# US 11,027,030 B2 · Kit for radiolabelling > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,027,030 B2 - Document ID: US11027030B2 - Status: Granted - Kind: B2 - Application number: 15/981,951 - Filed: 2018-05-17 - Published: 2018-09-20 - Granted: 2021-06-08 - Earliest claimed: 2014-08-29 - Assignees: Anmi S.A. - Applicants: Anmi S.A. - Inventors: Ludovic Wouters; Geoffroy Kaisin; André Luxen; Marc Léonard; Samuel Voccia - Web page: https://patentgrep.com/patent/US11027030B2 ## CPC - A61K 51/0482: {chelates from cyclic ligands, e.g. DOTA} - A61K 51/08: Peptides, e.g. proteins {, carriers being peptides, polyamino acids, proteins} - A61K 51/088: {conjugates with carriers being peptides, polyamino acids or proteins (antibodies A61K51/10)} - G01N 33/60: involving radioactive labelled substances - G21G 1/0005: {Isotope delivery systems (use of radioisotopes as tracers G21H5/02)} - A61K 2123/00: Preparations for testing in vivo - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q) - G21G: CONVERSION OF CHEMICAL ELEMENTS; RADIOACTIVE SOURCES (applications of radiation in general G21H5/00; handling particles, e.g. neutrons, or electromagnetic radiation not otherwise provided for G21K) ## Abstract The present invention relates to a kit for radiolabelling a targeting agent with gallium-68. The present invention also relates to the use of the kit for radiolabelling a targeting agent, and a method for radiolabelling a targeting agent with gallium-68 using the kit. ## Claims ### Claim 1 A radiolabelling kit comprising: a first vial, wherein said first vial is empty and under vacuum; a second vial, wherein said second vial comprises a suitable amount of acetate buffer for balancing the pH of an eluate from a gallium-68 generator to a pH value ranging from 3 to 5 when said eluate is eluted into the kit; and a third vial, wherein said third vial comprises a lyophilized chelate-functionalized targeting agent and a lyophilized metal inhibitor, wherein the chelator group of said chelate-functionalized targeting agent is selected from the group consisting of: NOTA, NODAGA, Tris(hydroxypyridinone) (THP), HBED, DFO 6SS, B6SS, PLED, YM103, and H2dedpa; and wherein said metal inhibitor is selected from the group consisting of: DOTA, tetra-tBu-DTPA, beta-cyclodextrin and a monosacccharide. ### Claim 2 (depends on 1) The radiolabelling kit according to claim 1, wherein the chelate-functionalized targeting agent is chelate-functionalized prostate-specific membrane antigen (PSMA)-targeting peptide. ### Claim 3 (depends on 1) The radiolabelling kit according to claim 1, wherein the monosaccharide is selected from the group consisting of glucose, fructose, and D-mannose. ### Claim 4 (depends on 1) The radiolabelling kit according to claim 1, wherein the kit comprises one or more of the list consisting of: a needleless transfer device for connecting two vials; an extension line comprising a proximal end adapted for connecting the extension line to a vial adapter and a distal end adapted for connecting the extension line to a needleless syringe; a vial adapter adapted for connecting an extension line or a needleless syringe to a vial; and a needleless syringe. ### Claim 5 (depends on 1) The radiolabelling kit according to claim 1, wherein the chelate-functionalized targeting agent is PSMA-11. ### Claim 6 (depends on 5) The radiolabelling kit according to claim 5, wherein the metal inhibitor is D-mannose. ### Claim 7 (depends on 1) An assembly comprising the radiolabeling kit according to claim 1 and a self-shielded device configured to hold said first vial. ### Claim 8 (depends on 7) The assembly according to claim 7, further comprising a gallium-68 generator. ### Claim 9 (depends on 7) The assembly according to claim 7, wherein the self-shielded device is invertible. ### Claim 10 (depends on 7) The assembly according to claim 7, wherein the self-shielded device comprises a support (2) and a container unit wherein said container unit comprises a container lid (3) and a container vessel (4) comprising a void space dimensioned to hold said first vial; and wherein the support comprises a base (1) and extending from the base and in fixed relation to the base at least one longitudinal member (6). ### Claim 11 (depends on 10) The assembly according to claim 10, wherein the dimensions of the void space suitable for holding the first vial are at most 10% larger than the dimensions of the first vial. ### Claim 12 (depends on 10) The assembly according to claim 10, wherein the at least one longitudinal member (6) is provided in revolute attachment with respect to the container vessel (4), where an axis of rotation is horizontal, non-parallel to a central axis of the first vial and/or parallel to an underside of the base (1). ### Claim 13 (depends on 10) The assembly according to claim 10, wherein the container lid (3) is in revolute attachment with respect to the container vessel (4), where an axis of rotation is vertical, parallel to a central axis of the first vial and/or non-parallel to an underside of the base (1). ### Claim 14 (depends on 10) The assembly according to claim 10, wherein the container unit is provided with a channel configured to hold a dismountable conduit for connecting the first vial within the self-shielding device to an environment external of the self-shielded device, wherein the channel configured to hold a dismountable conduit is provided at the interface of the container lid (3) and the container vessel (4). ### Claim 15 (depends on 7) The assembly according to claim 7, wherein the chelate-functionalized targeting agent is PSMA-11. ### Claim 16 (depends on 15) The assembly according to claim 15, wherein the metal inhibitor is D-mannose.