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Prostate-specific antigen targeting inhibitor of nuclide marker and preparation method of nuclide marker

A prostate-specific membrane antigen technology, applied in the field of nuclear medicine, to achieve stable properties, good imaging effects, high affinity and functional activity

Pending Publication Date: 2016-11-09
BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, metabolic imaging in molecular nuclear medicine is the most widely used clinically, and the most common one is 18 F-FDG, but because it is a non-specific imaging agent, has many deficiencies in the diagnosis of prostate cancer, so it is urgent to develop specific receptors for prostate cancer imaging, so as to truly take advantage of PET imaging

Method used

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  • Prostate-specific antigen targeting inhibitor of nuclide marker and preparation method of nuclide marker
  • Prostate-specific antigen targeting inhibitor of nuclide marker and preparation method of nuclide marker
  • Prostate-specific antigen targeting inhibitor of nuclide marker and preparation method of nuclide marker

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 Novel nuclide 64 Cu, 89 Preparation of Zr-labeled DKFZ-PSMA-617

[0024] To 10 μg of DKFZ-PSMA-617, add 0.2 mL of 0.1 M NaAC at pH 4.5-5.5 and 92.5 MBq of 64 CuCl 2 or 89 Zr 4+ The eluent was reacted at 95°C for 15 minutes to obtain the target compound 64 Cu-PSMA-617 or 89 Zr-PSMA-617.

[0025] When the labeling rate is less than 90%, the target compound is separated and purified by Sep-pak C18Column, so that the radiochemical purity of the target compound is greater than 99%.

[0026] Before use, the Sep-pak column needs to be activated with 5mL of absolute ethanol and 5mL of high-purity water, and the radioactive impurities are eluted with 3mL of normal saline, and then the target compound is eluted with 0.8mL of 80% ethanol 64 Cu-PSMA-617 or 89 Zr-PSMA-617.

[0027] The labeling rate and radiochemical purity were determined by Radio-HPLC. Analysis conditions: YMC-Pack ODS-A column, 1.0mL / min; 0.1% TFA Water (A), 0.1% TFA Acetontrile (C); 0-10min...

Embodiment 264

[0028] Example 2 64 In Vitro Stability Analysis of Cu-PSMA-617 Labeled Compounds

[0029] Take 20μL (1.3MBq) of separated sample 64 Cu-PSMA-617 was added to 1mL NaCl buffer solution, incubated at 30°C, and 25μL, 30μL, 40μL, 55μL, and 99μL were taken out at 5min, 30min, 1h, 2h, and 28h for Radio-HPLC detection. see results figure 2 , the results show that the compound 64 Cu-PSMA-617 has good stability.

Embodiment 364

[0030] Example 3 64 PET Imaging Test of Cu-PSMA-617 Labeled Compound in Animals

[0031] Take BALB / c nude mice (ten weeks old) implanted with human gastric adenocarcinoma BGC-823 cells in the armpit of the right upper limb, the tumor diameter is 1.0-2.0cm, and inject 18.5MBq of 64 Cu-PSMA-617-labeled compound 0.2mL was injected for PET imaging at 30min, 8h and 24h respectively. Before imaging, nude mice were anesthetized with oxygen mixed with 3% (volume fraction) isoflurane in the Summit AS-1-000-7 small animal anesthesia system, and 1% (volume fraction) isoflurane was maintained during the imaging process. Oxygen anesthesia with alkane, imaging time was 15min. see results image 3 .

[0032] Additionally, for compounds 89 The detection and analysis results of Zr-PSMA-617 showed that it was compatible with the compound 64 The in vitro stability and imaging effect of Cu-PSMA-617 are similar.

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Abstract

The invention provides a prostate-specific antigen targeting inhibitor of a nuclide marker. The targeting inhibitor is DKFZ-PSMA-617 of a radioactive nuclide marker. Radioactive nuclide includes at least one of 64Cu, 68Ga and 89Zr. The invention further provides a preparation method of the nuclide marker DKFZ-PSMA-617. The nuclide marker DKFZ-PSMA-617 is stable in property and good in development effect, has high affinity and functional activity on PSMA, is beneficial to diagnosis and accurate staging of early prostate cancer, and provides a new thought for diagnosis of breast cancer and gastric adenocarcinoma. Further preclinical animal level research proves that the inhibitor is expected to become a targeting PSMA developing agent and a tumor treatment agent with good application prospects.

Description

technical field [0001] The invention relates to the field of nuclear medicine, in particular to a nuclide-labeled prostate-specific membrane antigen targeting inhibitor and a preparation method thereof. Background technique [0002] With the in-depth development and integration of nuclear medicine and molecular biology, medical imaging technology has entered the era of molecular imaging, in which functional imaging by Positron Emission Tomography (PET) enables people to truly understand the Begin to recognize and diagnose diseases, especially highlight its advantages in the diagnosis and treatment of tumors. By tracking the changes of receptors in diseased tissues and the abnormality of cell signal transduction, it can overcome the defects in modern diagnostic techniques, provide the basis for early diagnosis of tumors, clinical staging, and curative effect evaluation, and evaluate the prognosis. Targeted therapy for tumors. [0003] At present, metabolic imaging in molecu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08A61K51/04A61P35/00A61P13/08A61K103/34
CPCA61K51/0482A61K51/088
Inventor 杨志韩雪迪朱华刘辰刘菲解清华
Owner BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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