A61K51/041

COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS

The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.

PHARMACEUTICAL COMPOSITIONS FOR IMAGING, DIAGNOSIS AND TREATMENT OF CANCER

The present invention relates to a pharmaceutical cold kit composition comprising a chelating agent linked to somatostatin receptor binding organic moiety, a stabilizer, a buffer, and a caking agent or bulking agent, wherein the composition is free of sequestering agent. Further, the present invention also relates to the process of preparing reconstituted or radiolabeled solution composition having high in use stability and radiochemical purity and use thereof for diagnostic and/or therapeutic purposes.

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.

Imaging Agents

The present invention relates to radiolabelled 4-(furo[3,2-c]pyridin-4-yl) derivatives and their use as radioactive tracers, and in particular their use as imaging agents.

RADIOLABELED COMPOUNDS AND USES THEREOF
20220106275 · 2022-04-07 ·

Radiolabeled compounds of Formula I are described. Processes for radiolabeling the compounds are described. Methods for radioactive imaging using the compounds are also described.

IN VIVO STABLE HG-197(M) COMPOUNDS, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF IN NUCLEAR MEDICAL DIAGNOSTICS AND ENDORADIONUCLIDE THERAPY (THERANOSTICS)

The present invention relates to in vivo stable .sup.197(m)Hg compounds according to formula (E) for use in nuclear medical diagnostics and endoradionuclide therapy (theranostics), particularly the treatment of cancer, a method for the production of the .sup.197(m)Hg compounds comprising the step of radiolabeling of organic precursor compounds with NCA .sup.197(m)Hg by electrophilic substitution; and the use of the .sup.197(m)Hg compounds for nuclear medical diagnostics and endoradionuclide therapy (theranostics), particularly the treatment of cancer.

177Lu-DOTA-HYNIC-iPSMA AS A THERAPEUTIC RADIOPHARMACEUTICAL TARGETING PROSTATE-SPECIFIC MEMBRANE ANTIGEN

The invention relates to a new lutetium-177 therapeutic radiopharmaceutical as an inhibitor of prostate-specific membran antigen (iPSMA), wherein 1,4,7,10-tetraazacyclododecane-N,N,N,N-tetraacetic acid (DOTA) bonded to the heterocyclic molecule hydrazinonicotinamide (HYNIC), generates a rigid chemical structure that minimises the number of conformers and intramolecular hydrogen bonds, thereby producing a favourable spatial orientation of the active site (Lys(Nal)-NHCONH-Glu) in the molecule, for biological recognition by the PSMA protein. The new 177Lu-DOTA-HYNIC-iPSMA radiopharmaceutical accumulates, with high affinity in vivo, in tumours that overexpress the PSMA protein, acting as a radiotherapeutic agent. The purpose of the invention is to provide a new specific radiopharmaceutical (molecular target radiopharmaceutical) for the treatment of tumours with PSMA over

COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS

The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.

Imaging Agents

The present invention relates to radiolabelled 4-(furo[3,2-c]pyridin-4-yl) derivatives and their use as radioactive tracers, and in particular their use as imaging agents.

Radiohalogenated Agents for in Situ Immune Modulated Cancer Vaccination

A method of treating a malignant solid tumor in a subject is disclosed herein. The method includes the steps of administering to the subject an immunomodulatory dose of a radiohalogenated compound that is differentially taken up by and retained within malignant solid tumor tissue, and performing in situ tumor vaccination in the subject by intratumorally injecting into (or treating via a separate method) at least one of the malignant solid tumors a composition that includes one or more agents capable of stimulating specific immune cells within the tumor microenvironment. In certain exemplary embodiments, the radiohalogenated compound has the formula:

##STR00001##

wherein R.sub.1 is a radioactive halogen isotope, n is 18 and R.sub.2 is N.sup.+(CH.sub.3).sub.3.