Described herein are nanoprobes comprising ultrasmall aminated and cRGDY-conjugated nanoparticles labeled with Zirconium-89 (.sup.89Zr) and methods of their use. The provided compositions are renally clearable and possess suitable blood circulation half-time, high tumor active targeting capability, dominant renal clearance, low liver accumulation, and a high tumor-to-background ratio. The described nanoprobes exhibit great potential as “target-or-clear” tracers to human subjects for systemic targeted imaging (or treatment) of cancer.

The present invention provides peptides and peptide-conjugates that bind to α.sub.vβ.sub.6 integrin. The peptide-conjugates can be used for a variety of imaging and therapeutic applications. Methods of use and peptide optimization are also provided herein.

The present invention provides bi-terminal PEGylated peptide conjugates that target an integrin such as α.sub.vβ.sub.6 integrin. In particular embodiments, the peptide conjugates of the present invention further comprise a biological agent such as an imaging agent or a therapeutic agent, e.g., covalently attached to one of the PEG moieties. The peptide conjugates of the present invention are particularly useful for imaging a tumor, organ, or tissue and for treating integrin-mediated diseases and disorders such as cancer, inflammatory diseases, autoimmune diseases, chronic fibrosis, chronic obstructive pulmonary disease (COPD), lung emphysema, and chronic wounding skin disease. Compositions and kits containing the peptide conjugates of the present invention find utility in a wide range of applications including, e.g., in vivo imaging and immunotherapy.

A method for preparing a complex comprising a radioisotope of gallium for use in radiotherapy or in a medical imaging procedure, said method comprising adding a gallium radioisotope solution obtained directly from a gallium radionuclide generator to a composition comprising a pharmaceutically acceptable buffer and optionally also a pharmaceutically acceptable basic reagent, in amounts sufficient to increase the pH to a level in the range of 3 to 8, wherein the composition further comprises a chelator that is able to chelate radioactive gallium within said pH range and at moderate temperature, said chelator being optionally linked to a biological targeting agent. Kits and compositions for use in the method are also described and claimed.

The invention relates to ligands and complexes of metal ions with the ligands useful in various applications, including therapeutic and diagnostic applications.

A pharmacological composition contains a complex having a structurally modified RGD polypeptide a radionuclide. This pharmacological composition is useful for diagnosis or treatment of the integrin αvβ3-positive tumors. The pharmacological composition may further contain an immunotherapeutic medicament and an optional nanoantibody molecular imaging probe. Treatment with a PD-L1 blockade after the targeted radioactive therapy can archive the optimal synergic efficacy. Moreover, with administration of PD-1 or PD-L1 nanoantibody molecular imaging probe, expression of PD-1 or PD-L1 in the tumor after targeted radiotherapy can be observed.

The present invention provides a fluorescent silica-based nanoparticle that allows for precise detection, characterization, monitoring and treatment of a disease such as cancer. The nanoparticle has a range of diameters including between about 0.1 nm and about 100 nm, between about 0.5 nm and about 50 nm, between about 1 nm and about 25 nm, between about 1 nm and about 15 nm, or between about 1 nm and about 8 nm. The nanoparticle has a fluorescent compound positioned within the nanoparticle, and has greater brightness and fluorescent quantum yield than the free fluorescent compound. The nanoparticle also exhibits high biostability and biocompatibility. To facilitate efficient urinary excretion of the nanoparticle, it may be coated with an organic polymer, such as poly(ethylene glycol) (PEG). The small size of the nanoparticle, the silica base and the organic polymer coating minimizes the toxicity of the nanoparticle when administered in vivo. In order to target a specific cell type, the nanoparticle may further be conjugated to a ligand, which is capable of binding to a cellular component associated with the specific cell type, such as a tumor marker. In one embodiment, a therapeutic agent may be attached to the nanoparticle. To permit the nanoparticle to be detectable by not only optical fluorescence imaging, but also other imaging techniques, such as positron emission tomography (PET), single photon emission computed tomography (SPECT), computerized tomography (CT), bioluminescence imaging, and magnetic resonance imaging (MRI), radionuclides/radiometals or paramagnetic ions may be conjugated to the nanoparticle.

In a compound of the present invention, in a macroscopic view of a chemical structure thereof, a chelating moiety is located at the center of the structure, an atomic group containing an albumin binding moiety binds to one side of the chelating moiety, and an atomic group containing a target molecule binding moiety binds to the other side of the chelating moiety. The chelating moiety is also preferably DOTA or a derivative thereof. The target molecule binding moiety preferably has a structure to bind to a target molecule expressed in a cancer tissue. The present invention also provides a radioactive labeled compound in which the compound is coordinated to a radioactive metal ion.

The disclosure provides multifunctional compounds for use in medical imaging and therapy, the compounds comprising two or more of (i) a chelating ligand moiety (CL); (ii) an optical probe moiety (OP); and (iii) a biological targeting moiety (BT). The disclosure further provides related compositions and methods.

A method for removing or controlling or quantifying the presence of aldehydes, in particular acetaldehyde, is described. Such a method is useful in prolonging the shelf life of a pharmaceutical product.