Radiopharmaceutical and methods

Abstract

The radiopharmaceutical 177Lu-PSMA I&T is provided, including in high purities with extended shelf life. Further provided are methods of synthesis of 177Lu-PSMA I&T and pharmaceutical compositions and methods of treatment that comprise 177Lu-PSMA I&T.

What is claimed is: 
     
         1 - 63 . (canceled) 
     
     
         64 . A complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA, produced by a method comprising the steps of:
 a) admixing in the complete absence of a gentisate compound:
 1) lutetium-177; 
 2) EuK-Sub-kf-iodo-y-DOTAGA; and 
 3) one or more ascorbate compounds in an amount between 55 mg/mL to 75 mg/mL; and 
   b) heating the admixed 1) lutetium-177, 2) EuK-Sub-kf-iodo-y-DOTAGA, and 3) one or more ascorbate compounds in the absence of a gentisate compound and at a temperature not exceeding 94° C.;   wherein a complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA is formed without the addition of a gentisate compound; and   c) cooling the complex formed in step b) and admixing the complex with one or more ascorbate compounds and one or more gentisate compounds to provide a radiopharmaceutical composition that maintains radiochemical purity of at least 95% for 3 days wherein the amount of one or more ascorbate compounds is between 10 mg/mL to 100 mg/mL and the amount of one or more gentisate compounds is between 5 mg/mL to 100 mg/mL.   
     
     
         65 . The complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA of  claim 64  which is:
 1) free of unchelated lutetium-177 in an amount of 1 weight % or less; and/or 
 2) free of radiochemical impurities in an amount of 3 weight % or less; and/or 
 3) free of chemical impurities in an amount of 5 weight % or less, 
 all weight % based on total weight of the complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA, and 
 where the complex is maintained at 30° C., or less and such purity levels are exhibited for 3 days or more following formation of the complex. 
 
     
     
         66 . The complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA of  claim 64  which is free of an impurity having a retention time of approximately 9 to 12 minutes by high-performance liquid chromatography. 
     
     
         67 . The complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA of  claim 64  wherein incorporation of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA is greater than 98 mole percent.