Patent ID: 8877901
Filing Date: 2014-11-04
Classification: A61K,A61P,C07K

Abstract:
1. A conjugate of a camptothecin drug and a targeting moiety (TM) of the formula: TM-[L]-CPT, where TM is a cancer targeting monoclonal antibody; CPT is selected from the consisting of camptothecin, 10-hydroxy camptothecin, SN-38, topotecan, lurtotecan, 9-aminocamptothecin, and 9-nitrocamptothecin; and L is a linker system of the type X-Y-Z wherein X is an antibody coupling moiety comprising a defined polyethylene glycol (PEG) wherein the defined PEG contains a defined number of monomeric units that is between 1 and 12 monomeric units, Y is a lysosomally cleavable polypeptide, and Z is 4-aminobenzyloxy moiety, which is connected to the CPT drug, wherein Z is connected to a 20-hydroxy group of CPT by a carbonate or carbamate bond and X is connected to TM by a bond between a thiol group and a thiol-reactive moiety selected from the group consisting of maleimide, vinylsulfone, bromoacetamide, and iodoacetamide.