Advertise With UsAdvertise on our extensive network of industry websites and newsletters.
Get the PBR newsletterSign up to our free email to get all the latest PBR
news.Preclinical studies have shown that EntreMed's novel tubulin binding agent, ENMD-1198, exerts antitumor activity strong enough to increase survival.
Subscribe to our email newsletter
A new chemical entity, ENMD-1198 is based on a modified chemical structure of 2-methoxyestradiol (2ME2) and is designed to decrease metabolism while retaining 2ME2’s multiple mechanisms of action. These actions include inducing apoptosis, binding microtubules, and inhibiting HIF-1alpha.
Study results demonstrated that ENMD-1198 is an orally active, microtubule disrupting agent that leads to arrest of cell division and apoptosis in tumor cells. In addition, ENMD-1198 also exerts antiangiogenic activity that further contributes to its overall antitumor effects. Preclinical results for ENMD- 1198 support its potential for broad application in cancer.
Data demonstrate that oral administration of ENMD-1198 leads to pronounced in vivo antitumor activity in preclinical cancer models resulting in a reduction in tumor burden and/or an increase in survival equivalent to cyclophosphamide.
Oral daily treatment with ENMD-1198 in an orthotopic animal model of human breast cancer led to the disruption of microtubules within tumor cells, as well as a substantial decrease in tumor cell proliferation and angiogenesis.