Pm-149 DOTA bombesin analogs for potential radiotherapy. in vivo comparison with Sm-153 and Lu-177 labeled DO3A-amide-betaAla-BBN(7-14)NH(2).
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 beta(-) emitter (1.07 MeV (95.9%)) with a half-life of 2.21 days. Pm-149 also emits a low abundance of an imageable gamma 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)NH(2) 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-betaAla-BBN complexes were compared in normal mouse biodistribution studies.
Hu
Fang
F
Department of Chemistry, University of Missouri, Columbia, MO 65211, USA.
Cutler
Cathy S
CS
Hoffman
Timothy
T
Sieckman
Gary
G
Volkert
Wynn A
WA
Jurisson
Silvia S
SS
D000818:Animals; D001839:Bombesin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D006573:Heterocyclic Compounds, 1-Ring / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use; D006801:Humans; D008187:Lutetium / Q000493:pharmacokinetics* / Q000627:therapeutic use; D008297:Male; D008657:Metabolic Clearance Rate; D008674:Metals, Rare Earth / Q000493:pharmacokinetics / Q000627:therapeutic use; D051379:Mice; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use; D011399:Promethium / Q000493:pharmacokinetics* / Q000627:therapeutic use; D011471:Prostatic Neoplasms / Q000378:metabolism* / Q000532:radiotherapy*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics / Q000627:therapeutic use; D015203:Reproducibility of Results; D012493:Samarium / Q000493:pharmacokinetics* / Q000627:therapeutic use; D012680:Sensitivity and Specificity; D014018:Tissue Distribution
D006573:Heterocyclic Compounds, 1-Ring; D008674:Metals, Rare Earth; D010446:Peptide Fragments; D019275:Radiopharmaceuticals; C469344:bombesin (7-14)amide, DO3A-amide-; C469343:bombesin (7-14)amide, DO3A-amide-beta-alanyl-; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid; D012493:Samarium; D008187:Lutetium; D001839:Bombesin; D011399:Promethium