EntreMed has begun a Phase I clinical trial to evaluate the safety, tolerability, pharmacokinetics, and clinical benefit of its novel tubulin binding agent, ENMD-1198, in patients with advanced cancer. Patients with advanced cancer whose disease has failed to respond to existing therapies or where no approved therapy is available are expected to be enrolled in the study.

ENMD-1198, a new chemical entity based on a modified chemical structure of 2-methoxyestradiol (2ME2), is designed to decrease metabolism while retaining 2ME2's multiple mechanisms of action, including inducing apoptosis, binding microtubules, and inhibiting HIF-1alpha. In preclinical studies, ENMD-1198 has been shown to be an orally active, microtubule disrupting agent that leads to arrest of cell division and apoptosis in tumor cells.