Neurokinin-1 (NK-1) receptor-binding agent delivery conjugates, compositions comprising NK-1 receptor-binding agent delivery conjugates, and methods for making and administering NK-1 receptor-binding agent delivery conjugates are provided. A conjugate may include an NK-1 receptor-binding moiety, a linker group containing at least one linker selected from the group of a releasable linker and a spacer linker, and an active agent linked to the linker group. The active agent may be selected from the group of fluorophore-containing compounds, radionuclide-containing compounds, and therapeutic agents for treatment of tumor cells characterized by over-expression of the NK-1 receptor.

Siderocalin-metal chelator combinations that bind metallic radioisotopes used in nuclear medicine with high affinity are described. The high affinity siderocalin-metal chelator combinations include a number of chelator backbone arrangements with functional groups that coordinate with metals. The siderocalin-metal chelator combinations can be used to deliver radionuclides for imaging and therapeutic purposes.

Disclosed herein is a radioimmune complex comprising an epidermal growth factor receptor (EGFR)-targeted antibody and a radioactive isotope of rhenium labeled thereon. The EGFR-targeted antibody is cetuximab or panitumumab.

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).

##STR00001##

Multinuclear complexes and methods for preparing them are provided. The discrete multinuclear complexes include a one or more transition metals and a radioisotope having the same coordination geometry as the transition metal. A bridging ligand is coordinated to the transition metal and the radioisotope to link the transition metal and the radioisotope and pendent ligands are coordinated to each of the transition metal and the radioisotope to stabilise the complex. The multinuclear complexes may include a radioisotope or radioelement that can be detected by medical equipment and may find use in therapy and/or the diagnosis of disease in patients.

The invention provides a method of preparing a .sup.89Zr-oxine complex of the formula ##STR00001##
The invention also provides a method of labeling a cell with the .sup.89Zr-oxine complex and a method for detecting a biological cell in a subject comprising administering the .sup.89Zr-oxine complex to the subject.

The invention relates to a marking precursor incorporating a chelator or fluorination group for radiolabelling with 44Sc, 47Sc, 55Co, 62Cu, 64Cu, 67Cu, 66Ga, 67Ga, 68Ga, 89Zr, 86Y, 90Y, 90Nb, 99mTc, 111ln, 135Sm, 140Pr, 159Gd, 149Tb, 160Tb, 161Tb, 165Er, 166Dy, 166Ho, 175Yb, 177Lu, 186Re, 188Re, 213Bi and 225Ac or with 18F, 131I or 211At, and one or two biological targeting vectors which are coupled to the chelator or fluorinating group via one or more squaric acid groups.

Described herein are methods of treating cancer by inducing favorable effects on tumor microenvironment (e.g., including macrophage polarization, cytokine profile, and/or immunophenotype) via administration of nanoparticles (e.g., silica-based ultra-small nanoparticles and nanoparticle conjugates such as nanoparticle drug conjugates). In certain embodiments, the methods may be used in concert with, or as part of, checkpoint inhibition therapy (e.g., anti-PD1) or radiotherapy, or a combination of both radiotherapy and checkpoint inhibitor therapy.

A method for producing a radiopharmaceutical, the method capable of maintaining a radioactive compound retaining a chemical structure and radioactivity at the time of production and after the production, and maintaining a usable period of a radiopharmaceutical; and a radiopharmaceutical are provided. The method for producing a radiopharmaceutical that has a radioactive component containing a radioactive dithiosemicarbazone copper complex includes: a stabilization step of adding a stabilizing agent containing at least one compound selected from the group consisting of ascorbic acid, methionine, sodium ascorbate, mannitol, and butylhydroxyanisole to a solution containing the radioactive component; and a filtration step of filtering the solution containing the radioactive component or a precursor thereof with a sterilization filter. In the radiopharmaceutical, a concentration of the radioactive component is 200 MBq/mL or more in terms of radioactivity concentrations.