Abstract: Macrocyclic chelators for chelation of alpha-emitting radiometal ions, such as actinium-225 are provided. Also provided are radiometal complexes containing an alpha-emitting radiometal ion bound to the macrocyclic chelator via coordinate bonding, and radioimmunoconjugates containing the radiometal complexes covalently linked to a targeting ligand, such as an antibody or antigen binding fragment thereof. The radioimmunoconjugates can be produced by click chemistry reactions. Methods of using the radiocomplexes and radioimmunoconjugates for selectively targeting neoplastic cells for radiotherapy and for treating neoplastic diseases and disorders are also described.

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 is a bilirubin derivative-based ultrasound contrast agent for diagnosis and treatment. The fine particles including the bilirubin derivative are sensitive to reactive oxygen species (ROS), bind with hydrophobic drugs, and can effectively chelate metals such as iron oxide nanoparticles. Therefore, the fine particle of the present invention can be used as an ultrasound contrast agent for diagnosis, as a magnetic resonance imaging contrast agent, or as a carrier for hydrophobic drugs or platinum-based drugs.

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: The present invention provides a method of imaging a subject's lung which comprises contacting the subject's lung with a matrix metalloproteinase inhibitor labeled with a radioisotope under conditions such that the inhibitor binds to matrix metalloproteinase in the lung, and then imaging the radiolabeled inhibitor bound to matrix metalloproteinase in the subject's lung. The invention also provides Ro 32-3555 labeled with a radioisotope.

Abstract: Provided herein are compounds useful for imaging granzyme B. An exemplary compound provided herein is useful as a radiotracer for position emission tomography (PET) and/or single photon emission tomography (SPECT) imaging. Methods of imaging granzyme B, combination therapies, and kits comprising the granzyme B imaging agents are also provided.

Abstract: Provided herein are radiopharmaceutical compositions and uses thereof. The radiopharmaceutical compositions can comprise one or more stabilizing agents, an aqueous vehicle, and a conjugate that comprises a targeting ligand and a radionuclide bound to a metal chelator. The targeting ligand can be a small molecule compound or a peptide such as a monocyclic peptide. The targeting ligand can be configured to bind with a tumor target. The stabilizing agent can comprise a radiolysis stabilizer, a free metal chelator, and/or a pH stabilizer. Further provided herein are methods of preparing the radiopharmaceutical compositions and methods of treating cancer by administering the described radiopharmaceutical compositions.

Abstract: A composition containing Brilliant Blue G (BBG) or a pharmaceutically acceptable salt thereof, and a positional isomer of Brilliant Blue G (BBG) or a pharmaceutically acceptable salt thereof, the composition containing 90 wt % or more and 100 wt % or less of one or both of Brilliant Blue G (BBG) and the pharmaceutically acceptable salt thereof in the total of the Brilliant Blue G (BBG), the pharmaceutically acceptable salt of Brilliant Blue G (BBG), the positional isomer of Brilliant Blue G (BBG), and the pharmaceutically acceptable salt of the positional isomer of Brilliant Blue G (BBG), a method for producing said composition, and a method of removing the ocular membrane of a human patient.

Abstract: The liquid vehicles can be used to create dilute solutions of water-soluble pharmaceutical or non-pharmaceutical oral contrast agents. The liquid vehicles are formulated to provide desired osmolalities, viscosities, pH, and taste masking capabilities to match the particular intentions of the user and to complement the inherent differences in the various oral contrast agents. The liquid vehicles comprise an aqueous medium, an osmotic agent to adjust osmolality, a buffering agent, a viscosity agent, and sweeteners and flavoring agents to improve palatability.

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 nanoparticle-lipid composite carriers as theranostic agents, particularly for diagnosis and/or treatment of cancers and related diseases and conditions. In particular embodiments, the carrier composites comprise a lipid core and an outer shell of functionalized nanoparticles (fNPs).

Abstract: The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V): and salts thereof, wherein R1, R2, A, and X10-X19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

Abstract: The invention provides a novel class of MRI contrast agents based on biogenic hemin and compositions and methods of preparation and use thereof.

Abstract: Provided herein are radiopharmaceutical compositions and uses thereof. The radiopharmaceutical compositions can comprise one or more stabilizing agents, an aqueous vehicle, and a conjugate that comprises a targeting ligand and a radionuclide bound to a metal chelator. The targeting ligand can be a small molecule compound or a peptide such as a monocyclic peptide. The targeting ligand can be configured to bind with a tumor target. The stabilizing agent can comprise a radiolysis stabilizer, a free metal chelator, and/or a pH stabilizer. Further provided herein are methods of preparing the radiopharmaceutical compositions and methods of treating cancer by administering the described radiopharmaceutical compositions.

Abstract: The present invention relates to a method for treating cancer. This method involves providing a first agent comprising a first targeting component coupled to a first cancer therapeutic component and providing a second agent comprising a second targeting component coupled to a second cancer therapeutic component. The first and second targeting components have different biodistributions and/or pharmacokinetics. The first and second agents are administered to a subject having cancer to treat the cancer. Also disclosed is a combination therapeutic comprising the first and second agents.

Abstract: A compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[({2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl}amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclo dodecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.

Abstract: The present provides a Positional Isotopomer NMR Tracer Analysis (PINTA) method that can be used to noninvasively assess rates of hepatic mitochondrial oxidation (VCS) and/or pyruvate carboxylase (VPC) flux in a subject. In certain embodiments, the methods utilize a combined NMR/gas chromatography-mass spectrometry analysis of plasma following infusion of [3-13C]lactate and glucose tracer. The method of the invention provides investigators with a tool to non-invasively examine the role of altered hepatic mitochondrial metabolism and study the effects of therapeutic interventions for the treatment of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and type 2 diabetes (T2D).

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 invention comprises a method for the generation of 227Th of pharmaceutically tolerable purity comprising i) preparing a generator mixture comprising 227Ac, 227Th and 223Ra; ii) loading said generator mixture onto a strong base anion exchange resin; iii) eluting a mixture of said 223Ra and 227Ac from said strong base anion exchange resin using a first mineral acid in an aqueous solution; iv) eluting 227Th from said strong base anion exchange resin using a second mineral acid in an aqueous solution whereby to generate a first 227Th solution containing contaminant 223Ra and 227Ac; v) loading the first 227Th solution onto a strong acid cation exchange resin; vi) eluting at least a part of the contaminant 223Ra and 227Ac from said strong acid cation exchange resin using a third mineral acid in aqueous solution; and vii) eluting the 227Th from said strong acid cation exchange resin using a first aqueous buffer solution to provide a second 227Th solution.

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.