IT-101 is a novel polymer-based conjugate of the anti-cancer agent camptothecin and is currently in Phase 1 clinical development. It consists of multiple camptothecin molecules conjugated to a cyclodextrin-polyethylene glycol copolymer via individual glycine linkers. The parent copolymer has an average molecular weight of approximately 85 kDa and is freely soluble in water1. IT-101 was designed to address several key limitations of camptothecin such as poor solubility, short circulation half-life and limited stability of the active form which contributed to its poor clinical activity and severe toxicity2-4.One key feature of IT-101 is that it self assembles into nanoparticles large enough to avoid kidney filtration but small enough to facilitate tumor distribution via the enhanced permeability and retention (EPR) effect5. We will present data using several orthogonal analytical techniques which characterize the size and composition of the IT-101 nanoparticles.J. Cheng et al. Bioconjugate Chem. 2003, 14, 1007-17.J. Gottlieb et al. Cancer Chemother Rep. 1970, 54, 461-70.C. Moertel et al. Cancer Chemother Rep. 1972, 56, 95-101.F. Muggia et al. Cancer Chemother Rep. 1972, 56, 515-21.T. Schluep et al. Cancer Chemother Pharmacol. 2006, 57, 654-62.

IT-101 nanoparticle characterization

240th National Meeting (2010)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.