RADIOPHARMACEUTICAL AND METHODS
The radiopharmaceutical 177 Lu-PSMA I&T is provided, including in high purities with extended shelf life. Further provided are methods of synthesis of 177 Lu-PSMA I&T and pharmaceutical compositions and methods of treatment that comprise 177 Lu-PSMA I&T.
1 - 70 . (canceled)
71 . A pharmaceutical composition comprising:
(a) a complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA;
(b) one or more ascorbate compounds.
72 . The composition of claim 71 wherein the composition is free of a gentisate adduct impurity.
73 . The composition of claim 71 wherein the composition comprises one or more gentisate compounds.
74 . The composition of claim 71 wherein the composition is an aqueous formulation.
75 . The composition of claim 71 wherein the complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA comprises in optical excess the following structure:
76 . The composition of claim 71 wherein the complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA comprises in optical excess the following structure:
77 . A pharmaceutical composition comprising:
(a) a complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA;
(b) one or more stabilizer compounds,
wherein the composition at least substantially free of a gentisate acid adduct impurity.
78 . A method for treating a patient suffering from cancer, comprising:
a) admixing 1) lutetium-177, 2) EuK-Sub-kf-iodo-y-DOTAGA in the substantial or complete absence of a gentisate compound, and 3) one or more stabilizer compounds;
b) heating the admixed 1) lutetium-177 and 2) EuK-Sub-kf-iodo-y-DOTAGA in the substantial or complete absence of a gentisate compound, wherein a complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA is formed in the absence of a gentisate compound; and
c) administering the complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA to the patient.
79 . The method of claim 78 wherein the subject is suffering from prostate cancer.
80 . The method of claim 78 wherein 1) lutetium-177, 2) EuK-Sub-kf-iodo-y-DOTAGA and 3) one or more stabilizer compounds are admixed in the absence of a gentisate compound.
81 . The method of claim 78 wherein 1) lutetium-177, 2) EuK-Sub-kf-iodo-y-DOTAGA and 3) one or more stabilizer compounds are heated in the absence of a gentisate compound.
82 . The method of claim 78 wherein one or more ascorbate compounds are admixed with 1) lutetium-177 and 2) EuK-Sub-kf-iodo-y-DOTAGA.
83 . The method of claim 78 further comprising adding one or more ascorbate compounds to the complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA.
84 . The method of claim 83 wherein the one more gentisate compounds are added while or after heating is reduced or terminated.
85 . The method of claim 78 further comprising adding one or more gentisate compounds to the complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA.
86 . The method of claim 83 further comprising adding one or more gentisate compounds to the complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA.
87 . The method of claim 85 wherein the one more gentisate compounds are added while or after heating is reduced or terminated.
88 . The method of claim 86 wherein the one more gentisate compounds are added while or after heating is reduced or terminated.
89 . The method of claim 80 wherein the complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA does not contain an impurity having a relative retention time of approximately of 9 to 12 minutes by high-performance liquid chromatography.
90 . A complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA obtainable by a method comprising:
a) admixing 1) lutetium-177, 2) EuK-Sub-kf-iodo-y-DOTAGA in the substantial or complete absence of a gentisate compound, and 3) one or more stabilizer compounds; and
b) heating the admixed 1) lutetium-177 and 2) EuK-Sub-kf-iodo-y-DOTAGA in the substantial or complete absence of a gentisate compound, wherein a complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA is formed in the absence of a gentisate compound.
91 . A pharmaceutical composition comprising a complex of claim 90 .
92 . The pharmaceutical composition of claim 91 wherein the complex comprising the following compound in optical excess:
93 . The pharmaceutical composition of claim 91 wherein the complex comprising the following compound in optical excess:
94 . The pharmaceutical composition of claim 91 wherein the composition comprises one or more stabilizer compounds.
95 . The pharmaceutical composition of claim 91 wherein the composition comprises one or more ascorbate compounds.
96 . The pharmaceutical composition of claim 95 wherein the composition comprises one or more gentisate compounds.
97 . The pharmaceutical composition of claim 91 wherein the composition is free of a gentisate adduct impurity.
98 . A method of treating a subject suffering from cancer, comprising administering to the subject an effective amount of a composition of claim 91 .
99 . The method of claim 99 wherein the subject is suffering from prostate cancer.