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Preparation and biodistribution of [125I]Melphalan: a potential radioligand for diagnostic and therapeutic applications

✍ Scribed by A. M. Amin; S. E. Soliman; H. A. El-Aziz

Publisher
John Wiley and Sons
Year
2009
Tongue
French
Weight
138 KB
Volume
53
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

This paper addresses the development of a new radiopharmaceutical for cancer imaging and therapy. The optimization of the labeling conditions of thymidine analogue, melphalan, with^125^I is described. High radiochemical yield 96.8% was obtained by reacting 0.2 mg melphalan with ^125^I in the presence of choloramin‐T as oxidizing agent in 0.5 M phosphate buffer, pH 7, at 70°C for 15 min. Preliminary in vivo study was done in non‐tumor bearing mice. The results revealed that this new tracer,^125^I‐melphalan, has a high affinity to be localized in the tumor site for a long period, which indicates the specificity of this tracer to the tumor cells. The labeled compound was cleared quickly from most of the body organs. These findings suggest that ^125^I‐melphalan allows imaging and treatment of cancer. ^125^I‐melphalan meets most of the requirements necessary to be used as a successful diagnostic and therapeutic agent: it is a low‐molecular‐weight molecule that diffuses readily in the tissues, and dose not induce an antibody response. Copyright © 2009 John Wiley & Sons, Ltd.

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