One-Step Labeling of Antibodies to High Specific Activity with Actinium-225

摘要

Provided herein is a one-step method for chelating actinium-225 to a construct comprising a chelator linked to a bio-molecule, such as, an antibody or monoclonal antibody, via a bifunctional ligand in, for example, a 3-arm configuration. Also provided are methods for increasing the radiochemical yield of an actinium-225-chelant-biomolecule complex and for producing a high specific activity actinium-225 complex. The chelation is performed at a physiological temperature, about 37° C. Also provided are high specific activity actinium-225 complexes, that is, actinium-225 chelated to the chelator-biomolecule construct and pharmaceutical compositions thereof. Further provided are methods of treating a neoplastic disease or disorder with the actinium-225 complexes.

主权项

1. A one-step chelation process for actinium-225, comprising:
chelating, under physiological conditions, actinium-225 to a chelator construct comprising a bifunctional ligand conjugated to said chelator in a 3-arm configuration and covalently linking a biomolecule thereto.