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Semafore's SF1126 Exhibits Antitumor and Antiangiogenic Activity

INDIANAPOLIS, Jan. 9 /PRNewswire/ -- Semafore Pharmaceuticals Inc. today announced that a paper published in Cancer Research (2008; Vol. 68, Issue 1: 206-215) reports that SF1126, the company's lead product candidate, exhibits antitumor and antiangiogenic activity.

The paper, entitled "A Vascular Targeted Pan Phosphoinositide 3-Kinase Inhibitor Prodrug, SF1126, with Antitumor and Antiangiogenic Activity," is based on preclinical studies conducted by Semafore and collaborators at Children's Healthcare of Atlanta, Emory University School of Medicine, and M.D. Anderson Cancer Center. Phosphoinositide 3-kinase (PI3K) is a powerful pathway and an emerging cancer target for inhibition. In the studies reported, SF1126 showed favorable pharmacokinetics and pharmacodynamic effects as indicated by inhibition of downstream signaling elements both in vitro and in vivo. In addition, SF1126 displayed potent antitumor and antiangiogenic activity in vivo, in mouse models, against a variety of human cancer cell types, including prostate, breast, neuroblastoma, and glioblastoma.

SF1126 differs from other known PI3K inhibitors in that it has a homing feature designed to localize more drug in the tumor compartment. Based on the studies reported in the paper, SF1126 also significantly enhanced the activity of docetaxel in a combination regiment in a prostate cancer model.

"The data further support our belief that SF1126 is a viable pan PI3K inhibitor as we continue Phase I clinical trials," said Ed Jacobs, Semafore's president and chief executive officer. "SF1126 continues to support the paradigm shift in cancer treatment that will see the application of highly targeted therapeutic drugs that inhibit the powerful PI3K pathway."

About SF1126

SF1126 is a small molecule conjugate containing a pan-PI3K inhibitor that selectively inhibits all PI3K class IA isoforms and other key members of the PI3K superfamily, including DNA-PK and mTOR. A major factor in tumor resistance to approved chemotherapy agents is thought to be the activation of the PI3K/PTEN pathway. As a result, it is thought that inhibiting this pathway, via SF1126, could cause the resetting of sensitivity to approved agents and exhibit synergistic anticancer effects. SF1126 is currently in multiple phase I trials in cancer patients.

About Semafore

Semafore is a clinical stage drug discovery and development company focused on small molecule modulators of the PI3 kinase and PTEN cell signaling pathway, a promising target pathway for multiple disorders, including the company's focus -- cancer. Semafore is one of the first biopharmaceutical companies to focus on both PI3K and PTEN and has successfully discovered and is developing a portfolio of drug candidates addressing these targets. For more information see the company's Web site at


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