REPORT DEMONSTRATES ACTIVITY OF 2ME2 WITH PACLITAXEL IN HEAD AND NECK CARCINOMA

EntreMed has announced a published preclinical report supporting the use of 2-methoxyestradiol (2ME2) in combination with paclitaxel in the treatment of recurrent or advanced head and neck squamous cell carcinoma (HNSCC).

Paclitaxel is a first-line treatment for recurrent HNSCC. These findings, published in the December 2004 issue of Clinical Cancer Research, demonstrated that 2ME2 exhibited both antitumor and antiangiogenic activity in an animal model of HNSCC.

EntreMed is currently conducting clinical studies with 2ME2 (Panzem) in patients with advanced cancer. Specifically, the study demonstrated that 2ME2, alone or in combination with paclitaxel, significantly inhibited tumor growth in a preclinical xenograft model. The study also showed that 2ME2 inhibits tumor cell proliferation and promotes apoptosis (cell death) in vitro, as well as providing an additive or synergistic effect with paclitaxel. The study further demonstrated that 2ME2 inhibits HIF-1alpha (hypoxia- inducible factor) nuclear activity in a dose-dependent manner and that 2ME2 affects the expression of HIF-1alpha regulated genes, specifically up- regulating bid, a pro-apoptotic bcl-2 family member, and inhibits the expression of vascular endothelial growth factor, an angiogenic growth factor.