LNA-Based HIF-1 Alpha Inhibitor Shows Early Signs Of Clinical Benefit

Main Category: Cancer / Oncology
Also Included In: Clinical Trials / Drug Trials;  Pharma Industry / Biotech Industry
Article Date: 05 Jun 2009 - 2:00 PDT

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Santaris Pharma announced that the cancer drug EZN-2968 - an inhibitor of HIF-1alpha, jointly developed by Enzon Pharmaceuticals and Santaris Pharma A/S - was well tolerated and showed early signs of clinical benefit in previously treated cancer patients with advanced malignancies. EZN-2968 is being evaluated in patients with solid tumors and lymphoma. The study data, which was presented at the 2009 American Society of Clinical Oncology (ASCO) annual meeting in Florida last week, demonstrated that EZN-2968 is well tolerated, and that early signs of clinical benefit - prolonged stable disease - were observed in several patients.

"We have yet to see a dose limiting toxicity and we continue to be encouraged by the early clinical signals in this program," said Jeffrey H. Buchalter, Enzon's Chairman and Chief Executive Officer. "The duration of clinical benefit in certain histologies has exceeded our expectations at this phase of development. We look forward to advancing this promising compound into Phase II trials later this year, once a dose is determined."

"We are encouraged by the progress in the development of this LNA-based HIF-1 alpha inhibitor. The fact that LNA-based RNA inhibitors are beginning to show signs of clinical benefit in cancer patients is very rewarding and is further evidence of the potential of our LNA Drug Platform to generate effective and safe medicines to treat important diseases across a broad range of therapeutic areas," said S0ren Tulstrup, President & CEO of Santaris Pharma A/S.

HIF-1 alpha is a well-validated target in many common solid tumors. EZN-2968 is the first drug candidate to target the HIF-1 transcription factor, which regulates expression of many key genes important in cancer biology, including genes that regulate angiogenesis, cell metabolism, cell proliferation, cell death (apoptosis) and cell invasion. HIF-1 alpha protein is low in normal cells, but reaches high intracellular concentrations in a variety of cancers and is strongly correlated with poor prognosis and resistance to therapy. Enzon is currently conducting two Phase I studies, evaluating the HIF-1 alpha antagonist in different dosing schedules. The HIF-1 alpha inhibitor is licensed from Santaris Pharma A/S.

The collaboration between Santaris Pharma and Enzon Pharmaceuticals started in 2006 and by 2008 Santaris Pharma had delivered eight LNA based cancer drugs to Enzon Pharmaceuticals of which EZN-2968 was the first. The development of the remaining seven compounds is in progress. Moving forward Enzon is committed to the late stage pre-clinical development of these lead candidates. Santaris Pharma holds the European commercial rights to all the jointly developed cancer compounds.

Santaris Pharma (founded in 2003) is a privately held biopharmaceutical company developing new classes of RNA medicines targeting disease-related mRNAs and miRNAs based on its proprietary LNA Drug Platform. 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. The Company and its corporate partners currently have four compounds in clinical development and a full pipeline in late preclinical development.

Source: Santaris Pharma