PI3K inhibitor

From Yenra

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 Pharmaceuticals' 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.