Aminocarboxylate complexes and octreotide complexes with no carrier added 177Lu, 166Ho and 149Pm.
Several aminocarboxylate complexes of the "no carrier added" (NCA) radiolanthanides (149)Pm, (166)Ho and (177)Lu were evaluated using our in vitro hydroxyapatite and serum stability model and in vivo in normal CF-1 mice [10]. The aminocarboxylate chelates evaluated with the NCA radiolanthanides for in vitro stability were EDTA, CDTA, DTPA, MA-DTPA and DOTA. In addition, the NCA radiolanthanide complexes with DTPA-octreotide (DTPA-OCT) were synthesized and evaluated, as a model for a peptide conjugated aminocarboxylate complex. The biodistribution studies of the NCA complexes with DTPA, DOTA and DTPA-OCT showed that the in vitro model correctly predicted the in vivo stability of the radiolanthanide complexes, with Ln-DOTA > Ln-DTPA > Ln-DTPA-OCT.
Department of Chemistry, University of Missouri, Columbia, MO, USA.
Wen Ping
WP
Li
C Jeff
CJ
Smith
Cathy S
CS
Cutler
Timothy J
TJ
Hoffman
Alan R
AR
Ketring
Silvia S
SS
Jurisson
D000818:Animals; D002614:Chelating Agents / Q000494:pharmacology; D004355:Drug Stability; D006207:Half-Life; D006695:Holmium / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D008187:Lutetium / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D015282:Octreotide / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D011399:Promethium / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D011868:Radioisotopes / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D019275:Radiopharmaceuticals / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D014018:Tissue Distribution
D002614:Chelating Agents; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D008187:Lutetium; D015282:Octreotide; D006695:Holmium; D011399:Promethium