Novel VQ polypeptide radioactive medicine and preparation method thereof

A radiopharmaceutical and radionuclide technology, applied in the field of radiopharmaceuticals with novel heptapeptide sequences and their preparation, can solve the problem of low early diagnosis rate of colon cancer

Active Publication Date: 2013-10-02
PEKING UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Due to the limitations of traditional endoscopy, it can only reveal ana...

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  • Novel VQ polypeptide radioactive medicine and preparation method thereof
  • Novel VQ polypeptide radioactive medicine and preparation method thereof
  • Novel VQ polypeptide radioactive medicine and preparation method thereof

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Embodiment 1

[0034] A VQ polypeptide radiopharmaceutical, including VQ polypeptide, a bifunctional chelator (Chelator) and a radionuclide (Nuclide), the VQ polypeptide is a linear hepeptide, and the linear hepeptide sequence is arginine-arginine- Proline-Methionine-Proline-Leucine-Glutamine VRPMPLQ (Val-Arg-Pro-Met-Pro-Leu-Gln, VQ), the radionuclide passes through a bifunctional chelating agent The VQ linear heptapeptide is labeled, the VQ polypeptide radiopharmaceutical is Nuclide-Chelator-VQ, and the VQ polypeptide radiopharmaceutical is a colorless transparent liquid injection.

[0035] Further, the bifunctional chelating agent is HYNIC (hydrazinonicotinamide). In the present invention, HYNIC is used as a bifunctional chelating agent, and tricine (trimethylolglycine) and TPPTS (trisodium triphenylphosphine-3,3',3''-trisulfonate) are used as a synergistic complex. Body so that " 99m "Tc-HYNIC core" has better stability in vivo and in vitro.

[0036] Further, the radionuclide is 99m Tc, the ...

Embodiment 2

[0045] This embodiment is an improvement made on the basis of Embodiment 1. For the same parts in this embodiment as Embodiment 1, please refer to the content disclosed in Embodiment 1 for understanding. The content disclosed in Embodiment 1 should also be regarded as this embodiment. The content is not repeated here.

[0046] a. Preparation of HYNIC-VRPMPLQ (HYNIC-VQ)

[0047] HYNIC-NHS (2 mg, 4.8 μmol) and VQ (1.2 mg, ~1.2 mmol) dissolved in 2 mL of N,N-Dimethylform amide (DMF, N,N-dimethylformamide) and H 2 O mixture (1:1 = v:v), adjust the pH to 8.5-9.0 with 0.1 N NaOH, and stir overnight at room temperature. The product was separated and purified by HPLC method 1, and the fraction with a retention time of 13.7 minutes was collected. The collected liquids were combined and lyophilized to obtain about 1 mg of product HYNIC-VQ (with a yield of about 35%) with a purity greater than 95%. ESI-MS mass spectrum analysis result: m / z =976.19 ([M+H] + ), C 43 H 71 N 14 O 10 S] + The t...

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Abstract

The invention relates to a VQ polypeptide radioactive medicine which comprises VQ polypeptide, a difunctional chelator and a radioactive nuclide, wherein the VQ polypeptide is linear heptad of which the sequence is VRPMPLQ (Val-Arg-Pro-Met-Pro-Leu-Gln, VQ), the radioactive nuclide marks the VQ linear heptad through the difunctional chelator, the VQ polypeptide radioactive medicine is Nuclide-Chelator-VQ, and the VQ polypeptide radioactive medicine is colorless and transparent liquid injection. The VQ polypeptide radioactive medicine can be used for early diagnosis of various tumors, the medicine enables the radioactive nuclide 99 mTc to be marked on the VQ polypeptide molecule through the difunctional chelator, marked medicine in body is concentrated to a tumor part through the targeting effect of the VQ polypeptide, and by using nuclear medicine single photon emission tomograph, imaging diagnosis is performed on various tumors.

Description

technical field [0001] The invention relates to a radiopharmaceutical for tumor diagnosis and treatment, in particular to a novel heptapeptide sequence radiopharmaceutical and a preparation method thereof. Background technique [0002] Colon cancer is one of the common malignant tumors, with the highest incidence in the 40-50 age group. According to the world epidemiological survey, it is found that colon cancer has the highest incidence rate in North America, Western Europe, Australia, New Zealand and other places, ranking the top two in visceral tumors. Due to the limitations of traditional endoscopy, it can only reveal anatomical changes, so that the early diagnosis rate of colon cancer is not high. In addition, flat lesions as well as lesions of polyposis syndrome or inflammatory bowel disease origin are usually overlooked by routine endoscopy, which greatly delays the early detection and effective prevention of precancerous lesions. Therefore, there is an urgent need ...

Claims

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Application Information

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IPC IPC(8): A61K51/08C07K1/13A61K103/10
Inventor 王凡史继云贾兵刘昭飞赵慧云
Owner PEKING UNIV
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