-9

N-Formyl-leurosine labeled with 14 C in the formyl group was administered to six patients with malignant disease, and the pharmacokinetic behavior of the drug was determined. Chromatographic studies on plasma showed the presence of unchanged drug and 7 metabolites. No metabolites were found in the urine. The plasma decay curve of the unchanged drug was biphasic with half-life values of t 1 2α = 18.6 min and t 1 2β = 4.28 hr . Within 72 hr only 30–40% of the radioactivity could be recovered in urine and feces in 5 patients. One patient consumed laxatives during the treatment. In this case 95% of the 14 C-dose was recovered. The contribution made by fecal elimination was 80%.