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64Cu labeled PSMA targeted inhibitor as well as preparation method and application thereofCu

An inhibitor and targeting technology, applied in the field of nuclear medicine, can solve problems such as short half-life, achieve stable properties, good retention effect, and good imaging effect

Inactive Publication Date: 2018-06-22
BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 18 Although F-NODA-PSMA can accurately provide lesion information and metastasis, if it is used to guide surgery, it still has the disadvantage of a relatively short half-life

Method used

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  • 64Cu labeled PSMA targeted inhibitor as well as preparation method and application thereofCu
  • 64Cu labeled PSMA targeted inhibitor as well as preparation method and application thereofCu
  • 64Cu labeled PSMA targeted inhibitor as well as preparation method and application thereofCu

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 164

[0026] Example 1 64 Cu-labeled PSMA targeting inhibitor (ie 64 Preparation of Cu-NODA-PSMA)

[0027] Add 5 μL NODA-PSMA (4 mM), 200 μL NaAc (0.1M) and 50 μL 64 CuCl 2 370MBq), shake well, and react at 95°C for 15 minutes to obtain the target compound, namely 64 Cu-labeled PSMA-targeting inhibitor. After the reaction, use Sep-pak C18Column Light to separate and purify the target compound. Before use, Sep-pak C18Column Light needs to be activated with absolute ethanol and high-purity water, and the radioactive impurities are eluted with water, and finally the target compound is eluted with 80% ethanol compound, passed through a 0.2 μm sterile filter, and prepared an injection with physiological saline.

[0028] 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 (B); 0-10min (B): 15%-60%. figure 1 The results show that after purification by Sep-PakC18Light...

Embodiment 264

[0029] Example 2 64 In Vitro Stability Analysis of Cu-NODA-PSMA Labeled Compounds

[0030] Get 20 μ L (1.3MBq) of embodiment 1 preparation 64 Cu-NODA-PSMA was added to 1 mL of normal saline, and incubated at room temperature for 6 hours. After 24 hours and 40 hours, an appropriate amount of solution was taken out for Radio-HPLC detection. the result shows 64 Cu-NODA-PSMA still has high radiochemical purity after being placed at room temperature for 40 hours, and the HPLC detection results after incubation for 40 hours are shown in figure 2 .

[0031]Take 20μL (1.3MBq) of separation sample 64 Cu-NODA-PSMA was added to 1 mL of 5% human serum albumin (HAS) solution and incubated at 37°C for 2 hours. After 13 hours and 36 hours, an appropriate amount of the solution was taken out for Radio-HPLC detection. the result shows, 64 Cu-NODA-PSMA still has high radiochemical purity after incubation in HSA at 37°C for 36 hours. The HPLC results after incubation for 36 hours are show...

Embodiment 364

[0032] Example 3 64 Biodistribution Experiment of Cu-NODA-PSMA in Normal Mice

[0033] Take 12 normal Kunming female mice and inject 0.2mL prepared in Example 1 through the tail vein respectively. 64 Cu-NODA-PSMA (18.5MBq) was sacrificed by cervical dislocation 50 minutes, 30 minutes, 60 minutes and 120 minutes after injection, respectively, and the heart, liver, lung, kidney, spleen, stomach, muscle, bone, blood, The large intestine, small intestine and other related tissues and organs were wiped and weighed, and the radioactivity count was measured by γ-Counter. There were 3 mice in each phase. The percent injected dose per gram (%ID / g) of each tissue was calculated, and the results are shown in Table 1.

[0034] Table 1 64 Biodistribution of Cu-NODA-PSMA in normal mice (ID% / g, x±SD, n=3)

[0035]

[0036] the result shows, 64 Cu-NODA-PSMA is rapidly cleared in the blood, rapidly metabolized by the kidneys and out of the body through the urinary tract, and has low u...

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Abstract

The invention provides a novel 64Cu labeled PSMA targeted inhibitor as well as a preparation method and an application thereof. The 64Cu labeled PSMA targeted inhibitor is a 64Cu labeled NODA-PSMA conjugate; the inhibitor, when used as a prostate PET molecular probe, is good in stability and good in developing effect; the inhibitor is conducive to diagnosis and accurate staging of early prostate and is beneficial for guiding surgical resection; and the inhibitor can offer a diagnosis basis for recurrence as well as local and distant metastasis of the prostate; therefore, the inhibitor has an important clinical application value.

Description

technical field [0001] The present invention relates to the field of nuclear medicine, in particular, to a 64 Cu-labeled PSMA targeting inhibitor and its preparation method and application. Background technique [0002] With the intensification of population aging process, the incidence of prostate cancer has ranked sixth in the incidence of male malignant tumors in my country. Surgery is an important means of prostate cancer treatment. How to accurately resect the lesion is the doctor's choice. The important problem is that nuclear medicine molecular probes can perform specific imaging on lesions, and the lesions can be detected by hand-held radioactive detectors, so as to guide surgical resection. However, due to the physiological non-specific uptake of molecular probes in the body, this will not only affect the detection of lesions but also cause unnecessary radiation to the operator to a certain extent. The lesions were highly specific and had good tumor uptake and high...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61K103/00
CPCA61K51/08
Inventor 杨志刘特立朱华
Owner BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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