The present invention relates to a set of antibodies which bind to antigens on target cells and which target radionuclides to said cells, and to methods of using the same. The antibodies each comprising a Fab binding to the target antigen fused at the C-terminus of the VH to the N-terminus of the Fc and a VH or VL binding to a radiolabelled compound. The VH or VL are fused at the C-terminus to the N-terminus of the Fc. VH and VL form an antigen binding site when the antibody binds via the scFv to the target antigen.

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. ##STR00001##

The present invention relates to novel tetrazine compounds of formula I, wherein one of R.sub.1-R.sub.5 is .sup.18F, for use in pretargeted in vivo imaging. The compounds are suitable for use in click chemistry, i.e. reactions that join a targeting molecule and a reporter molecule. The invention further relates to precursors to formula I, wherein one of R.sub.1-R.sub.5 is SnR.sub.3, B(OR).sub.2, B(0H).sub.2. Formula (I).

##STR00001##

Disclosed are compounds, compositions, systems, and methods useful for treating disease (such as cancer and tumors), or binding, detecting, and affecting compounds, compositions, cells, tissues, and organs, where the compounds, compositions, systems, and methods include or involve toxic compounds and where the toxic effect of the compounds, compositions, systems, and methods is reduced by providing a cleavage site to facilitate separation of the toxic component from other components of the compound, composition, or system. Preferably the system is a composition delivery system comprising or using a composition as disclosed herein. In some forms, the cleavage of the composition delivers a therapeutic agent and avoids organ damage by the composition.

The present invention provides extracorporeal removal of targeting vectors applied in pretargeted therapy and diagnostics in animals and humans. The method and the means for extracorporeal removal of the targeting vectors is based on binding agents with inverse electron demand Diels-Alder (IEDDA) cycloaddition reactivity. The targeting vector comprises a therapeutic agent, a diagnostic agent or a theranostic agent and a chemical entity with IEDDA reactivity whereas the extracorporeal means comprises a column with a biocompatible solid support to which a chemical entity with complementary IEDDA reactivity is attached.

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 compositions and methods for the treatment of cancer. Specifically, the compositions of the present technology include novel clearing agents that may be used in pretargeted radioimmunotherapy.

The present disclosure relates generally to immunoglobulin-related compositions (e.g., antibodies or antigen binding fragments thereof) that can bind to the CDS 3 protein. The antibodies of the present technology are useful in methods for detecting and treating Alzheimer's disease or a CD33-associated cancer in a subject in need thereof.

Disclosed are compounds, compositions, systems, and methods useful for treating disease (such as cancer and tumors), or binding, detecting, and affecting compounds, compositions, cells, tissues, and organs, where the compounds, compositions, systems, and methods include or involve toxic compounds and where the toxic effect of the compounds, compositions, systems, and methods is reduced by providing a cleavage site to facilitate separation of the toxic component from other components of the compound, composition, or system. Preferably the system is a composition delivery system comprising or using a composition as disclosed herein. In some forms, the cleavage of the composition delivers a therapeutic agent and avoids organ damage by the composition.

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.