EntreMed says studies demonstrate significant antitumor effect of ENMD-1198

By E. Janene Geiss

Philadelphia, Nov. 17 - EntreMed, Inc. said preclinical results for its novel tubulin binding agent ENMD-1198 demonstrate that it is an orally active, microtube disrupting agent that leads to arrest of cell division and apoptosis in tumor cells.

ENMD-1198 is a new chemical entity based on a modified chemical structure of 2-methoxyestradiol, or 2ME2, and designed to decrease metabolism while retaining 2ME2's multiple mechanisms of action, including inducing apoptosis, binding microtubules and inhibiting HIF-lalpha, according to a company news release.

The study also demonstrated that ENMD-1198 exerts antiangiogenic activity that further contributes to its overall antitumor effects. Preclinical results support its potential for broad application in cancer, officials said.

"ENMD-1198 is a novel molecule with potent antitumor and antiangiogenic properties. Although ENMD-1198 shares many of the mechanisms of 2ME2, its activity profile is significantly different and, as such, we expect that the two compounds will be used to treat different tumors. On this basis, we are planning to move forward with clinical development of both compounds for use in treating cancer patients," EntreMed vice president and chief medical officer Carolyn F. Sidor said in the release.

The findings were presented Thursday during a poster session at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics in Philadelphia.

Results from the IND-directed preclinical 28-day toxicology studies also were presented, demonstrating that ENMD-1198 affects cell populations with a high proliferative rate, including bone marrow, gastrointestinal tract and lymphoid organs, officials said. These effects are common with approved cancer agents and can be monitored in the clinic.

EntreMed has completed IND-enabling studies for this compound, Sidor said, and the company remains on schedule for submitting an IND by the end of this year.

Rockville, Md.-based EntreMed is a clinical-stage pharmaceutical company developing therapeutics primarily for cancer and inflammation.

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