The anti-arthritic activity of Panzem (2-methoxyestradiol, or 2ME2) was evaluated in a preclinical animal model of rheumatoid arthritis. Data from the study demonstrated that oral treatment with 2ME2 resulted in a dose-dependent decrease in severity of arthritic disease as determined by standard clinical measurements.
A decrease in clinical symptoms with 2ME2 administration was accompanied by a marked inhibition of tissue and joint damage that are hallmarks of rheumatoid arthritis, such as inflammatory cell infiltrates, articular cartilage erosion, pannus formation, and bone resorption.
These data demonstrate that in this animal model of rheumatoid arthritis, 2ME2 decreases inflammation, halts disease progression, and indicates that 2ME2 has disease modifying antirheumatic drug (DMARD) properties.
Dr Carolyn Sidor, EntreMed’s vice president and chief medical officer, commented on the study, “It is now accepted that angiogenesis is a main contributor in the development and promotion of rheumatoid arthritis. Therefore, a potential way to attenuate the development of this disease is to disrupt the blood supply. The data being presented demonstrate that 2ME2, a known antiangiogenic agent, has the potential to be a disease modifying antirheumatic drug candidate.”
The data were presented at the XXXV International Congress of Physiological Sciences during the annual meeting of the American Association of Immunologists in San Diego, California.
In addition to preclinical studies, EntreMed is currently evaluating 2ME2 formulations (Panzem Capsules and Panzem NCD) in phase I and II clinical cancer studies.