Prostate cancer pet diagnostic reagents 68 ga-hbbed-ancp-psma and its preparation method and application

A technology of HBBED-ANCP-PSMA, 68ga-hbbed-ancp-psma, applied in the field of medicine, can solve the problems of inapplicability of targeted therapy, not patent protection, etc., to achieve fast labeling speed, high labeling rate, good hydrophilicity sexual effect

Active Publication Date: 2022-06-24
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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  • Prostate cancer pet diagnostic reagents <sup>68</sup> ga-hbbed-ancp-psma and its preparation method and application
  • Prostate cancer pet diagnostic reagents <sup>68</sup> ga-hbbed-ancp-psma and its preparation method and application
  • Prostate cancer pet diagnostic reagents <sup>68</sup> ga-hbbed-ancp-psma and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] This embodiment provides a PET diagnostic reagent for prostate cancer 68 The preparation method of Ga-HBBED-ANCP-PSMA, described method comprises the 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 degree of substitution of 0.3 mmol / g, adding it to the reactor, adding DMF, and soaking for 30 min. After that, the DMF was drained, and 3 times the volume of 20% Pip / DMF was added, and nitrogen protection was used to remove Fmoc. Input N,N'-succinimidyl carbonate (DSC), N,N-diisopropylethylamine (DIPEA) and 4-dimethylaminopyridine (DMAP) in proportion, 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 protection. Add H-Glu(OtBu)-OtBu·HCl (Compound 2) into the reac...

Embodiment 2

[0059] In vitro stability assay:

[0060] 68 The radiochemical stability of Ga-HBBED-ANCP-PSMA was carried out in two systems, calf serum and phosphate buffered saline. PBS method: placed in 0.5 mL of phosphate buffered saline (PBS, pH=7.4), placed at 37°C, incubated for 30, 60, 90, 120, and 150 min, and the radiochemical purity was determined by HPLC to determine its in vitro purity. stability. Serum method: place in 0.5 mL of 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 30 min to 150 min, the radiochemical purity decreased slightly, but the stability remained above 98%, indicating that 68 The stability of Ga-HBBED-ANCP-PSMA in PBS is good, 68 Ga 3+ Binding to HBBED ligands is stable. The in vitro stability results in the ...

Embodiment 3

[0063] Measurement of the fat-water partition coefficient:

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

[006...

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Abstract

The invention discloses a prostate cancer PET diagnostic reagent 68 Ga‑HBBED‑ANCP‑PSMA and its preparation and use. said 68 The structural formula of Ga-HBBED-ANCP-PSMA is as follows: the preparation method comprises the following steps: (S1) adopting solid phase synthesis method to synthesize precursor compound HBBED-ANCP-PSMA; (S2) using direct labeling method to carry out 68 Ga radiolabeled. said 68 Ga‑HBBED‑ANCP‑PSMA has the characteristics of fast labeling speed and high labeling rate, and also has the advantages of good stability, good hydrophilicity, high sensitivity and high specificity. in addition, 68 Ga‑HBBED‑ANCP‑PSMA clears faster in blood and has higher tumor uptake.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a PET diagnostic reagent for prostate cancer 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 are 427,500 new cases worldwide and 361,800 deaths due to prostate cancer each year, ranking second in incidence and fifth in mortality among male cancers. high cancer. Prostate-specific antigen (PSA) screening can provide early diagnosis for most patients, but for some patients with high risk or metastases, it cannot give an accurate diagnosis. Early and accurate diagnosis and staging are essential for the selection of effective treatment. Traditional imaging modalities such as computed tomography (CT) and magnetic resonance imaging (MRI) have certain drawbacks, especially at low PSA levels, with high rates of missed and misdiagnosed. The use of positron emi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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