LNA-based HIF-1 Alpha Inhibitor Shows Early Signs of Clinical Benefit
News Jun 16, 2009
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 Soren 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.