Pharmacokinetics of 2-methyl-9-hydroxyellipticinium acetate (NSC-264137) in cancer patients (phase I study).

Abstract

In 12 cancer patients we studied the pharmacokinetics of a new antitumor compound, elliptinium, which is a quaternary ammonium derivative of ellipticine, after i.v. infusion. The main parameters were calculated by means of the ADAPT program based upon plasma concentrations and urinary elimination determined by a high performance liquid chromatographic assay and fluorescence detection. The mean apparent volume of distribution for the central compartment, V1, is 2.8 l, the total plasma clearance is 971 ml/min, with a renal clearance of 127 ml/min. The mean elimination half-life, t1/2, z, is 23.7 hr, but shows a large interindividual variation. Urinary elimination is quite low (16%), with the main part (12%) excreted in the first 24 hr. In vitro plasma protein binding (78%) was found to be independent of the concentration (0.1-5.0 micrograms/ml).

• Authors: A Gouyette, D Huertas, J P Droz, J Rouesse, J L Amiel
• Journal: European journal of cancer & clinical oncology (Eur J Cancer Clin Oncol) Vol. 18 Issue 12 Pg. 1285-92 (Dec 1982) ISSN: 0277-5379 [Print] England
• PMID: 6891926 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Alkaloids
• Antineoplastic Agents
• Ellipticines
• elliptinium

Topics

• Adult
• Aged
• Alkaloids (metabolism)
• Antineoplastic Agents (blood, metabolism)
• Chromatography, High Pressure Liquid
• Drug Evaluation
• Ellipticines (metabolism)
• Female
• Humans
• Kinetics
• Male
• Middle Aged
• Neoplasms (blood, metabolism)
• Protein Binding