EntreMed, Inc, a clinical-stage pharmaceutical company developing therapeutics for the treatment of cancer and inflammatory diseases, has commenced a phase I, dose-escalation study for its selective kinase inhibitor, ENMD-2076, in advanced cancer patients.

Dr Wells Messersmith, University of Colorado Cancer Centre, will serve as co-principal investigator for the study. Additional centres are expected to join Colorado as study sites this quarter.

ENMD-2076 is a novel, selective kinase inhibitor with potent activity against Aurora A and tyrosine kinases linked to the promotion of cancer and inflammatory diseases. ENMD-2076 acts through multiple pathways resulting in antiproliferative activity and the inhibition of angiogenesis. ENMD-2076 has demonstrated substantial, dose-dependent efficacy as a single agent in multiple preclinical models, including tumour regression in breast, colon, and leukaemia models. Importantly, ENMD-2076 is an oral agent that has shown an acceptable toxicity profile in preclinical studies without cardiovascular toxicity.

The phase I study will assess safety and tolerability of orally administered ENMD-2076 in refractory cancer patients. In addition, pharmacokinetics will be assessed to determine a dose-dependent response to treatment with ENMD-2076.

Carolyn F. Sidor, M.D., M.B.A., vice president and chief medical officer, EntreMed, commented on the study, "Commencement of this phase I study marks the achievement of a critical milestone in our clinical development programme and further supports our strategy of focusing on orally-administered, small molecule drugs with multiple mechanisms of action. Data from preclinical studies with ENMD-2076 demonstrate its significant ant tumour potential as a single agent in a variety of tumour types. Through this Phase 1 study, we expect to not only determine ENMD-2076's safety profile and appropriate Phase 2 dosing schedule, but which tumour types may be better suited for this compound. We plan to initiate a second Phase 1 study in patients with haematological cancers later this year."

The administration of ENMD-2076 to the first patient in this important phase I study will trigger a milestone payment by EntreMed pursuant to EntreMed's acquisition of Miikana Therapeutics, Inc. in January 2006. Under the terms of the merger agreement with Miikana, the dosing of the first patient triggers a $2 million payment to the former Miikana stockholders, either in cash or shares of EntreMed common stock.

James S. Burns, president and chief executive officer, EntreMed said, "ENMD-2076 is an exciting selective kinase inhibitor with potent single agent activity that has induced tumour regression in multiple preclinical models. ENMD-2076, developed internally, is consistent with our focus on investing behind oncology drug candidates with strong single-agent activity and with our continuing interest in selective kinase inhibitors. In parallel with the clinical trial, we will seek a pharmaceutical or biotech partner to help accelerate the development of our novel selective kinase inhibitor."