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

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]...

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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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