Abrégé

The present disclosure relates to αvβ3 and/or αvβ5 integrins antagonist radiopharmaceuticals and their use in a theragnostic approach for selection and therapy of human subjects with tumors overexpressing αvβ3 and/or αvβ5 integrins. In particular, the present disclosure relates to a pharmaceutical composition of αv 177Lu radiolabeled αvβ3 and/or αvβ5 integrins antagonist, for use in treating tumors overexpressing αvβ3 and/or αvβ5 integrins in a human subject eligible for said treatment, wherein said subject has been selected for the treatment by PET/CT or PET/MRI or SPECT/CT or SPECT/MRI imaging with the same αvβ3 and/or αvβ5 integrins antagonist but with 68-Ga as radiometal for use as imaging agent.

Classes IPC  ?

• A61K 51/04 - Composés organiques

Abrégé

The present disclosure relates to prostate specific membrane antigen (PSMA) ligands. In particular, the disclosure relates to PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal. The disclosure also relates to the use of these compounds in imaging and in the treatment of prostate cancer.

Classes IPC  ?

• A61K 51/04 - Composés organiques
• A61P 35/00 - Agents anticancéreux

Abrégé

The present disclosure relates to ?v?3 and/or ?v?5 integrins antagonist radiopharmaceuticals and their use in a theragnostic approach for selection and therapy of human subjects with tumors overexpressing ?v?3 and/or ?v?5 integrins. In particular, the present disclosure relates to a pharmaceutical composition of ?v 177Lu radiolabeled ?v?3 and/or ?v?5 integrins antagonist, for use in treating tumors overexpressing ?v?3 and/or ?v?5 integrins in a human subject eligible for said treatment, wherein said subject has been selected for the treatment by PET/CT or PET/MRI or SPECT/CT or SPECT/MRI imaging with the same ?v?3 and/or ?v?5 integrins antagonist but with 68-Ga as radiometal for use as imaging agent.

Classes IPC  ?

• A61K 51/04 - Composés organiques

Abrégé

The present disclosure relates to αvβ3 and/or αvβ5 integrins antagonist radiopharmaceuticals and their use in a theragnostic approach for selection and therapy of human subjects with tumors overexpressing αvβ3 and/or αvβ5 integrins. In particular, the present disclosure relates to a pharmaceutical composition of αv 177Lu radiolabeled αvβ3 and/or αvβ5 integrins antagonist, for use in treating tumors overexpressing αvβ3 and/or αvβ5 integrins in a human subject eligible for said treatment, wherein said subject has been selected for the treatment by PET/CT or PET/MRI or SPECT/CT or SPECT/MRI imaging with the same αvβ3 and/or αvβ5 integrins antagonist but with 68-Ga as radiometal for use as imaging agent.

Classes IPC  ?

• A61K 51/04 - Composés organiques
• A61P 35/00 - Agents anticancéreux

Abrégé

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.

Classes IPC  ?

• C07K 1/13 - Marquage de peptides
• A61K 51/04 - Composés organiques
• A61K 51/08 - Peptides, p. ex. protéines
• A61K 51/12 - Préparations contenant des substances radioactives utilisées pour la thérapie ou pour l'examen in vivo caractérisées par un aspect physique particulier, p. ex. émulsion, microcapsules, liposomes
• C07K 14/655 - Somatostatines
• A61K 9/08 - Solutions

Abrégé

The present invention relates to combination therapies of radiolabelled somatostatin receptor binding compounds with PARR inhibitors.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines
• A61K 31/502 - PyridazinesPyridazines hydrogénées condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. cinnoline, phtalazine
• A61P 35/00 - Agents anticancéreux
• A61K 51/04 - Composés organiques

Abrégé

The present disclosure relates to methods for radiolabelling PSMA binding ligands with a radioactive isotope, preferably 68Ga, 67Ga or 64Cu, and their kits.

Classes IPC  ?

• A61K 51/04 - Composés organiques
• A61K 51/12 - Préparations contenant des substances radioactives utilisées pour la thérapie ou pour l'examen in vivo caractérisées par un aspect physique particulier, p. ex. émulsion, microcapsules, liposomes
• C07B 59/00 - Introduction d'isotopes d'éléments dans les composés organiques
• A61K 103/00 - Métaux radioactifs
• A61K 103/30 - Terres rares

Abrégé

The present invention relates to methods for labeling a PSMA binding ligand with a radioactive isotope, preferably 68Ga, 67Ga or 64Cu, said method comprising the steps of: i. providing a single vial comprising, in dried form, said PSMA binding ligand of 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.

Classes IPC  ?

