The Phase I study is designed to evaluate the safety, tolerability, and pharmacokinetics of the HIF-1 alpha antagonist in a daily for five days schedule.
Hypoxia-inducible factor-1 alpha or HIF-1 alpha (EZN-2968) is a key regulator of a large number of genes important in cancer biology, such as angiogenesis, cell proliferation, apoptosis and cell invasion. HIF-1 alpha is low in normal cells, but elevated in a variety of cancers.
High expression of HIF-1 alpha is strongly correlated with poor prognosis and resistance to therapy. Therefore, drugs that inhibit HIF-1 alpha are expected to block multiple mechanisms that control cancer progression.
Enzon licensed the HIF-1 alpha antagonist from Santaris in July 2006 along with the Survivin antagonist and six additional proprietary product candidates created using the Locked Nucleic Acid technology platform, all directed against novel cancer targets selected by Enzon.