Janssen Biotech, Inc.

Vadim Dudkin

Shalom Goldberg

Rhys Salter

Fengbin Song

Michael J McCauley

Kristen Wiley

John M Keith

Theresa Marie McDevitt

Joseph Erhardt

Rebecca Wissner

Macrocyclic chelators for chelation of alpha-emitting radiometal ions, such as actinium-225 are provided. Also provided are radiometal complexes containing an alpha-emitting radiometal ion bound to the macrocyclic chelator via coordinate bonding, and radioimmunoconjugates containing the radiometal complexes covalently linked to a targeting ligand, such as an antibody or antigen binding fragment thereof. The radioimmunoconjugates can be produced by click chemistry reactions. Methods of using the radiocomplexes and radioimmunoconjugates for selectively targeting neoplastic cells for radiotherapy and for treating neoplastic diseases and disorders are also described.

Macrocyclic chelators and methods of use thereof

Improved methods of radiolabeling antibodies using click chemistry are described. Also described are pharmaceutical compositions and uses related to the radiolabeled antibodies produced by the methods.

Radiolabeling of polypeptides

Engineered antibodies useful for site-specific conjugation by a transglutaminase are described. Also described are methods of site-specific conjugation of the antibodies, the site-specifically conjugated antibodies, and pharmaceutical compositions and uses related to the site-specifically conjugated antibodies.

Site-specific conjugation of glycosylated monoclonal antibodies with transglutaminase

Provided herein are methods for site-specific conjugation of glycan intact antibodies by a transglutaminase. According to particular embodiments, the reaction conditions are maintained or reduced to a low-ionic strength condition, which allows for efficient and fast conjugation without the need for antibody deglycosylation. Also described are pharmaceutical compositions and uses related to the conjugation method.

Growing community of inventors

Chalfont, PA, United States of America

Vadim Dudkin