A61K51/1093

DIELS-ALDER CONJUGATION METHODS
20220378918 · 2022-12-01 · ·

Described herein are protein-payload conjugates and compositions thereof that are useful, for example, for target-specific delivery of therapeutic and/or imaging agent moieties. In certain embodiments, provided are specific and efficient methods for producing protein-payload constructs (e.g., antibody-drug conjugates) utilizing a combination of transglutaminase and Diels-Alder techniques. Antibody-drug conjugates and compositions which comprise glutaminyl-modified antibodies, Diels-Alder adducts, and reactive payloads and are provided.

Trivalent Radioisotope Bio-Targeted Radiopharmaceutical, Methods Of Preparation And Use

A targeted radiopharmaceutical comprising a targeting species chemically-bonded to a PCTA-chelated Q.sup.+3 trivalent radioactive ion of Formula I

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is disclosed. Six of R.sup.1 through R.sup.7 are H and the seventh is a reacted functionality, Z, that forms the chemical bond with the targeting species, T. “g” is a number whose average value is 1 to about 12. X.sup.1, X.sup.2, and X.sup.3, are substituent groups that can coordinate to the Q.sup.+3 ion and/or help neutralize the ionic charge. Anion Y.sup.− is optionally present to balance the ionic charge. A pharmaceutical composition comprising a theranostic effective amount of a targeted radiopharmaceutical of Formula I in a pharmaceutically acceptable diluent is also contemplated, as are a method for treating and/or diagnosing a mammalian host having a disease, disorder or condition characterized by undesired angiogenesis, tumor growth and/or tumor metastasis.

Antigen Specific Binding Domains and Antibody Molecules
20220372125 · 2022-11-24 ·

The present disclosure relates to an antigen specific binding domain which binds to RON (Macrophage Stimulating Protein Receptor or Recepteur d'Origine Nantais). The disclosure also extends to chimeric antigen receptors (and a cell expressing the same), antibody molecules (including full length antibodies and fragments thereof, as well as antibody conjugates) containing the antigen binding domains disclosed herein. Also disclosed herein are pharmaceutical compositions comprising the cells, antibody molecules as disclosed herein. The present disclosure also refers to the use of the antigen binding domains, the chimeric antigen receptors, the antibody molecules and the pharmaceutical compositions disclosed herein in therapy, more particularly in treating cancer. Also disclosed herein are radiolabelled antibody conjugates comprising the antigen binding domains as disclosed, and their use in methods of treatment or diagnosis.

IGF-1R MONOCLONAL ANTIBODIES AND USES THEREOF

The present invention relates to conjugates including a chelating moiety of a metal complex thereof and a therapeutic or targeting moiety, methods for their production, and uses thereof.

REAGENTS AND METHODS FOR LABELING MOLECULES WITH ASTATINE ISOTOPES IN HIGHER OXIDATION STATES

Reagents and methods for labeling biomolecules with astatine isotopes in higher oxidation states. The reagents and methods allow for efficient labeling of biomolecules, such as antibodies, without the formation of high molecular weight by products that arise due to .sup.211At-promoted dimerization and higher aggregation of the conjugated biomolecules, and diminish cellular retention of astatine caused by cellular oxidization of the bonded astatine atom in vivo.

NANOPARTICLE IMMUNOCONJUGATES

Disclosed herein are nanoparticle immunoconjugates useful for therapeutics and/or diagnostics. The immunoconjugates have diameter (e.g., average diameter) no greater than 20 nanometers (e.g., as measured by dynamic light scattering (DLS) in aqueous solution, e.g., saline solution). In certain embodiments, the conjugates are silica-based nanoparticles with single chain antibody fragments attached thereto.

RI-LABELED HUMANIZED ANTIBODY

The RI-labeled anti-MUC5AC humanized antibody of the present invention is a conjugate of a chelating agent chelated with a radionuclide and an antibody (the radionuclide is a metal nuclide that emits α particle or positron, and the antibody is a humanized antibody specifically binding to MUC5AC), and is superior in specificity for MUC5AC and accumulation in tumor. Therefore, it is extremely useful for the treatment and/or diagnosis of diseases in which MUC5AC is overexpressed, particularly cancer.

Method of treating autoimmune inflammatory crohn's disease

This invention concerns compositions and methods of treating or diagnosing inflammatory disorders and other disorders, as well as compositions and methods of treating HIV.

SUSTAINED IMMUNOTHERAPY

Methods of inducing CD8+ T cell infiltration into a tumor in a patient in need thereof comprising administering a radioimmunoconjugate that is capable of binding a target expressed by at least some cells in a tumor.

AGENTS FOR CLEAVING LABELS FROM BIOMOLECULES IN VIVO

Disclosed herein are compounds, combinations, and kits that can be used to more quickly remove radionuclides from a subject, preferably a human being. Said compounds, combinations and kits can also be used to increase the tumor-to-blood ratio, or to more rapidly and/or conveniently achieve such an increase, of a label in targeted imaging or targeted radiotherapy in a subject, preferably a human being.