Technetium-99m labeled FAPI derivative modified by D-proline glycine containing polypeptide as well as preparation method and application of technetium-99m labeled FAPI derivative modified by D-proline glycine containing polypeptide

A technology of proline glycine, -99m, applied in the field of FAPI derivatives and preparation, can solve the problems of tumor uptake value to be improved and high uptake

Active Publication Date: 2022-05-10
BEIJING NORMAL UNIVERSITY
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  • Description
  • Claims
  • Application Information

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Problems solved by technology

In 2020, our research group developed a technetium-99m-labeled isocyanide-containing FAPI derivative (patent number: ZL202011382815.2), but the drug has high uptake in non-target organs such a...

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  • Technetium-99m labeled FAPI derivative modified by D-proline glycine containing polypeptide as well as preparation method and application of technetium-99m labeled FAPI derivative modified by D-proline glycine containing polypeptide
  • Technetium-99m labeled FAPI derivative modified by D-proline glycine containing polypeptide as well as preparation method and application of technetium-99m labeled FAPI derivative modified by D-proline glycine containing polypeptide
  • Technetium-99m labeled FAPI derivative modified by D-proline glycine containing polypeptide as well as preparation method and application of technetium-99m labeled FAPI derivative modified by D-proline glycine containing polypeptide

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Embodiment Construction

[0017] The present invention is described in detail below through the examples: a technetium-99m labeled FAPI derivative containing D-proline glycine polypeptide modification, the structural formula is 99m Tc(HYNIC-PG n -FAPI)(tricine / TPPTS)(n=2), its structural formula is as follows:

[0018]

[0019] In the structural formula: HYNIC-PG 2 -The nitrogen atom on the hydrazine group in the FAPI molecule, the phosphorus atom in the co-ligand TPPTS, and the oxygen and nitrogen atoms in the tricine and 99m Tc coordinates to get 99m Tc(HYNIC-PG 2 -FAPI) (tricine / TPPTS) complex.

[0020] 99m Tc(HYNIC-PG 2 -FAPI) (tricine / TPPTS) complex preparation method, its preparation steps are as follows:

[0021] a. HYNIC-PG 2 - Synthesis of FAPI

[0022] Weigh 50mg (0.10mmol) FAPI in a round bottom flask, add 2mL DMF to dissolve, then add 78mg (0.12mmol) compound 1, 41mg (0.20mmol) dicyclohexylcarbodiimide (DCC), 14mg (0.10mmol) ) 1-hydroxybenzotriazole (HOBt) and 10.17mL (1.00mmol...

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Abstract

The invention discloses a technetium-99m labeled FAPI derivative containing D-proline glycine polypeptide modification and a preparation method and application of the technetium-99m labeled FAPI derivative containing D-proline glycine polypeptide modification, wherein the structural general formula of the technetium-99m labeled FAPI derivative is 99mTc (HYNIC-PGn-FAPI) (Tricine/TPPTS). The < 99m > Tc (HYNIC-PGn-FAP) (trickine/TPPTS) complex is prepared by the following two steps: synthesis of a ligand HYNIC-PGn-FAPI and preparation of the < 99m > Tc (HYNIC-PGn-FAP) (trickine/TPPTS), and the < 99m > Tc (HYNIC-PGn-FAP) (trickine/TPPTS) complex is obtained. The complex is simple and convenient to prepare, high in radiochemical purity and good in stability, has very high uptake and target-to-non-target ratio at the tumor site of a U87MG tumor-bearing mouse, has specific binding with FAP in tumors, and is a novel tumor radiopharmaceutical with clinical application value.

Description

technical field [0001] The invention belongs to the field of radiopharmaceuticals, and in particular relates to technetium-99m-labeled FAPI derivatives modified with D-proline-glycine-containing polypeptides, a preparation method and application. Background technique [0002] Fibroblast activating protein (FAP) is a potential target for tumor detection and treatment. Radionuclide-labeled fibroblast activating protein inhibitor (FAPI) and its derivatives are used as tumor imaging agents and become the focus of current international radiopharmaceutical research. A big hit. In 2020, our research group developed a technetium-99m-labeled isocyanide-containing FAPI derivative (patent number: ZL202011382815.2), but the drug has high uptake in non-target organs such as liver and kidney, and the uptake value of the tumor needs to be improved Insufficient, so the development of better performance 99m Tc-labeled FAPI tumor imaging agent has important practical significance. [0003]...

Claims

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Application Information

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IPC IPC(8): C07K5/02C07K7/02C07K1/02A61K51/08A61K103/10
CPCC07K5/0202C07K7/02A61K51/08Y02P20/55
Inventor 张俊波阮晴王倩娜江雨豪冯俊红王学斌唐志刚张站斌陆洁
Owner BEIJING NORMAL UNIVERSITY
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