EntreMed, Inc. (ENMD), a clinical-stage pharmaceutical company developing therapeutics for the treatment of a variety of cancers, has received US patent covering methods of treatment and formulations for its clinical-stage compound, 2-methoxyestradiol (2ME2).

Patent No. 8,399,440, entitled “Disease Modifying Anti-Arthritic Activity of 2-Methoxyestradiol,” was granted on March 19, 2013, by the US Patent & Trademark Office and contains composition and method claims covering the combination of 2ME2 and methotrexate for the treatment of rheumatic diseases, including rheumatoid arthritis.

2ME2 is an orally active compound that has antiproliferative, antiangiogenic and anti-inflammatory properties. The inhibition of angiogenesis is an important approach to the treatment of both cancer and rheumatoid arthritis. 2ME2 has potential as a single agent in rheumatoid arthritis based on its antiangiogenic, anti-inflammatory, and anti-osteoclastic (bone resorption) properties. 2ME2 has also demonstrated positive preclinical results for multiple sclerosis.

Rheumatic diseases are characterized by inflammation and loss of function in one or more connecting or supporting structures of the body. Rheumatoid arthritis (RA) is a rheumatic disease characterized by persistent synovial tissue inflammation. In time, this persistent inflammation can lead to bone erosion, destruction of cartilage, and complete loss of joint integrity.

Ken K. Ren, EntreMed’s CEO, commented, “This patent further expands the intellectual property coverage for 2ME2. We have increasing evidence that 2ME2 has anti-inflammatory properties, providing us with potential opportunities to treat diseases such as rheumatoid arthritis. Clinical trial activities have previously been conducted with 2ME2 in RA, and in December 2012, preclinical results for 2ME2 were published online in the Early Edition of Proceedings of the National Academy of Sciences (PNAS). We believe 2ME2 has therapeutic value to the management of multiple sclerosis, RA and possible other autoimmune disorders and we are currently exploring strategies for the development of 2ME2 including potential partnership opportunities. EntreMed’s 2ME2 patent estate now provides composition, method, use, and formulation patent coverage through 2022.”