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 trial. The single-center, dose-escalation study will be conducted at the University of Colorado at Denver and Health Sciences Center in Aurora, Colorado.
In preclinical studies the compound has been shown to be an orally active, microtubule disrupting agent that leads to arrest of cell division and apoptosis in tumor cells.
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.
“Results from preclinical studies with this compound highlight its significant antitumor activity and multiple mechanisms of action, including inhibiting three transcription factors, HIF-1alpha, NF-kappaB and Stat3, known to promote tumorigenesis,” said Dr Carolyn Sidor, EntreMed’s vice president and chief medical officer.