Design and development of IT-101, a cyclodextrin-containing polymer conjugate of camptothecin.

IT-101 (Insert Therapeutics-101) is a linear, cyclodextrin-containing polymer conjugate of camptothecin (CPT). When formulated properly, the polymer conjugate self-assembles into nanoparticles of ca. 30 nm diameter and near neutral zeta potential. The nanoparticles show long circulation half-lives in animals and humans and localize in tumors. The nanoparticles enter the tumor cells and slowly release the CPT causing them to disassemble into individual polymer chains that are sufficiently small to be cleared renally. IT-101 is currently being investigated in human clinical trials. Here, the design and development of IT-101 is described with emphasis on features distinguishing it from other polymer-containing therapeutics.