Verastem Announces New Research Published in the Journal Cell That Highlights the Potential of FAK Inhibition to Enhance the Efficacy of Anti-Tumor Immunotherapy

On September 24, 2015 Verastem, Inc. (NASDAQ:VSTM), focused on discovering and developing drugs to treat cancer by the targeted killing of cancer stem cells, reported that researchers from the University of Edinburgh have published a study in the journal Cell which highlights the potential of FAK inhibition to enable the body’s immune system to fight cancer (Press release, Verastem, SEP 24, 2015, View Source [SID:1234507543]).

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The paper discusses results from preclinical research showing that focal adhesion kinase (FAK), a protein which is often overproduced in tumors, enables cancer cells to evade attack by the immune system. In this study, researchers discovered that FAK inhibition can modulate the balance of immune cells in the tumor enabling an immune response to destroy the cancer cells.

Dr. Alan Serrels, one of the lead authors, at the Edinburgh Cancer Research UK Centre at the University of Edinburgh, said: "FAK is hi-jacked by cancer cells to protect them from the immune system. This exciting research reveals that by blocking FAK, we’ve now found a promising new way to help the immune system recognise the cancer and fight it. FAK inhibitors are already in clinical trials and have generally been well tolerated, so could potentially be an excellent complement to existing immunotherapy treatments."

The research, which was carried out in mice with squamous cell carcinoma, showed complete T-cell mediated tumor regression when the mice were administered the FAK inhibitor. This research is the first to demonstrate that FAK inhibition increases the presence of cytotoxic T cells in the tumor and decreases the presence of immunosuppressive T regulatory cells.

"This is a ground-breaking paper which shows that FAK inhibitors can induce tumor regression through a T cell-mediated mechanism," said Jonathan Pachter, Ph.D., Verastem Head of Research and co-author of the study. "These early data are encouraging and provide important support for the thesis that FAK inhibitors such as defactinib may be useful in combination with immuno-oncology agents with the goal of yielding more durable responses for a greater number of cancer patients."
The research was funded by Cancer Research UK, European Research Council, and Medical Research Council.
The full press release from Cancer Research UK can be accessed here: http://bit.ly/1gRLBC0

The paper, titled "Nuclear FAK controls chemokine transcription, Tregs and evasion of anti-tumor immunity," can be accessed at http://bit.ly/1KTb3mW.

About VS-6063
VS-6063 (defactinib) is an orally available compound designed to target cancer stem cells through the potent inhibition of focal adhesion kinase (FAK). Cancer stem cells are an underlying cause of tumor resistance to chemotherapy, recurrence and ultimate disease progression. Research has demonstrated that FAK activity is critical for the growth and survival of cancer stem cells. VS-6063 is currently being studied in the registration-directed COMMAND trial in mesothelioma (www.COMMANDmeso.com), a "Window of Opportunity" study in patients with mesothelioma prior to surgery, a Phase 1/1b study in combination with paclitaxel in patients with ovarian cancer, a trial in patients with KRAS-mutated non-small cell lung cancer and a trial evaluating the combination of VS-6063 and VS-5584 in patients with relapsed mesothelioma. VS-6063 has been granted orphan drug designation for use in mesothelioma in the U.S. and EU.

About VS-4718
VS-4718 is an orally available compound designed to target cancer stem cells through the potent inhibition of focal adhesion kinase (FAK). VS-4718 is currently being studied in a Phase 1 dose escalation study in patients with advanced cancers.