Abstract: Theranostic agents incorporating a chelating moiety that can chelate a radioactive metal isotope and a PSMA-targeting moiety are disclosed herein. The theranostic agents, which can be used to treat and/or detect cancers associated with increased PSMA expression, have the formula: and include complexes, anions or salts thereof. R1 includes a chelating moiety; a is 0 or 1; n is an integer from 12 to 21; and R2 includes a prostate specific membrane antigen (PSMA)-targeting moiety. Optionally, the chelating moiety is chelated to a metal atom, where the metal atom is a positron or single photon emitting metal isotope, or an alpha, beta, or Auger emitting metal isotope.

Abstract: The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: A compound or a pharmaceutically acceptable salt thereof of formula (I): (A)-x1-(B)-x2-(C), wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x1 is a spacer covalently connecting (A) and (B); x2 is a spacer or a chemical single bond connecting (B) and (C); wherein (C) has the formula wherein R1 to R4, R9, a, b, Y and X1 to X4 have the meaning as indicated in the claims and description. The invention further relates to compositions comprising said compounds as well as a method for detecting neoplastic cells in a sample in vitro with the aid of the compounds or composition.

Abstract: The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.

Abstract: A lipid-, polymer-, and metal-based system of modified nanostructures of active biomedical and pharmaceutical agents used for in vivo (whole body/organ or tissue-specific) imaging. The modified nanostructure system involves various combinations of excipients (lipids, oils, surfactant, polymers, metals, carbon, nanotubes, etc.) in a formulation that allows a user to: (1) sustain the bioluminescent, fluorescent, or contrast signal for a longer period than conventional systems without repetitive administration (e.g., nanostructure system of luciferin), (2) target specific sites of interest (e.g., organ, tissue, receptors, proteins, etc.) for enhanced imaging of the targeted site (e.g. nanostructure system of XenoLight DIR with CREKA allows imaging of tumor vasculature), and (3) increase bioluminescent, fluorescent, or contrast signal flux.

Abstract: The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.

Abstract: Compositions comprising high levels of high specific activity copper-64, and process for preparing said compositions. The compositions comprise from about 2 Ci to about 15 Ci of copper-64 and have specific activities up to about 3800 mCi copper-64 per microgram of copper. The processes for preparing said compositions comprise bombarding a nickel-64 target with a low energy, high current proton beam, and purifying the copper-64 from other metals by a process comprising ion exchange chromatography or a process comprising a combination of extraction chromatography and ion exchange chromatography.

Abstract: Provided herein are curcumin analogues that are able to interact with amyloid beta (A?) and to attenuate the copper-induced crosslinking of A?. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

Abstract: Borylated Amino Acid (“BAA”) compositions and methods of making BAAs are disclosed herein. Consequently, the BAAs can be administered to patients as a Neutron Capture Agent and provide a method of treating cancer, immunological disorders and other disease by utilizing a Neutron Capture Therapy modality.

Abstract: Radioisotope-labeled small molecule activity-based probes that target the cancer associated serine hydrolase neutral cholesterol ester hydrolase 1 (NCEH1) are described. The probes can undergo a reaction with the NCEH1, resulting in covalent bonding of a portion of the probe molecule to the NCEH1. Also described are methods of labeling NCEH1 in biological samples, such as cells or tissue, and methods of visualizing tumors using the radioisotope-labeled NCEH1 probes as tracer compounds, either alone or in combination with assessing the efficacy of a cancer treatment or potential cancer treatment.

Abstract: A method for treating melanoma or preventing the development of melanoma comprising administration of a composition comprising 64Zne(Asp)2 in a therapeutically effective amount. Such administration may be via injection such as intratumoral and/or intravenous injection and may be once a day or more than once a day. A composition for the treatment of or prevention of melanoma comprising 64Zne(Asp)2 in a therapeutically effective amount. The composition may be a liquid suitable for injection.

Abstract: The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds. The disclosure also relates to compositions for incorporating the compounds as used for the targeted imaging of tumors. Conjugation of the amino acid linking groups increase specificity and detection of the compound. Methods and compositions for use thereof in diagnostic imaging are contemplated.

Abstract: The invention provides a compound of formula (I), and salts, solvates and radiolabelled forms thereof, together with complexes of the compound of formula (I) with TSPO, and methods for forming such complexes, and methods for detecting the compound of formula (I), such as in complex with TSPO.

Abstract: The invention relates to a new lutetium-177 therapeutic radiopharmaceutical as an inhibitor of prostate-specific membrane 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)-NH—CO—NH-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 overexpression.

Abstract: A method of performing a chelating reaction comprising contacting a divalent metal with a compound of Formula (I): or a salt thereof wherein: each of R1-R4 is independently selected from the group consisting of CH2COORa and CH2C(?O)NHRa; each of R5-R12 is independently selected from the group consisting of H and -L-X; each Ra is independently selected from the group consisting of H and -L-X; each L is independently selected from the group consisting of absent and a linking group; and each X is a biological agent; and wherein the contacting occurs at a temperature below about 40° C. to form a chelated composition.

Abstract: Provided herein are compositions and methods for remotely and non-invasively subjecting targeted biological structures with light emissions or chromogenic changes.

Abstract: The present disclosure provides an oral care composition and a preparation method, and an application thereof. The composition includes: a drug-loaded micelle, wherein the drug-loaded micelle includes a polymer micelle and an enamel restoration drug physically wrapped in the polymer micelle, and the polymer micelle is micelle particles formed by a water-soluble polymer with a structure shown by Formula I in an aqueous solution with presence of tannic acid and the micelle particles have a shell connected to a salivary protein polypeptide through chemical bonds. The oral care composition in the present disclosure enables the salivary protein polypeptide to adhere to the surfaces of teeth so as to open the borate ester bond between the tannic acid and the water-soluble polymer in an acidic environment generated by the dental caries and release the tannic acid and sodium fluoride, thus achieving the purpose of preventing dental caries and restoring tooth defects.

Abstract: A process for the preparation of a carrier-free Ga-68 solution from an irradiated Zn target, systems comprising components used in the process, and compositions comprising Ga-68 prepared by the process. Purification of Ga-68 is carried out by feeding an irradiation target solution comprising Zn-68, Ga-68 and solid target assembly metals into a system comprising three chromatography columns in succession.

Abstract: A method for making metal nanorods comprises combining a source of metal cations with at least one surfactant to form a mixture, wherein the metal cations are reduced and the metal nanorods are produced. Metal nanorods produced by the method and uses thereof. The metal nanorods are useful in devices such as lateral flow devices.

Abstract: The invention relates to medicine, particularly to agents for magnetic resonance diagnostics for oncological diseases. Developed for this purpose are a diagnostic preparation and a diagnostic method based on using said diagnostic preparation, in which a deuterated derivative of 3-O-methylglucose or a mixture of at least two different deuterated derivatives of 3-O-methylglucose is used as said preparation. The method according to the invention includes conducting magnetic resonance imaging and/or magnetic resonance spectroscopy on deuterium nuclei at a time after administration of the diagnostic preparation sufficient for the diagnostic preparation to accumulate in the tumor tissue of a subject in order to produce a magnetic resonance image and/or a magnetic resonance spectrum accordingly. The proposed method enables a highly informed diagnosis of oncological diseases.

Abstract: Imaging and radiotherapeutics agents targeting fibroblast-activation protein-? (FAP-?) and their use in imaging and treating FAP-? related diseases and disorders are disclosed.