A61K51/0478

99MTC-EDDA/HYNIC-IPSMA AS A RADIOPHARMACEUTICAL FOR DETECTING THE OVEREXPRESSION OF PROSTATE-SPECIFIC MEMBRANE ANTIGEN

The invention relates to a novel radiopharmaceutical that inhibits the prostate-specific membrane antigen (iPSMA), containing hydrazinonicotinamide (HYNIC) as a critical chemical group in increasing in the lipophilicity of the molecule for binding to the hydrophobic sites of the PSMA, combined with the conventional use of HYNIC as a chelating agent for radiometal .sup.99mTc, in which the ethylenediaminetetraacetic acid (EDDA) is used to complete the coordination sphere of the radiometal. The novel radiopharmaceutical .sup.99mTc-EDDA/HYNIC-iPSMA detects, with high affinity and sensitivity in vivo, the overexpressed PSMA protein in prostate cancer cells using SPECT molecular imaging techniques in nuclear medicine. The aim of the invention is to provide a novel specific radiopharmaceutical (radiopharmaceutical for molecular targets) for SPECT, with high sensitivity for the detection of tumours with overexpression of PSMA.

Chelated PSMA Inhibitors
20190309000 · 2019-10-10 ·

Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells.

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Radiopharmaceutical solutions with advantageous properties
10434198 · 2019-10-08 · ·

The present invention relates to radiopharmaceutical compositions comprising the mother nuclide .sup.224Ra, its daughter nuclide .sup.212Pb, and a complexing agent that complexes with the daughter nuclide. The use of targeted chelate scavengers for .sup.224Ra daughter nuclide opens up the possibility for using .sup.224Ra based solutions for medial treatments.

RADIO-PHARMACEUTICAL COMPLEXES

The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a coupling moiety terminating in a carboxylic acid group; b) coupling said octadentate chelator to at least one tissue-targeting moiety targeting prolyl endopeptidase FAP; and c) contacting said tissue-targeting chelator with an aqueous solution comprising an ion of at least one alpha-emitting thorium isotope. A method of treatment of a neoplastic or hyperplastic disease comprising administration of such a tissue-targeting thorium complex, as well as the complex and corresponding pharmaceutical formulations are also provided.

COMPOSITIONS FOR THERAPEUTICS, TARGETED PET IMAGING AND METHODS OF THEIR USE

Described herein is a chelator for radiolabels (e.g., .sup.89Zr) for targeted PET imaging that is an alternative to DFO. In certain embodiments, the chelator for .sup.89Zr is the ligand, 3,4,3-(LI-1,2-HOPO) (HOPO), which exhibits equal or superior stability compared to DFO in chemical and biological assays across a period of several days in vivo. As shown in FIG. 1, the HOPO is an octadentate chelator that stabilizes chelation of radiolabels (e.g., .sup.89Zr). A bifunctional ligand comprising p-SCN-Bn-HOPO is shown in FIG. 4 and FIG. 5. Such a bifunctional ligand can eliminate (e.g., .sup.89Zr) loss from the chelate in vivo and reduce uptake in bone and non-target tissue. Therefore, the bifunctional HOPO ligand can facilitate safer and improved PET imaging with radiolabeled antibodies.

Copper-cysteamine and methods of use

Structure and luminescence properties of a new Cu-Cysteamine (Cu-Cy) crystal material are provided. The crystal structure of the Cu-Cy is determined by single crystal X-ray diffraction. It is found that the compound crystallizes in the monoclinic space group C2/c and cell parameters are a=7.5510(4) , b=16.9848(7) , c=7.8364(4) , =104.798(3). The new Cu-Cy crystal material of the invention is also useful for treatment of cancer.

METHODS AND KITS FOR PREPARING RADIONUCLIDE COMPLEXES
20240165277 · 2024-05-23 · ·

A method for preparing a complex comprising a radioisotope of gallium for use in radiotherapy or in a medical imaging procedure, said method comprising adding a gallium radioisotope solution obtained directly from a gallium radionuclide generator to a composition comprising a pharmaceutically acceptable buffer and optionally also a pharmaceutically acceptable basic reagent, in amounts sufficient to increase the pH to a level in the range of 3 to 8, wherein the composition further comprises a chelator that is able to chelate radioactive gallium within said pH range and at moderate temperature, said chelator being optionally linked to a biological targeting agent. Kits and compositions for use in the method are also described and claimed.

PET IMAGING OF ZINC TRANSPORT

A method for producing a solution including a positron emitting zinc cation of .sup.63Zn, and the method comprises bombarding a solution target including .sup.63Cu with high energy protons to produce a solution including a positron emitting zinc cation. A method for detecting or ruling out Alzheimer's disease in a patient comprises administering to a patient a detectable amount of a compound including a positron emitting zinc cation, wherein the zinc cation is targeted to -amyloid in the patient, and acquiring an image to detect the presence or absence of -amyloid in the patient. A method for detecting or ruling out cancer in a patient comprises administering to a patient a detectable amount of a compound including a positron emitting zinc cation, wherein the zinc cation is targeted to tissue in the patient; and acquiring an image using a medical imaging technique to detect zinc distribution in tissue in the patient.

SYSTEMS AND METHODS FOR RAPID NEURAL NETWORK-BASED IMAGE SEGMENTATION AND RADIOPHARMACEUTICAL UPTAKE DETERMINATION

Presented herein are systems and methods that provide for automated analysis of three-dimensional (3D) medical images of a subject in order to automatically identify specific 3D volumes within the 3D images that correspond to specific organs and/or tissue. In certain embodiments, the accurate identification of one or more such volumes can be used to determine quantitative metrics that measure uptake of radiopharmaceuticals in particular organs and/or tissue regions. These uptake metrics can be used to assess disease state in a subject, determine a prognosis for a subject, and/or determine efficacy of a treatment modality.

CHELATING PLATFORM FOR DELIVERY OF RADIONUCLIDES

Siderocalin-metal chelator combinations that bind metallic radioisotopes used in nuclear medicine with high affinity are described. The high affinity siderocalin-metal chelator combinations include a number of chelator backbone arrangements with functional groups that coordinate with metals. The siderocalin-metal chelator combinations can be used to deliver radionuclides for imaging and therapeutic purposes.