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Technetium-99m-labeled FAPI derivative containing D-proline modification as well as preparation method and application of technetium-99m-labeled FAPI derivative

A -99m, proline technology, 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: 2022-03-11
BEIJING NORMAL UNIVERSITY
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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 as liver and kidney, and the uptake value of the tumor needs to be improved Therefore, it is of great practical significance to develop 99mTc-labeled FAPI tumor imaging agent with better performance

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  • Technetium-99m-labeled FAPI derivative containing D-proline modification as well as preparation method and application of technetium-99m-labeled FAPI derivative
  • Technetium-99m-labeled FAPI derivative containing D-proline modification as well as preparation method and application of technetium-99m-labeled FAPI derivative
  • Technetium-99m-labeled FAPI derivative containing D-proline modification as well as preparation method and application of technetium-99m-labeled FAPI derivative

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[0017] The present invention is described in detail below by way of examples: a technetium-99m labeled FAPI derivative containing D-proline modification with technetium-99m, the general structural formula is 99m Tc(HYNIC-DP-FAPI)(tricine / TPPTS), its structural formula is as follows:

[0018]

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

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

[0021] a. Synthesis of HYNIC-DP-FAPI

[0022] Weigh 33 mg (0.068 mmol) of FAPI into a round bottom flask, add 1 mL of DMF to dissolve, then add 0.120 mL (0.90 mmol) of triethylamine and 45 mg (0.084 mmol) of compound 1, and react at 60°C for 6 hours. After the reaction, the solvent was...

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Abstract

The invention discloses a technetium-99m labeled FAPI derivative containing D-proline modification and a preparation method and application of the technetium-99m labeled FAPI derivative containing D-proline modification, wherein the structural general formula of the technetium-99m labeled FAPI derivative is 99mTc (HYNIC-DP-FAPI) (Tricine / TPPTS). The < 99m > Tc (HYNIC-DP-FAPI) (trickine / TPPTS) complex is prepared by the following two steps: synthesis of a ligand HYNIC-DP-FAPI and preparation of the < 99m > Tc (HYNIC-DP-FAPI) (trickine / TPPTS), and the < 99m > Tc (HYNIC-DP-FAPI) (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, in particular to a technetium-99m labeled FAPI derivative containing D-proline modification, a preparation method and an 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] The linker connects the targe...

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Application Information

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IPC IPC(8): C07F13/00C07D401/14A61K51/04A61K103/10
CPCC07F13/005C07D401/14A61K51/0482Y02P20/55
Inventor 张俊波阮晴王倩娜江雨豪冯俊红王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
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