Back to Archived News
Semafore Pharmaceuticals Announces Issuance of Key U.S. Patent Covering Composition of Matter for Novel PI3K/mTOR Pathway Inhibitor
Monday, February 22, 2010
Indianapolis, IN -- Semafore Pharmaceuticals today announced today announced the United States Patent and Trademark Office (PTO) has issued United States Patent Number 7,662,977 entitled "PI-3 Kinase Inhibitor Prodrugs." This composition of matter patent covers a genus of novel compounds that includes SF1126, Semafore’s clinical stage, small molecule inhibitor of phosphoinositide-3-kinase (PI3K) and mammalian target of rapamycin (mTOR), two key members of the PI3K signaling pathway that is vital to several essential biological processes, such as cell proliferation and survival. PI3K is commonly altered in human cancers, making inhibition of the target attractive for cancer therapy.
"We believe that the issuance of this U.S. patent recognizes the novelty and inventiveness of Semafore’s approach to create product candidates, such as SF1126, that are designed to deliver more active drug to the tumor while sparing normal tissue," said Joseph Garlich, Ph.D., Semafore’s Chief Scientific Officer. "The issuance of the new U.S. patent is a significant milestone for the Company and greatly enhances the intellectual property portfolio around our lead clinical agent, SF1126."
Semafore Pharmaceuticals also announced today that the Company received approval for a protocol amendment to expand an ongoing Phase I study to include B-cell malignancies, such as indolent non-Hodgkins lymphoma (NHL) and chronic lymphocytic leukemia (CLL). While PI3K is among the most frequently activated signaling pathways in cancer, patients with B-cell malignancies have not been treated to date with SF1126 despite promising preclinical data that provides a rationale to explore its therapeutic activity in this setting.
About SF1126
Semafore Pharmaceuticals’ lead product candidate, SF1126, inhibits both the phosphoinositide-3-kinase (PI3K) and mammalian target of rapamycin (mTOR), two key members of the PI3K signaling pathway that is vital to several essential biological processes, such as cell proliferation and survival. PI3K is commonly altered in human cancers, making inhibition of the target attractive for cancer therapy.
In view of the fact that mTOR can be activated in a PI3K-independent manner, dual PI3K-mTOR inhibitors, such as SF1126, are expected to offer a therapeutic advantage. As a prodrug that is administered in an inactive form, SF1126 is also unique among clinical stage, dual PI3K-mTOR inhibitors. Once administered, SF1126 targets specific transmembrane cell adhesion proteins known as integrins that are expressed in new tumor vasculature and within the tumor compartment. Because of the targeted design of SF1126, there is a markedly lower chance of inhibiting PI3K and mTOR in healthy, non-cancerous cells which reduces the potential for side-effects. In preclinical studies, SF1126 has shown attractive pharmacokinetic and pharmacodynamic properties and compelling efficacy in xenograft models, both as a single agent and in combination with other therapies.
Data from an ongoing Phase I clinical trial of SF1126 in patients with solid tumors recently presented at the 2009 American Society of Clinical Oncology (ASCO) Annual Meeting demonstrated selective inhibition of the PI3K pathway in tumor tissue but not in normal skin tissue. Notably, there were no clinically significant changes in glucose or insulin levels reported at biologically active doses. Upon completion of single agent Phase I trials, Semafore Pharmaceuticals expects to initiate combination trials in the near future.
About Semafore Pharmaceuticals
Semafore Pharmaceuticals is a 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. The PI3K signaling pathway is vital to several biological processes, such as cell proliferation and survival, and is commonly altered in human cancers, making inhibition of the target attractive for cancer therapy. For more information see the company’s web site at www.semaforepharma.com
Back to Archived News
