In a breast cancer model, ENMD-1198 was shown to inhibit a protein called HIF-1alpha which is over-expressed in more than 70% of human tumors. This over-expression correlates with tumor aggressiveness, metastases and poor prognosis.
ENMD-1198 represents a second generation of 2ME2-like molecules with potential for broad application in cancer and other diseases.
Preclinical studies identified ENMD-1198 as an orally active, microtubule disrupting agent that leads to arrest of cell division in tumor cells and apoptosis. In addition, ENMD-1198 also exerts antiangiogenic activity that contributes to its overall antitumor effects, mechanisms it shares with 2ME2.
The company hopes to submit an investigational new drug application for the compound by the end of 2005.