EntreMed, Inc. announced today that preclinical results for its compound 2-methoxyestradiol (2ME2) were published on line in this week’s Early Edition of Proceedings of the National Academy of Sciences (PNAS). The study was conducted at The Campbell Family Institute for Breast Cancer Research at Princess Margaret Hospital and was led by Tak W. Mak, Ph.D.

Tak W. Mak, Ph.D., Director, The Campbell Family Cancer Research Institute, commented on the study, “Multiple sclerosis (MS) is among the most common autoimmune disorders in the northern hemisphere. There exists significant unmet medical need for safe and effective drugs to treat MS. In this study, we demonstrated that 2ME2, an endogenous metabolite of estradiol, significantly inhibits lymphocyte activation and proliferation and dramatically suppresses development of experimental MS.

Our analysis of cellular signaling pathways further reveals that 2ME2 exerts a potent inhibition of Nuclear Factor of Activated T cells (NFAT). By extension, the study provides for the first time a molecular rational for the use of 2ME2 as a tolerable oral immunomodulatory agent for autoimmune disorders such as MS. Other studies have shown that in humans, plasma levels of 2ME2 may increase dramatically during the last months of pregnancy, which intriguingly appears to correlate temporally with the remission of clinical symptoms reported in some pregnant MS and rheumatoid arthritis (RA) patients. We believe that 2ME2 may offer a safe and effective treatment for such autoimmune disorders.”

Ken Ren, Ph.D., EntreMed’s Chief Executive Officer further commented, “In addition to ENMD-2076 for oncology, 2ME2 represents another important asset for our company with its strong IP position and sound safety profile. Together with our previous findings of its disease modifying activity in RA animal models, this study further extends 2ME2's therapeutic value to the management of MS, RA and possibly other autoimmune disorders.”

Dr. Ren continued, “We appreciate the international recognition by our peers. For the next step, we intend to further advance 2ME2 development as part of our global drug development plan and strategy to leverage resources both in the US and China. We are currently exploring multiple strategies for the development of 2ME2 including possible partnership opportunities. We believe that the development of 2ME2 for autoimmune diseases fits well with our plan to build a robust product pipeline and to add value for our long term shareholders.”

The article is entitled “2-Methoxyestradiol inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation” and was authored by Gordon S. Duncan, Dirk Brenner, Michael W. Tusche, Anne Brustle, Christiane B. Knobbe, Andrew J. Elia, Thomas Mock, Mark R. Bray, Peter H. Krammer and Tak W. Mak.

The article is available at http://www.pnas.org/content/early/2012/11/30/1215558110.

Source: Daily Markets (05/12/12)