Extracellular targeted drug conjugates

摘要

The present invention relates to, inter alia, extracellular drug conjugates (EDC) in which an antibody or other targeting agent (e.g. a targeting moiety) is linked to a drug through a linker (e.g. a non-cleavable linker). These conjugates are useful in the treatment of disease and/or as a tool in the evaluation of biological systems.

主权项

1. A method for treating cancer, comprising administering to a human cancer patient in need of treatment for said cancer a therapeutically effective amount of an extracellular drug conjugate comprising a targeting moiety linked by a non-cleavable linker to a therapeutic agent,
wherein the targeting moiety comprises an antibody that binds to human FXYD5, wherein the therapeutic agent acts on an extracellular target and is selected from the group consisting of CEN08-178 (3-O-digitoxigenin-L-riboside), CEN08-193 (3-O-isodigitoxigenin-L-xyloside), CEN08-243 ((3S)-3-N-methoxyamino-scillarenin-L-neo-4-amino-4-deoxy-xyloside), CEN08-244 ((3S)-3-N-methoxyamino-scillarenin-L-neo-4-amino-4-deoxyriboside), CEN09-106 (scillarenin-4-amino-4-deoxy-L-xylopyranoside), and CEN09-107 (scillarenin-4-amino-4-deoxy-L-ribopyranoside), and wherein the non-cleavable linker comprises polyethylene glycol (PEG).