Pm-149 DOTA bombesin analogs for potential radiotherapy: in vivo comparison with Sm-153 and Lu-177 labeled DO3A-amide-βAla-BBN(7–14)NH₂

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• 作者：Hu ; Fang ; Cutler ; Cathy S. ; Hoffman ; Timothy ; Sieckman ; Gary ; Volkert ; Wynn A. ; Jurisson ; Silvia S.
• 关键词：Radiolanthanide ; Promethium-149 ; Samarium-153 ; Lutetium-177 ; DOTA analogs ; Bombesin ; GRP receptors
• 刊名：Nuclear Medicine and Biology
• 出版年：2002
• 出版时间：May, 2002
• 年：2002
• 卷：29
• 期：4
• 页码：423-430
• 全文大小：109 K

文摘

Promethium-149 (¹⁴⁹Pm) is one of only three radiolanthanides that can be prepared in no carrier added concentrations. This high specific activity radiolanthanide is thus suitable for targeting limited numbers of specific receptors found on many tumor cells. Promethium-149 is a moderate energy β^- emitter (1.07 MeV (95.9 % )) with a half-life of 2.21 days. Pm-149 also emits a low abundance of an imageable γ ray (286 keV (3 % )) that may allow in vivo tracking of the therapeutic dose. The ¹⁴⁹Pm and Sm complexes with the DO3A-amide chelator with zero and three carbon spacers to the bombesin peptide analog BBN(7–14)NH₂ were synthesized and characterized. The Sm complexes were synthesized for macroscopic characterization purposes (ESI-MS, in vitro cell binding) since no stable isotopes of Pm are known. The biological properties of the ¹⁴⁹Pm, ¹⁵³Sm and ¹⁷⁷Lu-DO3A-amide-βAla-BBN complexes were compared in normal mouse biodistribution studies.