A61K51/00

Chiral cyclen compounds and their uses

The present invention relates to the preparation of a series of chiral DOTA, DO3A, DO2A, DO1A, cyclen and their metal complexes, which display properties superior to those of previous DOTA-based compounds, and hence are potentially valuable as a platform for diagnostic applications. The chiral DOTAs reveal a high abundance of twisted square antiprism (TSA) geometry favoring them to be used as potential MRI contrast agents, whereas their rapid labelling properties at mild conditions make them excellent candidates for use as radiometal chelators.

MICRORNA-198 AS A TUMOR SUPPRESSOR IN OVARIAN CANCER
20220177889 · 2022-06-09 ·

A novel network of tumorigenic prognostic factors is identified that plays a critical role in advanced pancreatic cancer (PC) pathogenesis. This interactome is interconnected through a central tumor suppressive microRNA, miR-198, which is able to both directly and indirectly modulate expression of the various members of this network to alter the molecular makeup of pancreatic tumors, with important clinical implications. When this tumor signature network is intact, miR-198 expression is reduced and patient survival is dismal; patients with higher miR-198 present an altered tumor signature network, better prognosis and increased survival. Further, according to the present disclosure, MiR-198 replacement reverses tumorigenicity in vitro and in vivo. As such, an embodiment of the disclosure is a method of treating cancer in an individual, comprising the step of increasing the level of active microRNA-198 molecules in the pancreatic cancer tumor cells of the individual by an amount sufficient to cause an improvement in the pancreatic cancer in the individual

MICRORNA-198 AS A TUMOR SUPPRESSOR IN OVARIAN CANCER
20220177889 · 2022-06-09 ·

A novel network of tumorigenic prognostic factors is identified that plays a critical role in advanced pancreatic cancer (PC) pathogenesis. This interactome is interconnected through a central tumor suppressive microRNA, miR-198, which is able to both directly and indirectly modulate expression of the various members of this network to alter the molecular makeup of pancreatic tumors, with important clinical implications. When this tumor signature network is intact, miR-198 expression is reduced and patient survival is dismal; patients with higher miR-198 present an altered tumor signature network, better prognosis and increased survival. Further, according to the present disclosure, MiR-198 replacement reverses tumorigenicity in vitro and in vivo. As such, an embodiment of the disclosure is a method of treating cancer in an individual, comprising the step of increasing the level of active microRNA-198 molecules in the pancreatic cancer tumor cells of the individual by an amount sufficient to cause an improvement in the pancreatic cancer in the individual

Radiopharmaceutical compositions of radioactive halogenated benzylguanidine

The present disclosure concerns radiopharmaceutical compositions of radioactive halogenated benzylguanidine (such as radioiodinated MIBG) or a pharmaceutically acceptable salt, hydrate, or solvate thereof. In a preferred embodiment, the composition has at least 97% of radiochemical purity for at least 4 days. Advantageously, the compositions of the present disclosure may be devoid of parabens, which are carcinogenic and yet are used in known radioactive MIBG compositions. The present disclosure also provides processes of preparing a radioactive halogenated benzylguanidine composition. The compositions of the present disclosure can be used in diagnosis and treatment of various diseases.

System, emanation generator, and process for production of high-purity therapeutic radioisotopes
11348702 · 2022-05-31 · ·

An isotope production system, emanation generator, and process are disclosed for production of high-purity radioisotopes. In one implementation example, high-purity Pb-212 and/or Bi-212 isotopes are produced suitable for therapeutic applications. In one embodiment the process includes transporting gaseous radon-220 from a radium-224 bearing generator which provides gas-phase separation of the Rn-220 from the Ra-224 in the generator. Subsequent decay of the captured Rn-220 accumulates high-purity Pb-212 and/or Bi-212 isotopes suitable for direct therapeutic applications. Other high-purity product isotopes may also be prepared.

System, emanation generator, and process for production of high-purity therapeutic radioisotopes
11348702 · 2022-05-31 · ·

An isotope production system, emanation generator, and process are disclosed for production of high-purity radioisotopes. In one implementation example, high-purity Pb-212 and/or Bi-212 isotopes are produced suitable for therapeutic applications. In one embodiment the process includes transporting gaseous radon-220 from a radium-224 bearing generator which provides gas-phase separation of the Rn-220 from the Ra-224 in the generator. Subsequent decay of the captured Rn-220 accumulates high-purity Pb-212 and/or Bi-212 isotopes suitable for direct therapeutic applications. Other high-purity product isotopes may also be prepared.

Formulations and kits for radiotherapy and diagnostic imaging

Aqueous formulations and kits of radiopharmaceutical compounds of general Formula (II) protected from radiolysis with stabilisers, such as L-methionine and gentisic acid, are disclosed, wherein the compounds are based on sarcophagine ligands coordinated to a radioisotope, such as 64-copper, and linked to a tetrazine group for reaction with tumour targeting antibodies having functional reactive groups such as trans-cyclooctene, processes of preparing said radioligand formulations, and uses thereof for radioimaging, diagnosing and treating cancer. ##STR00001##

Au(III) complexes for [18F] Trifluoromethylation and methods for producing the same

Au(III) complexes for [.sup.18F] trifluoromethylation and methods for producing the same are disclosed. A gold complex comprises Au(CF.sub.3).sub.2LR, wherein L comprises a solubility supporting ligand and R comprises an organic substituent. The Au(III) complex can be used to prepare a positron emitting isotope that can be used as tracers for positron emitting tomography (PET) scans.

System and Process for Purification of Astatine-211 From Target Materials
20220148751 · 2022-05-12 · ·

A new column-based purification system and approach are described for rapid separation and purification of the alpha-emitting therapeutic radioisotope .sup.211At from dissolved cyclotron targets that provide highly reproducible product results with excellent .sup.211At species distributions and high antibody labeling yields compared with prior art manual extraction results of the prior art that can be expected to enable enhanced production of purified .sup.211At isotope products suitable for therapeutic medical applications such as treatment of cancer in human patients.

Method for producing radiohalogen-labeled compound and method for producing radiopharmaceutical

Provided is a method for producing a radiohalogen-labeled compound, the method comprises: a step in which a radiohalogen-labeling precursor compound (S-L) having a leaving group (L) capable of being nucleophilically substituted by a radioactive halide ion (X.sup.−) is subjected to a radiohalogenation reaction to obtain a reaction mixture RM1 which contains the radiohalogen-labeling precursor compound (S-L) and a reaction product (S—X) resulting from the radiohalogenation reaction; a step in which the reaction mixture RM1 is mixed with a polyvalent acid or a salt thereof to obtain a reaction mixture RM2; and a step in which the reaction product (S—X) is purified from the reaction mixture RM2 by a solid phase extraction method.