Neorx Corporation

University of Missouri

Jean-Luc E Vanderheyden

Alan R Fritzberg

Sudhakar Kasina

Jeffrey N Fitzner

Gary J Ehrhardt

Fu-Min Su

The present invention provides conjugates formed from calcified tissues targeting agents and radiolabeled compounds. One such conjugate comprises a chelate and a targeting agent that is capable of associating with calcified tissue, wherein the chelate contains at least one nitrogen atom or at least one sulfur atom or combinations thereof as the donor atoms. Another aspect of the invention provides method for using the conjugates for diagnostic and therapeutic purposes, including those related to bone cancer.

Conjugates for bone imaging and bone cancer therapy

The present invention provides conjugates formed from calcified tissues targeting agents and radiolabeled compounds. One such conjugate comprises a chelate and a targeting agent that is capable of associating with calcified tissue, wherein the chelate contains at least one nitrogen atom or at least one sulfur atom or combinations thereof as the donor atoms. Another aspect of the invention provides methods for using the conjugates for diagnostic and therapeutic purposes, including those related to bone cancer.

Water soluble irradiation targets are disclosed for the production of .sup.186 Re and .sup.188 Re. The irradiation targets are selected for both water solubility and absence of elements which would produce contaminating isotopes for medical therapeutic and diagnostic use. In one embodiment, .sup.186 Re or .sup.188 Re is produced by the direct irradiation of a water soluble irradiation target comprising .sup.185 Re or .sup.187 Re, respectively. Preferred targets for this purpose include aluminum perrhenate, lithium perrhenate and magnesium perrhenate. In another embodiment, a zirconyl tungstate generator comprising .sup.188 W for the production of .sup.186 Re is obtained by irradiating a soluble irradiation target comprising .sup.186 W, dissolving the irradiated target in aqueous solution, reacting the dissolved target with an aqueous solution comprising zirconyl ion to form an insoluble zirconium tungstate precipitate and disposing the precipitate in an elutable container. Preferred irradiation targets for this purpose include sodium tungstate and lithium tungstate. In each of the foregoing embodiments, the irradiation target is readily soluble in aqueous solution and may be used directly in solution form after irradiation, such as for ligand conjunction for medical diagnostic or therapeutic purposes, without cumbersome dissolution, neutralization, purification and other processing steps involving irradiated materials inherent in prior .sup.186 Re and .sup.188 Re production methods.

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Seattle, WA, United States of America

Jean-Luc E Vanderheyden