Labeling monoclonal antibodies with 90yttrium- and 111indium-DOTA chelates: a simple and efficient method.
Yttrium-90 and indium-111 have been attached to a monoclonal antibody with a bifunctional chelating agent (DOTA-peptide). Using the unique features of this DOTA-peptide and its complexes with trivalent yttrium and indium, the bifunctional chelating agent was prelabeled with either radiometal and then conjugated to chimeric monoclonal antibody L6. Both radiolabeling procedures and yield are suitable for the practical preparation of radiopharmaceuticals. Biodistribution studies in tumor-bearing mice showed that, e.g., on day 3 after intravenous injection of a 90Y immunoconjugate, liver uptake was 5.4 +/- 1.5% ID/g, bone uptake 2.0 +/- 0.5% ID/g, and tumor uptake 18.0 +/- 8.0% ID/g.
Li
M
M
Department of Chemistry, University of California, Davis 95616.
Meares
C F
CF
Zhong
G R
GR
Miers
L
L
Xiong
C Y
CY
DeNardo
S J
SJ
D000818:Animals; D000911:Antibodies, Monoclonal / Q000737:chemistry*; D002614:Chelating Agents / Q000737:chemistry*; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006573:Heterocyclic Compounds, 1-Ring; D007205:Indium Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*; D051379:Mice; D008819:Mice, Nude; D009374:Neoplasms, Experimental / Q000378:metabolism; D014018:Tissue Distribution; D015021:Yttrium Radioisotopes / Q000737:chemistry*
D000911:Antibodies, Monoclonal; D002614:Chelating Agents; D006571:Heterocyclic Compounds; D006573:Heterocyclic Compounds, 1-Ring; D007205:Indium Radioisotopes; D015021:Yttrium Radioisotopes; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid