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Formulations of PSMA imaging agents

A technology of preparation and aqueous preparation, applied in the field of preparation of compounds

Pending Publication Date: 2022-04-29
CLARITY PHARMA PTY LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This results in the release of radioactive isotopes

Method used

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  • Formulations of PSMA imaging agents
  • Formulations of PSMA imaging agents
  • Formulations of PSMA imaging agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0153] Labeling buffer (acetate, 50 μL, 1 M, pH 5.0) was added to an acid-washed 500 μL microcentrifuge tube, followed by 10 μL of the stock solution of Formula I. Add to the buffer solution [ 64 Cu]CuCl 2 0.02M HCl solution (25 μL, 116 MBq). The microcentrifuge tube was sealed and the radioactivity present in the reaction was measured using a dose calibrator. Transfer the centrifuge tube to an Eppendorf Thermomixer C and heat at 40°C for 20 minutes. At 20 minutes, the reactant was taken out from the thermomixer, and a sample (5 μL) was taken from the reactant, diluted with 1:1 ethanol:water solution (5 μL) and injected into a radioactive high-performance liquid chromatography system (QC1, 5 μL) middle. The reaction mixture was at room temperature while a final analysis was performed to determine if the radiochemical yield was >95%, which took 7 minutes.

Embodiment 2

[0155] Labeling buffer (acetate, 50 μL, 1 M, pH 5.0) was added to an acid-washed 500 μL microcentrifuge tube, followed by 5 μL of the stock solution of Formula I. Add to the buffer solution [ 64 Cu]CuCl 2 0.02M HCl solution (25 μL, 109 MBq). The microcentrifuge tube was sealed and the radioactivity present in the reaction was measured using a dose calibrator. Transfer the centrifuge tube to an Eppendorf Thermomixer C and heat at 40°C for 20 minutes. At 20 minutes, the reactant was taken out from the constant temperature mixer, and a sample (5 μL) was taken from the reactant, diluted with 1:1 ethanol:water solution (5 μL) and injected into a radioactive high performance liquid chromatography system (QC1, 5 μL )middle. The reaction mixture was at room temperature while a final analysis was performed to determine if the radiochemical yield was >95%, which took 7 minutes.

Embodiment 3

[0157] Labeling buffer (acetate, 600 μL, 1 M, pH 5.0) was added to an acid-washed 1500 μL microcentrifuge tube, followed by 20 μL of the stock solution of Formula I. Add to the buffer solution [ 64 Cu]CuCl 2 0.02M HCl solution (300 μL, 1136MBq). The microcentrifuge tube was sealed and the radioactivity present in the reaction was measured using a dose calibrator. Transfer the centrifuge tube to an Eppendorf Thermomixer C and heat at 40°C for 20 minutes. At 20 minutes, the reactant was taken out from the constant temperature mixer, and a sample (5 μL) was taken from the reactant, diluted with 1:1 ethanol:water solution (5 μL) and injected into a radioactive high performance liquid chromatography system (QC1, 5 μL )middle. The reaction mixture was at room temperature while a final analysis was performed to determine if the radiochemical yield was >95%, which took 7 minutes.

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Abstract

The present invention relates to formulations of radiolabeled compounds for radiotherapy and diagnostic imaging associated with prostate specific membrane antigen (PSMA).

Description

technical field [0001] The present invention relates to formulations of radiolabeled compounds for use in radiotherapy and diagnostic imaging in relation to prostate specific membrane antigen (PSMA). Background technique [0002] Prostate cancer is the leading cause of cancer-related death in men, and mortality is often attributed to difficulties in detecting the disease and following treatment. Prostate-associated tumors often show increased expression of prostate-specific membrane antigen (PSMA), an enzyme normally expressed in prostate tissue but frequently upregulated in certain prostate cancers. This means that PSMA is a good biomarker or target for imaging, diagnostic and prognostic purposes. However, successful imaging of prostate cancer has been difficult because PSMA is also expressed in other tissues, both normal and malignant. [0003] Radiolabeled complexes can be used in the imaging and treatment of cancers, such as prostate cancer, however, some complexes com...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/395A61K33/34A61K51/04A61P35/00C07D487/08C07F1/08
CPCA61K51/06A61K33/34A61K47/12A61K47/22A61K47/183A61K9/0019A61P35/00A61K31/395A61K51/0402A61K51/0497A61K51/0482C07B59/002C07B2200/05C07D487/08A61K51/121A61K47/20A61K2123/00A61K9/0029A61K51/0427C07F1/08
Inventor 保罗·斯蒂芬·唐纳利尼古拉斯·阿兰·齐亚劳森·凯尔·斯拜里E·M·万戴蒙凯文·卡尔·翁·宽
Owner CLARITY PHARMA PTY LTD