Novel peptides developed through EntreMed, Affymax collaboration show antiangiogenic activity in study

By E. Janene Geiss

Philadelphia, Dec. 13 - EntreMed, Inc. and Affymax, Inc. said Tuesday that preclinical data on novel peptides developed from a collaboration based on initial findings that a fragment of tissue factor pathway inhibitor demonstrated antiangiogenic activity in preclinical models and that this activity was modulated through the very low density lipoprotein receptor.

In preclinical studies, EntreMed and Affymax said they have discovered novel synthetic peptides that exhibited improved antiangiogenic activity and very low density lipoprotein (VLDL) receptor binding in vitro, according to a company news release.

These peptides were assessed in vivo in the Matrigel plug angiogenesis model and one of these peptides inhibited angiogenesis by negative 75% at 2 mg. These data demonstrate that structure-function studies have yielded novel synthetic peptides with significantly better antiangiogenic activity in preclinical models than a peptide fragment of tissue factor pathway inhibitor, officials said.

Additionally, these results suggest that the VLDL receptor is critical for the selection of molecules for further development.

"We are pleased with progress of this collaboration and the results to date. These data demonstrate the importance of our collaborative efforts with EntreMed and suggest a potential mechanism for developing drugs for the treatment of cancer and other diseases that are dependent on angiogenesis," said Robert B. Naso, executive vice president of research and development at Affymax, in the release.

The data were presented at the American Society for Hematology annual meeting held this week in Atlanta.

EntreMed said it has previously reported the identification of a peptide fragment of TFPI, a naturally occurring anti-coagulant protein that blocks tumor growth and angiogenesis in preclinical models. In preclinical studies, the TFPI- derived peptide's antiangiogenic mechanism of action has been shown, officials said.

Affymax, Inc. is a Palo Alto, Calif., clinical-stage pharmaceutical company that is developing synthetic peptide-based drugs against clinically validated targets for the treatment of kidney diseases and cancer.

EntreMed, Inc. is a Rockville, Md., clinical-stage pharmaceutical company developing therapeutic candidates primarily for the treatment of cancer and inflammation.

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