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Novel radionuclide labelled somatostatin analogue molecular probe and application thereof

A radionuclide and molecular probe technology, applied in the field of radionuclide-labeled molecular probes, can solve problems such as low affinity and missed diagnosis of tumors

Inactive Publication Date: 2015-04-08
BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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Problems solved by technology

However, these two analogues also have limitations in clinical application. It has been reported in the literature that octreotide only has a high affinity for SSTR2, but not for SSTR1, 3, 4, and 5. However, about 30% of SSTR-positive tumors express non- SSTR2, but expressing SSTR1, 3, 4, 5 receptors, somatostatin receptor imaging with octreotide may result in missed diagnosis of these tumors

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  • Novel radionuclide labelled somatostatin analogue molecular probe and application thereof
  • Novel radionuclide labelled somatostatin analogue molecular probe and application thereof
  • Novel radionuclide labelled somatostatin analogue molecular probe and application thereof

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Embodiment 1

[0032] (1) Carry out BCA modification on the somatostatin analog Pasireotide, retain one of the genes containing n-butylamine structure, and perform polypeptide modification on the other short-chain primary amine, using benzyl isothiocyanate-1, After modification with bifunctional chelating agents such as 4,7-triazacyclonona-1,4,7-tricarboxylic acid (NCS-Bz-DOTA) or NCS-Bz-DTPA, NCS-Bz-NOTA, carry out 68 Ga(T 1 / 2 = 68min; β + :1.9MeV) or 177 Lu(T 1 / 2 = 6.7d; β - : 0.497MeV) and other radioactive radionuclide imaging. The formation of SSTR-targeted molecular probes can be used for research on the diagnosis and treatment of neuroendocrine tumors.

[0033] (2) the aforementioned 68 Ga-labeled novel somatostatin analogs and their preparation method, sequentially add 19.5 μL NaAc (1mol / L) to 2 μL of labeled precursor DOTA-pasireotide (5 mg / mL), 92.5 MBq 68 GaCl 3 The eluate was reacted at 100°C for 20 minutes, and when the labeling rate was less than 90%, it was separated a...

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Abstract

The invention provides a novel radionuclide labelled somatostatin analogue molecular probe and its application and belongs to the field of radiopharmaceuticals labelling and nuclear medicine technologies. A bifunctional chelator couples cyclic polypeptide Pasireotide, and then radionuclide is used for labelling so as to obtain a radionuclide labelled neuroendocrine neoplasm specific somatostatin analogue radioactive molecular probe. The molecular probe can be combined with a tumor expression somatostatin receptor (SSTR), and SSTR positive tumor tissue can be accurately positioned by means of nuclear medicine. Thus, the purpose of disease target molecular imaging diagnosis and treatment is achieved. The synthesized molecular probe has higher affinity and functional activity for SSTR and is expected to become a somatostatin analogue developer and tumor therapeutic agent with a good prospect.

Description

technical field [0001] The invention relates to the technical fields of radiopharmaceutical labeling and nuclear medicine, in particular to a radionuclide-labeled molecular probe and its application. Background technique [0002] With the development of nuclear medicine, the application of molecular imaging, especially positron emission tomography (PET), has shown great potential and advantages in tumor diagnosis and treatment. Neuroendocrine tumors are a group of heterogeneous tumors originating from peptidergic neurons and neuroendocrine cells. Most neuroendocrine tumor cells express somatostatin receptors (SSTRs), currently positron radionuclides 68 Ga-labeled somatostatin analogs are widely used in clinical imaging of neuroendocrine tumors, which are helpful for early diagnosis and prognosis evaluation of tumors. 177 Lu, with a half-life of 6.7 days, not only emits β - Rays also emit gamma rays, and their drug research in the field of nuclear medicine therapy is very e...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61K49/00A61K103/00A61K101/02A61K103/10A61K103/20
Inventor 杨志刘菲朱华
Owner BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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