Related Experiment Videos
Distribution of clomesone in mice
1Kettering-Meyer Laboratory, Southern Research Institute, Birmingham, AL 35255-5305.
Cancer Treatment Reports
|December 1, 1987
Summary
Clomesone, a novel alkylating agent, is quickly eliminated from mouse plasma with a half-life of 11 minutes. Most of the drug and its metabolites bind to tissues and are excreted in urine.
Area of Science:
- Pharmacology
- Toxicology
- Drug Metabolism
Background:
- Clomesone is a novel alkylating agent with potential therapeutic applications.
- Understanding the pharmacokinetic profile of clomesone is crucial for its clinical development.
Purpose of the Study:
- To investigate the distribution and elimination of clomesone in mice following intravenous administration.
- To identify potential metabolites and assess tissue binding.
Main Methods:
- Intravenous administration of radiolabeled clomesone ([14C]clomesone) to mice at a dose of 35 mg/kg.
- Analysis of plasma and tissue radioactivity using liquid scintillation counting and high-pressure liquid chromatography (HPLC).
- Quantification of urinary excretion and assessment of macromolecular binding.
Main Results:
- Clomesone exhibited rapid elimination from plasma with a half-life of 11 minutes.
- Highest radioactivity concentrations were observed in liver, kidney, and small intestines.
- A significant portion of radioactivity was bound to tissue macromolecules, and 77.6% of the dose was recovered in urine within 24 hours.
- Less than 2% of the dose was excreted unchanged in urine.
Conclusions:
- Clomesone is rapidly cleared from circulation and extensively distributed into tissues.
- The drug and/or its metabolites undergo significant binding to tissue components.
- Urinary excretion is the primary route of elimination for clomesone and its metabolites.