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Article: ^sup 177^Lu-AMBA: Synthesis and Characterization of a Selective ^sup 177^Lu-Labeled GRP-R Agonist for Systemic Radiotherapy of Prostate Cancer
- Article from:
- The Journal of Nuclear Medicine
- Article date:
- July 1, 2006
- Author:
CopyrightCopyright Society of Nuclear Medicine Jul 2006. Provided by ProQuest LLC. (Hide copyright information)
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Gastrin-releasing peptide receptors (GRP-R) are upregulated in many cancers, including prostate, breast, and lung. We describe a new radiolabeled bombesin (BBN) analog for imaging and systemic radiotherapy that has improved pharmacokinetics (PK) and better retention of radioactivity in the tumor. Methods: DO3A-CH^sub 2^CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH^sub 2^ (AMBA) was synthesized and radiolabeled. The human prostate cancer cell line PC-3 was used to determine the binding (Kd), retention, and efflux of ^sup 177^Lu-AMBA. Receptor specificity was determined by in vitro autoradiography in human tissues. PK and radiotherapy studies were performed in PC-3 tumor-bearing male nude mice. ...