EntreMed Shows Increased Survival With MKC-1 in Preclinical Renal Cell Ca...( Results Consistent with MKC-...),Health

Results Consistent with MKC-1 Akt-mTOR Inhibitor Mechanism

ROCKVILLE, Md., Oct. 25 /PRNewswire-FirstCall/ -- EntreMed, Inc. (Nasdaq: ENMD), a clinical-stage pharmaceutical company developing therapeutics for the treatment of cancer and inflammatory diseases, today announced the presentation of results for its cell cycle inhibitor, MKC-1, in preclinical renal cell carcinoma (RCC) models. The results were presented at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics in San Francisco, California.

(Logo: http://www.newscom.com/cgi-bin/prnh/20010620/ENMDLOGO )

Activation of the oncogenic kinase Akt and the mTOR pathway are known to be adverse prognostic factors and contributors to the pathology of metastatic RCC, therefore inhibitors of these pathways are of significant interest for treatment of this disease. Human RCC cell lines in vitro were shown to have marked sensitivity to MKC-1. MKC-1 inhibited both Akt and mTOR pathway activation in vitro, and was further evaluated in a preclinical model consisting of a xenograft of the human RCC cell line, Caki-1. Orally- administered MKC-1, but not sunitinib malate (Sutent(R)), significantly increased survival of tumor-bearing animals in this model. Examination of tumors following five days of oral treatment with MKC-1 revealed inhibition of the Akt-mTOR pathway, as well as decreased angiogenesis and cell proliferation within the tumors. These preclinical results support further evaluation of MKC-1 for the treatment of renal cell carcinoma.

MKC-1 is a novel, orally-active cell cycle inhibitor with in vitro and in vivo efficacy aga
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