PRODRUG COMPRISING A SELF-CLEAVABLE LINKER

摘要

PROBLEM TO BE SOLVED: To provide alternative carrier-linked prodrugs, where a linker allows an autocatalytic cleavage to release a drug in an unmodified form without remaining residues originating from the linker.SOLUTION: A prodrug comprises a drug linker conjugate D-L. [D is a nitrogen containing biologically active moiety, such as exendin; L is a spacer comprising a non-biologically active linker moiety or the linker moiety represented by formula (I).] [R, R, R, R, R, and Rare independently H, CHand the like; X and Xare independently a methylene and the like; Xis a carbon atom and the like; Xis an oxygen atom and the like; wherein the dashed line indicates the attachment to the nitrogen of the biologically active moiety by forming an amide bond.]