Dual acting prodrugs

摘要

A prodrug is provided which includes at least two different pharmaceutically and/or diagnostically active compounds independently bound by cleavable linkers and a protein-binding moiety which is capable of binding to carrier a molecule.

主权项

1. A prodrug comprising
(i) at least a first pharmaceutically and/or diagnostically active compound, the first pharmaceutically and/or diagnostically active compound is a member selected from the group consisting of topotecan, irinotecan, 9-aminocamptothecin, camptothecin and derivatives thereof, (ii) at least a second pharmaceutically and/or diagnostically active compound, the second pharmaceutically and/or diagnostically active compound is a third generation multidrug resistance (MDR) modulator, (iii) two or more cleavable linkers, the cleavable linker is a p-aminobenzyloxycarbonyl (PABC) linker, and (iv) a protein-binding moiety, the protein-binding moiety is a maleinimide group, wherein the first and the second pharmaceutically and/or diagnostically active compounds are each bound to the cleavable linker, and wherein the first and the second pharmaceutically and/or diagnostically active compounds are different from each other.