The invention provides compositions, kits and methods to treat a hyperproliferative disorder with an agent that increases expression of MCR1 and an MCR1 ligand. The invention also provides a method of treating drug-resistant melanoma, comprising administering an MCR1 ligand to a patient in need thereof. The present invention also provides in certain embodiments a melanoma-targeting conjugate comprising Formula I:
T-L-X
wherein T is a MCR1 ligand, L is a linker, and X an anti-cancer composition, for the therapeutic treatment of a hyperproliferative disorder. The present invention also provides methods, kits and uses of the conjugate of Formula I.

The present invention provides a novel radioactive compound for imaging malignant melanoma and a use thereof as a contrast agent for PET imaging.

The present invention relates to: a composition for stabilizing a radiopharmaceutical, the composition comprising a vitamin B compound as an active component; and a radiopharmaceutical composition comprising the same. Due to the inclusion of the vitamin B compound, it is possible to stabilize the radiochemical purity of the radioactive compound by inhibiting the radioactive degradation thereof at room temperature as well as at high temperature.

A nanoparticle is provided. The nanoparticle includes a magnetic core including a magnetic nanocrystal, a fluorophore coupled to the magnetic core, at least one chelating compound coupled to the magnetic core, the at least one chelating compound being a compound that chelates copper-64 (.sup.64Cu), a compound that chelates technetium-99m (.sup.99mTc), or a combination thereof, and an iodine chelator coupled to the magnetic core. Methods of making the nanoparticle and of using the nanoparticle as a multi-modal contrast agent are also provided.

Compositions, methods, and uses of an alpha emitter are provided in which the alpha emitter is coupled to carrier protein via a cleavable coupling moiety. The coupling moiety is preferably cleavable in an acidic tumor microenvironment, and as such will enrich the alpha emitter upon cleavage within the tumor microenvironment.

This application relates to compounds of Formula I. R.sup.1a, R.sup.1b and R.sup.1c is —CO.sub.2H, —SO.sub.2H, —SO.sub.3H, —SO.sub.4H, —PO.sub.2H, —PO.sub.3H or —PO.sub.4H. R.sup.2 is a linker, e.g. butylene. R.sup.3 is a linkage, e.g. —O—, —S—, —S(O)—, S(O).sub.2—, —NHC(O)—, —C(O)NH—, or 1,2,3-triazole. R4 is —(CH.sub.2).sub.0-3CH(R.sup.7)(CH.sub.2).sub.0-3— wherein R.sup.7 is —(CH.sub.2).sub.5CH.sub.3 or certain aromatic fused-ring systems. R.sup.5 and R.sup.6 are hydrogen or methyl. Each Xaa.sup.1 (if present) is an amino acid. R.sup.X is a radiolabeling group, e.g.: a radiometal chelator optionally bound by a radiometal; an aryl substituted with a radioisotope; a prosthetic group containing a trifluoroborate; or a prosthetic group containing a silicon-fluorine-acceptor moiety. The compounds may be useful for imaging prostate-specific membrane antigen (PSMA)-expressing tissues or for treating PSMA-expressing diseases (e.g. cancer).

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Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells.

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The present invention discloses indicator fluids, reference indicator fluid, and usage thereof, and systems and methods for assessing movement of molecular substances within, to or from a cerebrospinal fluid, brain or spinal cord compartment of a human cranio-spinal cavity. Indicator fluid moving from the cerebrospinal fluid compartment enables measurements of levels of indicator fluid in blood or urine and assessment of the cranio-spinal cavity's ability to remove molecular substances. The indicator fluids may be contrast agents used for imaging, such as by computed tomography imaging, and magnetic resonance imaging, or imaging utilizing radioactive substances by positron emission tomography, single-photon emission computed tomography or scintigraphy. Using these imaging modalities, the invention describes indicator fluids, systems and methods enabling assessment of movement of substances within, to or from a cerebrospinal fluid, brain or spinal cord compartment of a cranio-spinal cavity, and from the human cranio-spinal cavity to lymphatic pathways or kidneys.

Disclosed herein are methods preparing a purified, carrier-free 68Ga solution. Tire present disclosure also provides systems for preparing a purified, carrier-free 68Ga solution. The present disclosure also provides compositions comprising the purified, carrier-free 68Ga solutions disclosed herein. Also provided are methods of administering compositions of the present disclosure to a patient in need thereof, for example, for imaging a disease or disorder, such as cancer.

The present invention relates to a conjugated compound comprising a marker M pharmaceutically acceptable, and a peptide or pseudo-peptide P having at most 30 amino acid residues and able to bind the Low-Density Lipoprotein Receptor (LDLR) and to its use in a method of labelling and/or detecting and/or treating cancerous cells in a subject by administration of the conjugated compound to the subject an analysis of the presence and/or the amount of marker.