Clinical Development Overview
These are our current clinical studies. For more details on a particular product candidate, click on its name.
Through the use of our PEGylation technology, we designed PEG-SN38 (EZN-2208), a PEGylated conjugate of SN38, to offer therapeutic advantages over unmodified SN38 and existing therapies. The PEGylated version allows parenteral delivery, increased solubility, higher exposure, more profound deoxyribonucleic acid (DNA) damage, inhibition of angiogenesis, and longer apparent half-life of SN38.
HIF-1 alpha antagonist (EZN-2968)
HIF-1 alpha is over-expressed in many cancer types, including common solid tumors. It is a key regulator of numerous genes important in cancer biology, and is associated with poor prognosis and resistance to therapy. Drugs targeting HIF-1 alpha thus have the potential to target multiple cancer processes.
Survivin antagonist (EZN-3042)
Survivin plays a vital regulatory role in both apoptosis and cell division. Survivin is highly expressed in many cancers and in newly formed endothelial cells engaged in angiogenesis, with little expression in normal adult tissues. Resistance of cancer cells to radiotherapy and cytotoxic drugs is strongly correlated with expression levels of Survivin. Clinically, Survivin expression is associated with poor prognosis, increased cancer recurrence, and resistance to therapy. .
Androgen receptor mRNA antagonist (EZN-4176)
The AR is a validated target for the treatment of prostate cancer. Several approved androgen-blocking or –binding agents have therapeutic benefit, but prostate cancer typically develops resistance to these agents. Enzon’s LNA-based AR mRNA antagonist provides a novel and innovative strategy for the treatment of prostate cancer. In preclinical studies, Enzon’s mRNA antagonist down-regulated the AR, inhibited tumor growth when given alone, and enhanced the anti-tumor activity of conventional agents that inhibit AR activity.
Enzon is developing additional LNA-based mRNA antagonists to other targets that drive tumor growth. We have worldwide rights, except for in Europe, to develop and commercialize the compounds. Lead molecules that target HER3 and beta-catenin have demonstrated anti-tumor activity in animal models of human cancer.