Prostate cancer PET diagnostic reagent 68Ga-NOTA-ANCP-PSMA and preparation method and application thereof

A technology of NOTA-ANCP-PSMA, 68ga-nota-ancp-psma, applied in the preparation methods of peptides, chemical instruments and methods, preparations for in vivo tests, etc. protection and other issues, to achieve the effect of fast marking speed, high marking rate and good stability

Active Publication Date: 2019-10-08
HTA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] PSMA-11 has been widely used clinically, and is not protected by patents, and has achieved good results, but it is suitable for diagnosis and not suitable for targeted therapy

Method used

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  • Prostate cancer PET diagnostic reagent 68Ga-NOTA-ANCP-PSMA and preparation method and application thereof
  • Prostate cancer PET diagnostic reagent 68Ga-NOTA-ANCP-PSMA and preparation method and application thereof
  • Prostate cancer PET diagnostic reagent 68Ga-NOTA-ANCP-PSMA and preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] This embodiment provides a prostate cancer PET diagnostic reagent 68 The preparation method of Ga-NOTA-ANCP-PSMA, described method comprises the steps:

[0042] (S1) The precursor compound NOTA-ANCP-PSMA is synthesized by solid phase synthesis;

[0043] Preparation of compound 3

[0044] The synthetic route is shown below. Using Fmoc-Lys(Dde)-Wang Resin (compound 1) as the starting material, weigh 3g of the raw material with a substitution degree of 0.3mmol / g, add it to the reactor, add DMF, and soak for 30min. Then drain the DMF, add 3 times the volume of 20% Pip / DMF, and fill with nitrogen gas to remove Fmoc, react for 30 minutes, drain the 20% Pip / DMF, wash with DMF 5 times, and the ninhydrin detection shows dark blue. Add N,N'-succinimidyl carbonate (DSC), N,N-diisopropylethylamine (DIPEA) and 4-dimethylaminopyridine (DMAP) in proportion, and the input ratio is resin:DSC: DIPEA:DMAP=1:6:12:1, add an appropriate amount of DMF, and react for 1 h under nitrogen prot...

Embodiment 2

[0059] In vitro stability assay:

[0060] 68 The radiochemical stability of Ga-NOTA-ANCP-PSMA was carried out in two systems of calf serum and phosphate buffer. PBS method: place in 0.5mL phosphate buffer (PBS, pH=7.4), place at 37°C, incubate for 30, 60, 90, 120, 150min, then use HPLC to measure its radiochemical purity to determine its in vitro stability. Serum method: place in 0.5mL calf serum solution, incubate at pH=7, 37°C. When incubated for 30, 60, 90, 120, and 150 min, the radiochemical purity was determined by HPLC to determine its in vitro stability.

[0061] Such as Figure 4 as shown, 68 The stability of Ga-NOTA-ANCP-PSMA in PBS system was good, and the radiochemical purity remained above 95.4% until 150min. The in vitro stability results in the BSA system showed that the radiochemical purity could be maintained at a level above 95% within 90 minutes, and then decreased slightly. illustrate 68 The stability of Ga-NOTA-ANCP-PSMA in BSA is poorer than that i...

Embodiment 3

[0063] Measurement of lipid-water partition coefficient:

[0064] Mark 68 Ga-NOTA-ANCP-PSMA was separated and purified by Sep-Pak C18 Cartridge, and eluted with 95% ethanol. The obtained marker was blown dry by dry nitrogen, and the obtained marker was dissolved in a 1.5mL EP tube (about 3.7MBq) using the same volume (0.5mL: 0.5mL) of n-octanol and phosphate buffer solution (pH=7.4) middle. Fully shake for 5 minutes, and centrifuge the layers in a centrifuge for 5 minutes at a speed of 2000 rpm. Take 100uL each of the organic phase and the aqueous phase in 1mL EP tubes, measure their radioactive counts in the well-type γ detector, and calculate the lipid-water partition coefficient P from the ratio of the radioactive counts of the organic phase and the aqueous phase. P=log(N o / N W )(N o and N W are the counts of the organic and aqueous phase samples, respectively). The operation was repeated 3 times, and the average value was taken as the lipid-water partition coeffic...

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Abstract

The invention discloses a prostate cancer PET diagnostic reagent 68Ga-NOTA-ANCP-PSMA and a preparation method and an application thereof. A structural formula of the 68Ga-NOTA-ANCP-PSMA is shown as the specification, and the preparation method comprises the following steps: (S1) synthesis of a precursor compound NOTA-ANCP-PSMA by a solid phase synthesis method; and (S2) 68Ga radiolabeling by usinga direct labeling method. The 68Ga-NOTA-ANCP-PSMA has the characteristics of fast labeling speed and high marking rate, and has the advantages of good stability, good hydrophilicity, high sensitivityand high specificity. In addition, 68Ga-NOTA-ANCP-PSMA can be rapidly cleared in the blood and has higher tumor uptake.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a prostate cancer PET diagnostic reagent 68 Ga-NOTA-ANCP-PSMA and its preparation method and application. Background technique [0002] Prostate cancer is the most common malignant tumor in men. As of 2018, there were 427,500 new cases worldwide every year, and the annual death toll from prostate cancer reached 361,800. It is the second most common male cancer and the fifth most fatal. high cancer. Prostate-specific antigen (PSA) screening can provide early diagnosis for most patients, but for some patients with high-risk or metastatic lesions, it cannot give an accurate diagnosis. Early and accurate diagnosis and staging are crucial for choosing effective treatment. Traditional imaging methods such as computed tomography (CT) and nuclear magnetic resonance (MRI) have certain defects, especially at low PSA levels, the rate of missed diagnosis and misdiagnosis is high. The use of posit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/02C07K1/04C07K1/06C07K1/13A61K51/08A61K51/04A61K103/00
CPCA61K51/0482A61K51/088C07K7/02
Inventor 温凯崔海平胡骥邓雪松罗田伟许林尹长峰于菁菁
Owner HTA CO LTD
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