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Another LNA-based RNA Inhibitor Enters Clinical Trials

COPENHAGEN, March 20 /PRNewswire/ -- Santaris Pharma announced today that the fourth LNA-based drug has been brought into the clinic. In the USA several patients with cancer have now been treated with the Company's Survivin inhibitor, which is jointly developed by Santaris Pharma and Enzon Pharmaceuticals. The U.S. Food and Drug Administration (FDA) recently accepted Enzon Pharma­ceutical's Investigational New Drug (IND) application for the use of the LNA-based Survivin inhibitor.

Survivin is a key protein that controls cancer growth by playing a significant role in cell division, as well as inhibiting the programming that controls cell death. The Survivin inhibitor was developed using the Locked Nucleic Acid technology. In preclinical animal studies, EZN-3042 inhibited Survivin expression and tumor growth. It also potentiated the antitumor activity of taxol, an approved cancer therapeutic.

"Survivin is considered one of the most promising cancer targets and we are pleased that we were able to quickly advance this important compound into patients," said Jeffrey H. Buchalter, chairman and chief executive officer of Enzon Pharmaceuticals.

EZN3042 is one of eight LNA-based RNA inhibitors being developed by Santaris Pharma and Enzon Pharmaceuticals through a comprehensive partnership within the therapeutic area of cancer. Another compound forming part of the collaboration, EZN2968, an LNA-based hif1alfa inhibitor, is currently being investigated in two Phase I/II trials against a variety of cancers. Under the terms of the agreement, Enzon will have exclusive rights to develop and commercialize these compounds in the U.S. and other non-European territories. Santaris Pharma will retain exclusive rights to commercialization in Europe.

"This is the fourth LNA-based drug that has been brought into the clinic in record time either by ourselves or by a partner of ours based on our highly effective Drug Discovery Engine," said Henrik 0rum, CSO at Santaris Pharma. "We are very pleased by the achievement of this milestone and look forward to seeing other new LNA-based compounds advance into clinical trials across a range of therapeutic areas in the near future."

At the Association for Cancer Research (AACR) meeting being held April 18-22, 2009 in Colorado, Enzon Pharmaceuticals will present data on EZN3042 as well as on new LNA targets. Abstracts related to those targets are now available on

"Novel releasable PEG-nanoparticles enhance delivery of RNA antagonist oligonucleotides in tumor cells and in mice"

"EZN-2208, a novel pegylated SN-38 drug conjugate, markedly inhibits tumor growth and metastatic spreading of human neuroblastoma"

"Androgen receptor (AR) down regulation by locked nucleic acid antisense oligonucleotides specifically inhibits the growth of AR-positive tumor cells"

"The antitumor activity of EZN-4150, a potent LNA-based PIK3CA antagonist"

"EZN-3042, a novel locked nucleic acid oligonucleotide against survivin, inhibits survivin expression and confers taxol sensitivity"

"EZN-3920, an LNA antisense oligonucleotide RNA antagonist, down modulates HER3 expression and PI3K/Akt signaling pathway and enhances antiproliferative effect of Gefitinib in tumor cells"

About Santaris Pharma

Santaris Pharma is a privately held biopharmaceutical company with exclusive rights to use the LNA Drug Platform to develop new classes of RNA medicines targeting mRNAs and miRNAs associated with disease. The Company's own research and development activities focus on microRNAs, infectious diseases and metabolic disorders. In addition, Santaris Pharma is leveraging its highly effective and efficient drug discovery engine to generate lead LNA drug candidates against a broad array of disease targets selected by strategic partners. Santaris Pharma was founded in 2003 and the Company and its corporate partners currently have four compounds in clinical development and a full pipeline in late preclinical development. Current partners are Enzon Pharmaceuticals, GlaxoSmithKline and Wyeth Pharmaceuticals. Santaris Pharma has since its inception raised nearly $100 million through private financing and up front payments.

About Enzon

Enzon Pharmaceuticals, Inc. is a biopharmaceutical company dedicated to developing, manufacturing and commercializing important medicines for patients with cancer and other life-threatening conditions. The Company has a portfolio of four marketed products, Oncaspar(R), DepoCyt(R), Abelcet(R) and Adagen(R). Enzon's drug development programs utilize several cutting-edge approaches, including its industry-leading PEGylation technology platform and the Locked Nucleic Acid (LNA) technology. Enzon's PEGylation technology was used to develop two of its products, Oncaspar and Adagen, and has created a royalty revenue stream from licensing partner-ships for other products developed using the technology. Enzon also engages in contract manufacturing for several pharmaceutical companies to broaden the Company's revenue base.

SOURCE Santaris Pharma A/S
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