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SF1126, Semafore's PI3 Kinase Inhibitor, Found to Block Angiogenic Signaling From Both VEGF and Bv8 in Multiple Cell Lines

INDIANAPOLIS, Aug. 26 /PRNewswire/ -- Semafore Pharmaceuticals Inc. announced data presented at the Seventh International Congress on Targeted Therapies in Cancer in Washington, D.C., showing additional antiangiogenic activity of vascular-targeted PI3 kinase (PI3K) inhibitor SF1126, by blocking both VEGF and Bv8 signaling.

PI3K is part of a very powerful pathway, the PI3/AKT /mTOR pathway that has been shown to play a major role in cancer. Studies have shown that by inhibiting this pathway, tumor growth can be suppressed.

SF1126, a vascular targeted pan-PI3K inhibitor conjugate currently in Phase I clinical trials, was shown to block the pAKT pathway through which the angiogenic factors VEGF and Bv8 are involved. Bv8 is a recently identified protein that, like VEGF, plays a role in the angiogenic process and can significantly upregulate pAKT levels thereby supporting tumor growth.

In vitro inhibition of the PI3K/AKT/mTOR pathway by SF1126 was demonstrated to impede the ability of angiogenic stimulants VEGF and Bv8 to activate AKT in a dose dependant manner in two cancer cell lines (786-0 -- renal cell and PC3 prostate) and one endothelial cell line (HBEC -- human brain endothelial cells). Inhibiting Bv8 with antibodies has also been shown by others to have antitumor effects in mouse xenograft models.

"SF1126 could have additional impact in treating cancer where Bv8 is an important component of angiogenesis," said Dr. Dennis McKeever, Semafore's Chief Executive Officer. "In addition to targeting angiogenesis, SF1126 blocks key targets involved in tumor growth including mTOR, DNA-PK, PIM-1 and PLK-1. This adds another layer of versatility to what SF1126 can do as an antitumor agent."

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 a leader in the development of PI3K inhibitors and one of the first biopharmaceutical companies to focus on both PI3K and PTEN. The company has successfully discovered and is developing a portfolio of drug candidates addressing these targets.

About SF1126

There is a strong and significant biological rationale for developing PI3 kinase inhibitors to treat cancer. Phosphoinositide 3-kinase (PI3K) is the gate keeper of one of the major pathways of intracellular signal transduction that regulates cell growth, proliferation, angiogenesis, migration, differentiation, and survival. Dysregulation of the PI3K signaling pathway is believed to play an integral role in the genesis of many cancers including both solid tumors and hematologic malignancies. Cancer research and pharmaceutical drug development efforts have been aimed at discovering and developing therapeutics that inhibit PI3K with the hope of controlling cancer cell division, angiogenesis (the formation of new blood vessels for cancer

growth), proliferation and metastasis. Semafore's innovative PI3K inhibitor, SF1126, promises such hope for cancer patients.

SF1126, is a proprietary small molecule conjugate containing a pan-PI3K inhibitor that selectively inhibits all PI3K class I isoforms and other key members of the PI3K superfamily, including mTOR, DNA-PK, PLK-1,CK2, ATM and PIM-1 kinases all known to be involved in the cascade of chemical signals that control cell division. Importantly, SF1126 is designed as a dual inhibitor of both angiogenesis and cell proliferation. SF1126 is engineered to target and bind to specific integrins (alpha gamma beta 3) that are expressed on the surface of new tumor vasculature and within the tumor endothelial compartment. In tumor xenograph models Semafore demonstrated enhanced drug uptake of SF1126 which was directly attributable to the alpha gamma beta 3 targeted moiety. SF1126 is water soluble, has favorable pharmacokinetics and is well tolerated.

SF1126 is currently in Phase I clinical trials in both solid tumors and multiple myeloma.

For more information see the company's Web site at

SOURCE Semafore Pharmaceuticals Inc.
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