Semafore's SF1126 Exhibits Antitumor and Antiangiogenic Activity

Thursday, January 10, 2008 General News
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INDIANAPOLIS, Jan. 9 Semafore Pharmaceuticals Inc. todayannounced that a paper published in Cancer Research (2008; Vol. 68, Issue 1:206-215) reports that SF1126, the company's lead product candidate, exhibitsantitumor and antiangiogenic activity.

The paper, entitled "A Vascular Targeted Pan Phosphoinositide 3-KinaseInhibitor Prodrug, SF1126, with Antitumor and Antiangiogenic Activity," isbased on preclinical studies conducted by Semafore and collaborators atChildren's Healthcare of Atlanta, Emory University School of Medicine, andM.D. Anderson Cancer Center. Phosphoinositide 3-kinase (PI3K) is a powerfulpathway and an emerging cancer target for inhibition. In the studiesreported, SF1126 showed favorable pharmacokinetics and pharmacodynamic effectsas indicated by inhibition of downstream signaling elements both in vitro andin vivo. In addition, SF1126 displayed potent antitumor and antiangiogenicactivity in vivo, in mouse models, against a variety of human cancer celltypes, including prostate, breast, neuroblastoma, and glioblastoma.

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

"The data further support our belief that SF1126 is a viable pan PI3Kinhibitor as we continue Phase I clinical trials," said Ed Jacobs, Semafore'spresident and chief executive officer. "SF1126 continues to support theparadigm shift in cancer treatment that will see the application of highlytargeted therapeutic drugs that inhibit the powerful PI3K pathway."

About SF1126

SF1126 is a small molecule conjugate containing a pan-PI3K inhibitor thatselectively inhibits all PI3K class IA isoforms and other key members of thePI3K superfamily, including DNA-PK and mTOR. A major factor in tumorresistance to approved chemotherapy agents is thought to be the activation ofthe PI3K/PTEN pathway. As a result, it is thought that inhibiting thispathway, via SF1126, could cause the resetting of sensitivity to approvedagents and exhibit synergistic anticancer effects. SF1126 is currently inmultiple phase I trials in cancer patients.

About Semafore

Semafore is a clinical stage drug discovery and development companyfocused on small molecule modulators of the PI3 kinase and PTEN cell signalingpathway, a promising target pathway for multiple disorders, including thecompany's focus -- cancer. Semafore is one of the first biopharmaceuticalcompanies to focus on both PI3K and PTEN and has successfully discovered andis developing a portfolio of drug candidates addressing these targets. Formore information see the company's Web site at Corporate Media Semafore Pharmaceuticals Inc. Russo Partners LLC Bob Marshall or Ed Jacobs David Schull or Timothy Engel (480) 278-8200 (212) 845-4271

SOURCE Semafore Pharmaceuticals Inc.

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