ROCKVILLE, Md., April 17, 2007 /PRNewswire-FirstCall/ -- EntreMed, Inc. , a clinical-stage pharmaceutical company developing therapeutics for the treatment of cancer and inflammatory diseases, today announced the presentation of preclinical data for its clinical-stage product candidate, ENMD-1198. The data were presented by EntreMed scientists and collaborators during two separate sessions at the American Association for Cancer Research (AACR) Annual Meeting being held this week in Los Angeles, California.
ENMD-1198, a new chemical entity (NCE) 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, disrupting microtubules, and inhibiting HIF-1 alpha. In preclinical studies, ENMD-1198 has been shown to be an orally active, antimitotic agent that leads to arrest of cell division and apoptosis in tumor cells. ENMD-1198 also exerts antiangiogenic activity that further contributes to its overall antitumor effects.
Results demonstrate that oral administration of ENMD-1198 was well tolerated and produced significant dose-dependent antitumor activity in a preclinical breast tumor model. Histologic staining and evaluation of tumor sections from the breast cancer model demonstrated a decrease in HIF-1 alpha, tumor cell growth (PCNA), and angiogenesis (CD31). HIF-1 alpha is a protein that is upregulated in many human tumors and has been shown to promote tumorigenesis and decrease tumor cell sensitivity to anticancer agents.
In a separate preclinical study, conducted by EntreMed
collaborators at the Children's Cancer Institute Australia for
Medical Research and the University of New South Wales, ENMD-1198
demonstrated antitumor activity against vinca alkaloid (micro