Design of a radiopharmaceutical for the palliation of painful bone metastases: rhenium-186-labeled bisphosphonate derivative

✍ Scribed by Kazuma Ogawa; Takahiro Mukai; Yasushi Arano; Hirofumi Hanaoka; Kazuyuki Hashimoto; Hiroshi Nishimura; Hideo Saji

• Book ID: 102375075
• Publisher: John Wiley and Sons
• Year: 2004
• Tongue: French
• Weight: 123 KB
• Volume: 47
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.864

✦ Synopsis

Abstract

To develop a radiopharmaceutical for the palliation of painful bone metastases based on the concept of bifunctional radiopharmaceuticals, we designed a bisphosphonate derivative attached to a stable ^186^Re‐monoaminemonoamidedithiol (MAMA) chelate (^186^Re‐MAMA‐BP) to improve the instability of ^186^Re‐HEDP. The precursor (Tr‐MAMA‐BP) of ^186^Re‐MAMA‐BP was synthesized by coupling the carboxyl group of the Tr‐MAMA derivative with the amino group of the bisphosphonate derivative. This ^186^Re‐labeled compound was prepared by a ligand exchange reaction using ^186^Re‐glucoheptonate with a radiochemical yield of 32.0 ± 4.1%. In the incubation study in buffered solution (pH 7.0), ^186^Re‐MAMA‐BP was more stable than ^186^Re‐HEDP. This suggests that ^186^Re‐MAMA‐BP is a potential radiopharmaceutical for the palliation of painful bone metastases. Copyright © 2004 John Wiley & Sons, Ltd.