EntreMed Presents Preclinical Data for Second Generation 2ME2 Compounds

EntreMed has presented preclinical results for its lead 2-methoxyestradiol (2ME2) analogs, demonstrating improved pharmacokinetic parameters, reduced metabolism and enhanced antitumor activity in preclinical animal models, and representing the next generation of molecules with potential for broad application in cancer and other diseases.

Results from a first preclinical study, conducted by EntreMed collaborators, demonstrated enhanced activity of ENMD-1198 both in vitro and in an orthotopic lung cancer model when compared to 2ME2. Furthermore, a dose-dependent increase in survival was observed, indicating the potential for ENMD-1198 in the treatment of human lung cancers.

In a second preclinical study, EntreMed scientists demonstrated that 2ME2 analogs improved median survival time significantly in a metastatic lung cancer model and reduced tumor volumes significantly in a separate orthotopic cancer model. The study further demonstrated that 2ME2 analogs are microtubule destabilizing agents that cause a reduction in HIF-1alpha protein levels. HIF-1alpha is over-expressed in more than 70 percent of human cancers and their metastases, including breast, prostate, head and neck, brain, and lung cancers.

Based on its antitumor activity, enhanced microtubule disruption and HIF-1alpha inhibition, analog ENMD-1198 is undergoing further preclinical evaluation and IND-directed toxicology studies.