The present disclosure provides bioorthogonal compositions for delivering agents in a subject. The disclosure also provides methods of producing the compositions, as well as methods of using the same.

Aqueous formulations and kits of radiopharmaceutical compounds of general Formula (II) protected from radiolysis with stabilisers, such as L-methionine and gentisic acid, are disclosed, wherein the compounds are based on sarcophagine ligands coordinated to a radioisotope, such as 64-copper, and linked to a tetrazine group for reaction with tumour targeting antibodies having functional reactive groups such as trans-cyclooctene, processes of preparing said radioligand formulations, and uses thereof for radioimaging, diagnosing and treating cancer.

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The present invention provides novel compounds that are useful as radiopharmaceuticals, imaging agents and for treatment of cancer.

The present disclosure provides bioorthogonal compositions for delivering agents in a subject. The disclosure also provides methods of producing the compositions, as well as methods of using the same.

The present invention provides a method for selective delivery of a therapeutic or diagnostic agent to a targeted organ or tissue by implanting a biocompatible solid support in the patient being linked to a first binding agent, and administering a second binding agent to the patient linked to the therapeutic or diagnostic agent, such that the therapeutic or diagnostic agent accumulates at the targeted organ or tissue.

The invention provides a novel trifunctional targeting construct and related compositions and methods that are useful in therapeutic, diagnostic (including imaging) of various biological and/or pathological conditions and diseases such as cancers and diabetes. The trifunctional targeting construct of the invention provides enhanced clearing step and reduced non-specific background via complete clearance of undesired antibody conjugates.

The invention is directed to a method for cancer treatment and prevention, specifically, a method of targeting and delivering therapeutic agents and/or imaging reagent to cells expressing Purinergic Receptor P2Y G-Protein Coupled 1 (P2RY1).

The present invention relates to compositions and methods employing conjugates that include a self-assembly and disassembly (SADA) polypeptide and a binding domain. The present invention encompasses the recognition that conjugates with a SADA polypeptide have certain improved biological properties. SADA-conjugates are described, along with uses thereof (e.g., as therapeutic or diagnostic agents) and methods of manufacture.

It is an object of the present invention to provide a clearing agent, by which after a fusion of the streptavidin mutant and a molecular probe has been administered, the fusion, which is not localized in a target site such as an affected site but remains in the body, can be promptly removed (cleared) from the body. The present invention provides a compound represented by the following formula (1) or a salt thereof:

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wherein X1a, X1b, X2a and X2b each independently represent O or NH; Y.sup.1 and Y.sup.2 each independently represent C or S; Z.sup.1 and Z.sup.2 each independently represent O, S or NH; V.sup.1 and V.sup.2 each independently represent S or S.sup.+O.sup.; n1 and n2 each independently represent an integer of 0 or 1; L10 and L12 each independently represent a divalent linking group; L11 represents a trivalent linking group; L14 represents a divalent linking group; and Sugar represents a sugar residue.

The present invention is directed to sarcophagine based compounds of formula (I). The compounds can complex a radioisotope, such as 64-copper and hence are useful in radioimaging and radiotherapy of cancers, e.g. colorectal cancer. The compounds work via a pre-targeting imaging approach in which the tetrazine reacts via click chemistry with a functional group such as a transcyclooctene which is pre-bound to a ligand such as a tumour specific antibody. ##STR00001##