Method to enhance tissue accumulation of radiolabeled compounds

US6630123B1 · kind B1 · utility

Assignee

• BOARD OF SUPERVISORS OF LOUISIANA STATE UNIVERSITY AND AGRICULTURAL AND MECHANICAL COLLEGE · US

Inventors

• Eugene A. Woltering · Kenner, US
• Gregory D. Espenan · Metairie, US

Key dates

• Filing date: Sep 18, 2000
• Grant date: Oct 7, 2003
• Expiry date: Sep 18, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K51/083
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Administration of a radioisotopic compound by infusion over a period of time greater than two hours, preferably greater than twelve hours, greatly increases the maximum radioactivity that accumulates in the target cell. The efficacy of the administration of the radiolabeled compound can be increased about five times higher than prior bolus injection or short infusion methods. This method enhances the tumor to background ratio by increasing the actual radioligand accumulated inside the target cells. This technique works for any radiolabeled compound whose cellular uptake is limitedly a cellular process of either binding to a cellular receptor or to a transport protein. Once the radiolabeled compound is bound and internalized, the ability of an unlabeled compound to compete with the radioligand is markedly decreased. The primary factor governing residence time after internalization is the physical half-life of the radioisotope, not biologic half-life.