A61K51/0402

METHODS FOR RADIOLABELING PSMA BINDING LIGANDS AND THEIR KITS

The present invention relates to methods for labeling a PSMA binding ligand with a radioactive isotope, preferably .sup.68Ga, .sup.67Ga or .sup.64Cu, said method comprising the steps of: i. providing a single vial comprising, in dried form, said PSMA binding ligand f the following formula (I): (I) at least one buffering agent, sodium chloride and a stabilizer against radiolytic degradation, ii. adding a solution of said radioactive isotope into said single vial, thereby obtaining a solution of said PSMA binding ligand of formula (I) with said radioactive isotope, iii. mixing the solution obtained in ii., and incubating it for a sufficient period of time for obtaining said PSMA binding ligand labelled with said radioactive isotope, and, iv. optionally, adjusting the pH of the solution.

##STR00001##

COPPER-CONTAINING THERAGNOSTIC COMPOSITIONS AND METHODS OF USE

The present technology provides compounds, as well as compositions including such compounds, useful for imaging and/or treatment of a non-small cell lung cancer, small cell carcinoma of the lung, bladder cancer, colon cancer, gallbladder cancer, pancreatic cancer, esophageal cancer, melanoma, liver cancer, primary gastric adenocarcinoma, primary colorectal adenocarcinoma, renal cell carcinoma, prostate cancer, a neuroendocrine tumor, a pituitary tumor, a vasoactive intestinal peptide-secreting tumor, a glioma, breast cancer, an adrenal cortical cancer, a cervical carcinoma, a vulvar carcinoma, an endometrial carcinoma, a primary ovarian carcinoma, a metastatic ovarian carcinoma, and/or a metastatic cancer. The compounds include a tumor targeting domain (that includes a moiety capable of recognizing or interacting with a molecular target on the surface of tumor cells), a blood-protein binding domain, and a sarcophagine-containing domain, where the moiety of the tumor targeting domain is distal to and sterically unimpeded by the blood-protein binding domain.

Radiopharmaceutical and methods
11491246 · 2022-11-08 · ·

The radiopharmaceutical .sup.177Lu-PSMA I&T is provided, including in high purities with extended shelf life. Further provided are methods of synthesis of .sup.177Lu-PSMA I&T and pharmaceutical compositions and methods of treatment that comprise .sup.177Lu-PSMA I&T.

Method of overcoming therapeutic limitations of nonuniform distribution of radiopharmaceuticals and chemotherapy drugs

Disclosed is a method for predicting the optimal amounts of radiopharmaceutical and/or chemotherapy agents to administer to a patient, by determining the level of saturation of the therapeutic agents in the patient's cells. The method comprises measuring cellular incorporation of the candidate therapeutic agents in a target cell population on a cell-by-cell basis. The method is able to identify an optimal cocktail of therapeutic agents for treatment of a disease. A method of high-throughput drug discovery incorporating this method, and a 2-stage targeting method of treating a disease using this method are also disclosed.

Stabilization of radiosynthetic intermediates

The present invention relates to a method for stabilizing radiosynthetic intermediates used in synthesis of .sup.18F radiolabeled aromatic amino acid derivatives toward decomposition caused by beta and gamma radiations by the use of radical scavengers and/or reductants and/or antioxidants.

COMPOSITIONS AND METHODS FOR IMAGING
20170296681 · 2017-10-19 ·

The present disclosure provides compositions for in vivo imaging of hydrogen peroxide; and methods for detecting hydrogen peroxide in vivo. The compositions and methods find use in various diagnostic applications, which are also provided.

18F-TAGGED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.

Metal Tricarbonyl Complexes Comprising Substituted Iminodiactic Acid Ligands and Uses as Radioisotope Tracers
20220306663 · 2022-09-29 ·

This disclosure relates to compositions comprising substituted iminodiacetic acid ligands and metal tricarbonyl complexes containing the ligands and derivatives thereof. In certain embodiments, the metal tricarbonyl complexes are used as radioisotope tracers such as renal tracers. In certain embodiments, the metal complexes comprise .sup.99mTc or Re. In certain embodiments, the ligands are substituted with a fluorine, a fluorine-18(F.sup.18) radioisotope, or other radionuclide.

PARA-AMINOHIPPURIC ACID (PAH) AS A RENAL PROTECTIVE SUBSTANCE
20220304964 · 2022-09-29 ·

The present application discloses para-aminohippuric acid (PAhI) or a pharmaceutically acceptable salt or carboxylic acid derivate thereof for use in a method for the reduction of nephrotoxic side effects of radiolabeled and non-radiolabeled therapeutic and diagnostic compounds in a subject. Also disclosed are pharmaceutical compositions comprising a radiolabeled and/or non-radiolabeled pharmaceutical compound and para-aminohippuric acid (PAH) or a pharmaceutically acceptable salt or carboxylic acid derivate thereof, and a pharmaceutically acceptable excipient, diluent, carrier or a combination thereof. Another subject of the present application is a method for the reduction of nephrotoxic side effects of radiolabeled and non-radiolabeled therapeutic and diagnostic compounds in a subject comprising administering to a subject para-aminohippuric acid (PAH) or a pharmaceutically acceptable salt or carboxylic acid derivate thereof in combination with a radiolabeled or non-radiolabeled therapeutic or diagnostic compound.

NOVEL THERANOSTIC AGENTS FOR PSMA POSITIVE CANCERS

The present disclosure provides compositions and methods for the detection and treatment of cancer. Specifically, the compositions of the present technology include novel radiohalogenated (e.g., radioiodinated) PSMA targeting agents and methods of using the same in diagnostic imaging as well as radiation therapy.