Disease modifying activity of 2ME2 demonstrated in preclinical rheumatoid arthritis studies

EntreMed a clinical-stage pharmaceutical company developing therapeutics primarily for the treatment of cancer and inflammatory diseases, has announced the presentation of positive preclinical results for its lead compound, 2-methoxyestradiol (2ME2), in models of rheumatoid arthritis.

The data were presented during the 7th World Congress on Inflammation, held recently in Melbourne, Australia.

Preclinical studies demonstrated that daily oral administration of 2ME2 resulted in a dose-dependent decrease in inflammation and tissue destruction in two distinct animal models of rheumatoid arthritis. Two parameters for assessing inflammatory responses, infiltration of inflammatory cells and pannus severity, showed a clear dose-dependent improvement with 2ME2- treatment. Cartilage lesion and bone resorption severity scores, two parameters that assess tissue destruction processes, also displayed a dose- dependent decline after treatment with 2ME2. Treatment with 100 mg/kg of 2ME2 was nearly 100% effective in the inhibition of inflammatory response and tissue destructive processes in a collagen-induced arthritis model. In addition, in an adjuvant-induced arthritis model, 2ME2 inhibited arthritis to a level comparable to standard of care agents, Enbrel and methotrexate.

Carolyn F. Sidor, MD, MBA, EntreMed Vice President and Chief Medical Officer commented on the presentation, "We continue to generate positive preclinical data demonstrating the impact of 2ME2 on inflammation and disease progression in rheumatoid arthritis. These data, as well as data from previous preclinical studies, support 2ME2's potential as a disease modifying anti-rheumatic drug (DMARD) candidate. While we continue evaluating 2ME2 (Panzem Capsules and Panzem NCD) in oncology, we will conduct further preclinical studies in rheumatoid arthritis to explore additional clinical opportunities for this compound. Our goal is to file an IND for 2ME2 in rheumatoid arthritis in 2006."



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