Prostatic cancer PET (polyethylene terephthalate) diagnostic reagent 68Ga-HBBED-ANCP-PSMA, preparation method thereof and application of diagnostic reagent

A technology of HBBED-ANCP-PSMA, 68ga-hbbed-ancp-psma, applied in the field of medicine, can solve the problems of not being patented, not suitable for targeted therapy, etc., achieving fast labeling speed, high labeling rate, good hydrophilicity sexual effect

Active Publication Date: 2019-10-11
HTA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • Prostatic cancer PET (polyethylene terephthalate) diagnostic reagent 68Ga-HBBED-ANCP-PSMA, preparation method thereof and application of diagnostic reagent
  • Prostatic cancer PET (polyethylene terephthalate) diagnostic reagent 68Ga-HBBED-ANCP-PSMA, preparation method thereof and application of diagnostic reagent
  • Prostatic cancer PET (polyethylene terephthalate) diagnostic reagent 68Ga-HBBED-ANCP-PSMA, preparation method thereof and application of diagnostic reagent

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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-HBBED-ANCP-PSMA, described method comprises the steps:

[0042] (S1) Synthesizing the precursor compound HBBED-ANCP-PSMA 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-HBBED-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] 68 The stability results of Ga-HBBED-ANCP-PSMA are as follows Figure 4 As shown, in the PBS system, from 30min to 150min, the radiochemical purity decreased slightly during the period, but the stability remained above 98% all the time, indicating that 68 Ga-HBBED-ANCP-PSMA has good stability in PBS, 68 Ga 3+ Binding to HBBED ligand is stable. The in vitro stability results in the BSA system showed th...

Embodiment 3

[0063] Measurement of lipid-water partition coefficient:

[0064] Mark 68 Ga-NHBBED-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 coeff...

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Abstract

The invention discloses a prostatic cancer PET (polyethylene terephthalate) diagnostic reagent 68Ga-HBBED-ANCP-PSMA, a preparation method thereof and an application of the diagnostic reagent. The structural formula of the 68Ga-HBBED-ANCP-PSMA is as shown in the specification. The preparation method includes the steps: (S1) synthesizing a precursor compound HBBED-ANCP-PSMA by a solid-phase synthesis method; (S2) performing 68Ga radioactive labeling by a direct labeling method. The 68Ga-HBBED-ANCP-PSMA has the advantages of high labeling speed, high labeling rate, good stability and hydrophilcity, high sensitivity, high specificity and the like. In addition, the 68Ga-HBBED-ANCP-PSMA is rapidly removed from blood, and tumor uptake is high.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a prostate cancer PET diagnostic reagent 68 Ga-HBBED-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 posi...

Claims

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Application Information

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IPC IPC(8): C07C275/16C07C273/18A61K51/04A61K103/00
CPCC07C275/16A61K51/0406C07C2601/14
Inventor 温凯崔海平胡骥邓雪松赵海龙陈孟毅尹长峰于菁菁
Owner HTA CO LTD
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