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

EZN-2968 inhibitor of HIF to target the HIF-1 transcription factor

Santaris Pharma has announced that the cancer drug EZN-2968, an inhibitor of HIF, is being evaluated in patients with solid tumors and lymphoma. EZN-2968 is well tolerated, and early signs of clinical benefit – prolonged stable disease – were observed in several patients.

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.

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.

Soren Tulstrup, President and CEO of Santaris, said: 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.