Semafore Pharmaceuticals to Present SF1126 Clinical Data at ASCO Annual Meeting

Phase 1 Study of Multi-Kinase, PI3K/mTOR Inhibitor in Solid Tumors and B-cell Malignancies Accepted for Poster Discussion Session

INDIANAPOLIS, May 26, 2011 (GLOBE NEWSWIRE) -- Semafore Pharmaceuticals today announced that Phase 1 clinical data for SF1126 will be presented at the 47th Annual Meeting of the American Society of Clinical Oncology (ASCO) being held June 3-7, 2011 in Chicago, Illinois. SF1126 is a novel peptidic prodrug that converts to LY294002, one of the most widely studied small molecule inhibitors of both phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR). The data presentation at ASCO 2011 will highlight the safety, tolerability and activity profile of SF1126 in patients with advanced solid tumors and B-cell malignancies.

A summary of the company's ASCO poster presentation is below and the full abstract can be accessed on the ASCO website at

Developmental Therapeutics - Experimental Therapeutics:
Saturday June 4, 2011 - 2:00 p.m. to 6:00 p.m. (CDT)
Abstract Number: 3015
Title: Phase I study of the multikinase prodrug SF1126 in solid tumors and B-cell malignancies
Poster Room: S403
Discussion Session: 
Saturday June 4, 2011 - 5:00 p.m. to 6:00 p.m. (CDT)
Location: Room S406

About SF1126 and the PI3K Pathway

The phosphatidylinositol 3-kinase (PI3K) signaling pathway is vital to several essential biological processes, such as cell growth, survival, motility, and metabolism. PI3K is commonly altered in human cancers, making inhibition of the target attractive for cancer therapy.  However, the role of PI3K in a wide range of normal biologic processes raises potential concerns about its inhibition in non-cancerous tissues.

As the only PI3K/mTOR inhibitor "prodrug" currently in development, Semafore's SF1126 product candidate is designed to overcome these concerns by accumulating preferentially in tumor tissue in an attempt to maximize efficacy and minimize toxicity.  SF1126 is a peptidic prodrug that converts to LY294002, one of the most widely studied small molecule inhibitors of multiple, cancer-specific kinase targets (including all Class I PI3K isoforms, mTOR, Pim-1, DNA-PK, and PLK1) that historically suffered from poor solubility.  LY294002 is conjugated to an Arg-Gly-Asp (RGD) peptide via a cleavable linker to form SF1126, which has improved properties for clinical use.  As a prodrug with enhanced solubility and site selectivity due to targeting of RGD-recognizing integrin receptors, SF1126 opened up a new avenue for the clinical development of LY294002.

About Semafore Pharmaceuticals

Semafore Pharmaceuticals is a private, clinical-stage biotechnology company dedicated to the discovery and development of novel small molecule signal transduction inhibitors targeting the phosphoinositide-3-kinase (PI3K) pathway for the treatment of cancer and other serious diseases.  In addition to SF1126, the Company's pipeline includes SF2626, a next-generation dual MEK/PI3K inhibitor that is designed to simultaneously inhibit an additional key pathway critical to cancer progression using a single molecule. For more information, visit the company's web site at


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