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.

Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.

This disclosure provides design, material, manufacturing method, and use alternatives for medical devices. An example medical device comprises a radioactive element positionable within a body lumen, the body lumen having an inner surface. The medical device also includes a frame attached to the radioactive element. The frame is also configured to position the radioactive element radially inward and away from the inner surface of the body lumen.

Novel .sup.18F-labelled tetrazines are provided which are highly reactive to be effective in vivo, suitable for pretargeted positron emission tomography (PET) and accessible in radiochemical yields (RCYs) which allow access to .sup.18F-labeled tetrazines for clinical applications. The .sup.18F-labelled tetrazines are developed using a Cu-mediated click indirect labelling approach. Only a subset of compounds appeared to be suitable for clinical pretargeted imaging strategies, and a particular compound which includes the use of an .sup.18F-labelled azide synthon having an azide structure with glucose as the linker and a triazole moiety within the linker, appears to be highly suited for clinical pretargeted imaging purposes.

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.

Compositions useful for target detection, imaging and treatment, as well as methods of production and use thereof, are disclosed herein.

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 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 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 present application discloses compositions and methods of use of .sup.68Ga labeled molecules. Preferably, the .sup.68Ga is attached to a peptide targetable construct and is used in a pretargeting technique with a bispecific antibody (bsAb). The bsAb comprises at least one binding site for a disease-associated antigen, such as a tumor-associated antigen, and at least one binding site for a hapten on the targetable construct. Exemplary haptens include In-DTPA and HSG. More preferably, the bsAb is administered about 24-30 hours before the targetable construct, and detection by PET imaging occurs about 1-2 hours after the targetable construct is administered. The methods and compositions are suitable for detection, diagnosis and/or imaging of various diseases, such as cancer or infectious disease.