The present invention relates to methods for labeling a PSMA binding ligand with a radioactive isotope, preferably .sup.68Ga, .sup.67Ga or .sup.64Cu, said method comprising the steps of: i. providing a single vial comprising, in dried form, said PSMA binding ligand f the following formula (I): (I) at least one buffering agent, sodium chloride and a stabilizer against radiolytic degradation, ii. adding a solution of said radioactive isotope into said single vial, thereby obtaining a solution of said PSMA binding ligand of formula (I) with said radioactive isotope, iii. mixing the solution obtained in ii., and incubating it for a sufficient period of time for obtaining said PSMA binding ligand labelled with said radioactive isotope, and, iv. optionally, adjusting the pH of the solution.

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A radiopeptide is provided which comprises (a) a radionuclide, wherein the radionuclide is terbium-161, (b) a chelator coordinating terbium-161, and (c) a peptide or peptide analogue, which is a somatostatin receptor (SSTR) antagonist. The radiopeptide is suitable for use in the treatment of tumor diseases.

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

This invention relates new radiopharmaceutical conjugates for use in improved methods of diagnosis and treatment of cancer. The radiopharmaceutical conjugate comprises, in sequence: a metabolite that targets tumour cells, bound to a chelating agent capable of containing a radionuclide, bound to a linker capable of binding with an EPR agent in vitro or in vivo; or a chelating agent capable of containing a radionuclide, bound to a metabolite that targets tumour cells, bound to a linker capable of binding with an EPR agent in vitro or in vivo. The radiopharmaceutical conjugates of the present invention provide active and passive targeted radio nuclide delivery systems that can help to improve the biodistribution and pharmacological toxicity of the radiopharmaceuticals used for the diagnosis and therapy of cancer.

A method of preparing a .sup.64Cu-BaBaSar-RGD.sub.2 solution is provided. The method includes lyophilizing a solution of BaBaSar-RGD.sub.2 and adding a .sup.64Cu solution to the lyophilized BaBaSar-RGD.sub.2.

The present disclosure relates to the synthesis of radionuclide complex solutions, in particular for their use in the commercial production of radioactive drug substances, for diagnostic and/or therapeutic purposes. In particular, the synthesis method comprises the following steps in the following order: a. providing a radionuclide precursor solution into a first vial, b. transferring the radionuclide precursor solution into a reactor, c. providing a reaction buffer solution into said first vial containing residual radionuclide precursor solution, d. transferring the buffer reaction solution and residual radionuclide precursor solution from said first vial into the reactor, e. transferring a peptide solution comprising the somatostatin receptor binding peptide linked to a chelating agent, into the reactor, f. reacting the somatostatin receptor binding peptide linked to a chelating agent with said radionuclide in the reactor to obtain the radionuclide complex, g. recovering said radionuclide complex.

The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.

The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.

A method for producing a radiopharmaceutical, the method capable of maintaining a radioactive compound retaining a chemical structure and radioactivity at the time of production and after the production, and maintaining a usable period of a radiopharmaceutical; and a radiopharmaceutical are provided. The method for producing a radiopharmaceutical that has a radioactive component containing a radioactive dithiosemicarbazone copper complex includes: a stabilization step of adding a stabilizing agent containing at least one compound selected from the group consisting of ascorbic acid, methionine, sodium ascorbate, mannitol, and butylhydroxyanisole to a solution containing the radioactive component; and a filtration step of filtering the solution containing the radioactive component or a precursor thereof with a sterilization filter. In the radiopharmaceutical, a concentration of the radioactive component is 200 MBq/mL or more in terms of radioactivity concentrations.

The present disclosure concerns radiopharmaceutical compositions of radioactive halogenated benzylguanidine (such as radioiodinated MIBG) or a pharmaceutically acceptable salt, hydrate, or solvate thereof. In a preferred embodiment, the composition has at least 97% of radiochemical purity for at least 4 days. Advantageously, the compositions of the present disclosure may be devoid of parabens, which are carcinogenic and yet are used in known radioactive MIBG compositions. The present disclosure also provides processes of preparing a radioactive halogenated benzylguanidine composition. The compositions of the present disclosure can be used in diagnosis and treatment of various diseases.