ENMD-1198 is a new chemical entity designed to increase anti-tumor and anti-angiogenic properties and improve metabolism. The drug is characterized by its multiple mechanisms of action, which include inducing apoptosis, binding microtubules, and inhibiting HIF-1alpha. HIF-1alpha is over-expressed in more than 70% of human tumors and its over-expression correlates with tumor aggressiveness, metastases and poor prognosis.
Preclinical studies identified ENMD-1198 as an orally active, microtubule disrupting agent that leads to arrest of cell division and apoptosis in tumor cells. Additionally, ENMD-1198 exerts antiangiogenic activity that contributes to its overall anti-tumor effects.
Oral daily treatment with ENMD-1198 in an orthotopic breast cancer model led to a reduction in tumor burden equivalent to the positive control cyclophosphamide, disruption of microtubules within tumor cells, and a substantial decrease in HIF-1alpha.