• A61K 51/04 - Composés organiques
• A61K 51/12 - Préparations contenant des substances radioactives utilisées pour la thérapie ou pour l'examen in vivo caractérisées par un aspect physique particulier, p. ex. émulsion, microcapsules, liposomes
• C07B 59/00 - Introduction d'isotopes d'éléments dans les composés organiques
• A61K 103/00 - Métaux radioactifs
• A61K 103/30 - Terres rares

Abrégé

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.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines
• A61K 51/04 - Composés organiques
• A61K 9/08 - Solutions

Abrégé

The present disclosure relates to gastrin-releasing peptide receptor (GRPR) targeting pharmaceuticals and their use in a theragnostic approach for selection and therapy of subjects with GRPR-expressing malignancies. In particular, the present disclosure relates to a pharmaceutical composition of a radiolabeled GRPR-antagonist, for use in treating GRPR-positive tumors in a human subject selected for said treatment, wherein said subject has been selected for the treatment by PET/CT or PET/MRI imaging with a corresponding 68Ga-labelled GRPR antagonist as contrast agent.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines
• A61P 35/00 - Agents anticancéreux
• A61K 103/00 - Métaux radioactifs
• A61K 103/30 - Terres rares

Abrégé

The present disclosure 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.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines
• A61K 51/12 - Préparations contenant des substances radioactives utilisées pour la thérapie ou pour l'examen in vivo caractérisées par un aspect physique particulier, p. ex. émulsion, microcapsules, liposomes
• A61K 103/30 - Terres rares

Abrégé

The present invention relates to methods for radiolabelling GRPR antagonists such as NeoB, and their kits. In particular, the invention to a method for labeling a gastrin-releasing peptide receptor (GRPR) antagonist with a radioactive isotope, preferably 68Ga, 67Ga or 64Cu, said method comprising the steps of: i. providing a first vial comprising said GRPR antagonist in dried form, ii. adding a solution of said radioactive isotope into said first vial, thereby obtaining a solution of said GRPR antagonist with said radioactive isotope, iii. mixing the solution obtained in ii. with at least a buffering agent and incubating it for a sufficient period of time for obtaining said GRPR antagonist labeled with said radioactive isotope, and, iv. optionally, adjusting the pH of the solution.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines
• A61K 51/12 - Préparations contenant des substances radioactives utilisées pour la thérapie ou pour l'examen in vivo caractérisées par un aspect physique particulier, p. ex. émulsion, microcapsules, liposomes
• A61K 103/00 - Métaux radioactifs

Abrégé

The present disclosure relates to prostate specific membrane antigen (PSMA) ligands. In particular, the disclosure relates to PSMA ligands having a glutamate-urea- lysine (GUL) moiety, a radioisotope and a chelating agent that can comprise a radiometal.

Classes IPC  ?

• A61K 51/04 - Composés organiques
• A61P 35/00 - Agents anticancéreux
• A61K 101/02 - Halogènes

Abrégé

The present disclosure relates to prostate specific membrane antigen (PSMA) ligands. In particular, the disclosure relates to PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal. The disclosure also relates to the use of these compounds in imaging and in the treatment of prostate cancer.

Classes IPC  ?

• A61K 51/04 - Composés organiques
• A61P 35/00 - Agents anticancéreux
• C07D 257/02 - Composés hétérocycliques contenant des cycles comportant quatre atomes d'azote comme uniques hétéro-atomes du cycle non condensés avec d'autres cycles

Abrégé

The present disclosure relates to prostate specific membrane antigen (PSMA) ligands. In particular, the disclosure relates to PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal. The disclosure also relates to the use of these compounds in imaging and in the treatment of prostate cancer.

Classes IPC  ?

• A61K 51/04 - Composés organiques
• A61P 35/00 - Agents anticancéreux
• A61K 103/00 - Métaux radioactifs
• A61K 103/30 - Terres rares

Abrégé

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.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines
• C07B 59/00 - Introduction d'isotopes d'éléments dans les composés organiques

Abrégé

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.

Classes IPC  ?

• C07B 59/00 - Introduction d'isotopes d'éléments dans les composés organiques
• A61K 51/08 - Peptides, p. ex. protéines

Abrégé

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.

Classes IPC  ?

• C07B 59/00 - Introduction d'isotopes d'éléments dans les composés organiques
• A61K 51/08 - Peptides, p. ex. protéines

Abrégé

The present invention relates to combination therapies of radiolabelled somatostatin receptor binding compounds with PARR inhibitors.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines
• A61K 31/502 - PyridazinesPyridazines hydrogénées condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. cinnoline, phtalazine
• A61P 35/00 - Agents anticancéreux
• A61K 103/30 - Terres rares

Abrégé

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.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines

Abrégé

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.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines

Abrégé

The present invention relates to methods of treating cancers that overexpress somatostatin receptors, e.g. neuroendocrine tumors (NET). In particular, the invention provides novel therapies based on the combination of a peptide receptor radionuclide therapeutic (PRRT) agent and immuno-oncology (I-O) therapeutic agents, wherein said I-O therapeutic agents are selected from the group consisting of LAG-3 inhibitors, TIM-3 inhibitors, GITR angonists, TGF-β inhibitors, IL15/IL-15RA complex, and selected PD-1 inhibitors.

Classes IPC  ?

• A61K 51/08 - Peptides, p. ex. protéines
• A61P 35/00 - Agents anticancéreux
• A61K 103/30 - Terres rares