Metal radionuclide chelating compounds for improved chelation kinetics

Abstract

Abstract The present invention provides metal chelating compounds, to chelates and chelate-targeting agent conjugates formed from the chelating compounds, and to methods for making and using these compositions. The chelating compounds incorporate two nitrogen atoms and three sulfur atoms ("N 2 S 3 "), two nitrogen atoms and four sulfur atoms ("N 2 S 4 "), or three nitrogen atoms and three sulfur atoms ("N 3 S 3 "). Metals, and metal oxides, capable of being chelated by the compounds include those that are radionuclides, such as 99m Tc and 186/188 Re. The targeting agent portion of the chelate-targeting agent conjugates provided includes antibodies, peptides, hormones, enzymes and biological response modifiers. Methods for making the conjugates are provided and encompass the addition of a metal, or metal oxide, to a chelating compound prior to attachment to a targeting agent as well as subsequent to the attachment. Another aspect of the invention provides kits for producing chelate-targeting agent conjugates for radiopharmaceutical use. An additional aspect of the invention provides methods for using the chelate-targeting agent conjugates for diagnostic and therapeutic purposes, such as detection of a target site and delivery of a radionuclide to the site, respectively.

Inventors

• 👤 Ananthachari Srinivasan
• 👤 Alan R. Fritzberg
• 👤 David S. Jones

Bibliographic Details