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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  • 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 ac

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
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Example Embodiment

[0040] Example 1

[0041] This embodiment provides a PET diagnostic reagent for prostate cancer 68 The preparation method of Ga-HBBED-ANCP-PSMA, the method includes the following steps:

[0042] (S1) The precursor compound HBBED-ANCP-PSMA was 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, weighing 3 g of the raw material with a substitution degree of 0.3 mmol / g, adding it to the reactor, adding DMF, and soaking for 30 min. After that, DMF was drained, added with 3 times the volume of 20% Pip / DMF, and filled with nitrogen protection to remove Fmoc, reacted for 30 minutes, drained 20% Pip / DMF, washed with DMF 5 times, ninhydrin detection showed dark blue. Put in 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 appropr...

Example Embodiment

[0058] Example 2

[0059] In vitro stability determination:

[0060] 68 The radiochemical stability of Ga-HBBED-ANCP-PSMA is carried out in two systems: calf serum and phosphate buffer. PBS method: placed in 0.5mL of phosphate buffer (PBS, pH=7.4), placed at 37℃, incubated for 30, 60, 90, 120, and 150 minutes, and then measured its radiochemical purity by HPLC to determine its in vitro stability. Serum method: Place in 0.5mL calf serum solution and incubate at pH=7 and 37°C. When incubating for 30, 60, 90, 120, and 150 minutes, the radiochemical purity was measured 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 30 min to 150 min, the radiochemical purity is slightly reduced during the period, but the stability always remains above 98%, indicating 68 Ga-HBBED-ANCP-PSMA has good stability in PBS, 68 Ga 3+ Stable binding with HBBED ligand. The in vitro stability results i...

Example Embodiment

[0062] Example 3

[0063] Measurement of fat-water partition coefficient:

[0064] Mark 68 Ga-NHBBED-ANCP-PSMA is separated and purified by Sep-Pak C18 Cartridge, eluted with 95% ethanol. The obtained marker was blown dry with dry nitrogen, and the same volume (0.5mL: 0.5mL) of n-octanol and phosphate buffer solution (pH=7.4) was used to dissolve the obtained marker in a 1.5mL EP tube (about 3.7MBq) in. Fully shake for 5 minutes, centrifuge and layer in a centrifuge for 5 minutes at a speed of 2000 rpm. Take 100uL each of the organic phase and the water phase in a 1mL EP tube, measure the radioactivity counts in the well-type γ detector, and calculate the lipid-water partition coefficient P from the ratio of the radioactivity counts of the organic phase and the water phase. P=log(N O / N W )(N O And N W Respectively count the organic phase and water phase samples). Repeat the operation 3 times, and take the average value as the lipid-water partition coefficient of the marker.

[...

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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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