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Published November 12, 2009 | public
Journal Article

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

Abstract

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.

Additional Information

© 2009 Elsevier B. V. Received 7 May 2009; accepted 13 May 2009. Available online 12 August 2009. I thank all my co-investigators who are listed on the publications referenced. I especially thank Thomas Schluep, who is the Chief Science Officer of Insert Therapeutics (now merged with Calando Pharmaceuticals, Inc.) for leading the efforts of taking laboratory scale materials into the clinic. Finally, I thank Jamie Oliver for his leadership in the clinical programs with IT-101. Lastly, I thank the patients who willingly participated in the clinical trials.

Additional details

Created:
August 21, 2023
Modified:
October 19, 2023