AR126667A1 - STABILIZED RADIOISOTOPE COMPOSITIONS AND THEIR USES - Google Patents
STABILIZED RADIOISOTOPE COMPOSITIONS AND THEIR USESInfo
- Publication number
- AR126667A1 AR126667A1 ARP220102049A ARP220102049A AR126667A1 AR 126667 A1 AR126667 A1 AR 126667A1 AR P220102049 A ARP220102049 A AR P220102049A AR P220102049 A ARP220102049 A AR P220102049A AR 126667 A1 AR126667 A1 AR 126667A1
- Authority
- AR
- Argentina
- Prior art keywords
- conjugate
- targeting ligand
- chelating agent
- metal chelating
- radiopharmaceutical
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 8
- 239000012217 radiopharmaceutical Substances 0.000 abstract 7
- 229940121896 radiopharmaceutical Drugs 0.000 abstract 7
- 230000002799 radiopharmaceutical effect Effects 0.000 abstract 7
- 239000003381 stabilizer Substances 0.000 abstract 7
- 239000003446 ligand Substances 0.000 abstract 6
- 230000008685 targeting Effects 0.000 abstract 6
- 239000002738 chelating agent Substances 0.000 abstract 4
- 239000002184 metal Substances 0.000 abstract 4
- 239000008135 aqueous vehicle Substances 0.000 abstract 3
- 239000007788 liquid Substances 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 108050001286 Somatostatin Receptor Proteins 0.000 abstract 2
- 102000011096 Somatostatin receptor Human genes 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 2
- 239000008365 aqueous carrier Substances 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229940010982 dotatate Drugs 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 238000003608 radiolysis reaction Methods 0.000 abstract 1
- -1 small molecule compound Chemical class 0.000 abstract 1
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Abstract
En el presente documento, se proporcionan composiciones radiofarmacéuticas y sus usos. Las composiciones radiofarmacéuticas pueden comprender uno o más agentes estabilizadores, un vehículo acuoso y un conjugado que comprende un ligando de direccionamiento y una unión radioisotópica a un agente quelante de metales. El ligando de direccionamiento puede ser un compuesto de molécula pequeña o un péptido tal como un péptido monocíclico. El ligando de direccionamiento puede configurarse para unirse a un objetivo tumoral. El agente estabilizador puede comprender un estabilizador por radiólisis, un agente quelante de metales libre y/o un estabilizador de pH. En el presente documento, se proporcionan también métodos para preparar las composiciones radiofarmacéuticas y métodos para tratar el cáncer mediante la administración de las composiciones radiofarmacéuticas descritas. Reivindicación 1: Una composición radiofarmacéutica líquida que comprende: (a) un conjugado, caracterizado porque el conjugado es ²²⁵Ac-DOTA-TATE; (b) uno o más agentes estabilizantes y (c) un vehículo acuoso. Reivindicación 2: Una composición radiofarmacéutica líquida que comprende: (a) un conjugado, caracterizado porque el conjugado es ²²⁵Ac-DOTA-TOC; (b) uno o más agentes estabilizantes y (c) un vehículo acuoso. Reivindicación 3: Una composición radiofarmacéutica líquida que comprende: a) un conjugado caracterizado porque comprende (I) un ligando de direccionamiento, donde el ligando de direccionamiento se une a un receptor de somatostatina (SSR), (II) un agente quelante metálico unido por enlace covalente al ligando de direccionamiento y (III) un radionucleido, donde el radionucleido es ²²⁵Ac y está unido al agente quelante metálico; b) uno o más agentes estabilizantes y c) un vehículo acuoso.Provided herein are radiopharmaceutical compositions and their uses. Radiopharmaceutical compositions may comprise one or more stabilizing agents, an aqueous carrier, and a conjugate comprising a targeting ligand and a radioisotopic attachment to a metal chelating agent. The targeting ligand may be a small molecule compound or a peptide such as a monocyclic peptide. The targeting ligand can be configured to bind to a tumor target. The stabilizing agent may comprise a radiolysis stabilizer, a free metal chelating agent and/or a pH stabilizer. Also provided herein are methods for preparing the radiopharmaceutical compositions and methods for treating cancer by administering the described radiopharmaceutical compositions. Claim 1: A liquid radiopharmaceutical composition comprising: (a) a conjugate, characterized in that the conjugate is ²²⁵Ac-DOTA-TATE; (b) one or more stabilizing agents and (c) an aqueous vehicle. Claim 2: A liquid radiopharmaceutical composition comprising: (a) a conjugate, characterized in that the conjugate is ²²⁵Ac-DOTA-TOC; (b) one or more stabilizing agents and (c) an aqueous vehicle. Claim 3: A liquid radiopharmaceutical composition comprising: a) a conjugate characterized in that it comprises (I) a targeting ligand, wherein the targeting ligand binds to a somatostatin receptor (SSR), (II) a metal chelating agent linked by covalent bond to the targeting ligand and (III) a radionuclide, where the radionuclide is ²²⁵Ac and is linked to the metal chelating agent; b) one or more stabilizing agents and c) an aqueous vehicle.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202017665202A | 2020-02-04 | 2020-02-04 | |
| US202063329306P | 2020-04-08 | 2020-04-08 | |
| US202163228535P | 2021-08-02 | 2021-08-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR126667A1 true AR126667A1 (en) | 2023-11-01 |
Family
ID=89061550
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220102049A AR126667A1 (en) | 2020-02-04 | 2022-08-01 | STABILIZED RADIOISOTOPE COMPOSITIONS AND THEIR USES |
Country Status (1)
| Country | Link |
|---|---|
| AR (1) | AR126667A1 (en) |
-
2022
- 2022-08-01 AR ARP220102049A patent/AR126667A1/en unknown
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