New data also demonstrated excellent in vitro activity of Enzon’s customized linker technology when applied to the locked nucleic acid (LNA) antagonists, the company said. The study showed that PEG-SN38 (EZN-2208) displayed potent in vitro cytotoxicity against a panel of human cancer cell lines and that it outperformed Camptosar in various preclinical cancer models including colorectal, breast, pancreatic, prostate, and lung cancers.
Biodistribution data showed high and prolonged exposure of SN38 within tumors, supporting the enhanced permeation and retention (EPR) effect.
The data reported in this study found that a series of PEGylated LNA molecules created using Enzon’s customized PEG linkers, improved the cellular uptake of the molecule and had a potent dose-dependent and specific target mRNA gene down modulation without transfection.
Jeffrey Buchalter, Enzon’s chairman and CEO, said: “We continue to be encouraged by the positive preclinical results of PEG-SN38 and it further validates our ongoing Phase I program. Furthermore, while LNA therapy is efficacious in preclinical cancer models, the further enhancement of the pharmaceutical properties of LNA molecules using our Customized Linker Technology, could prove to be a unique approach for more efficient delivery of RNA targeted therapy.”