|February 24, 2014|
|Cancer Research Publication Highlights Importance of Merlin Loss and Cancer Stem Cells in Mesothelioma|
Research Demonstrates Cooperativity between Loss of Merlin and p16/ARF in Driving the Development of Highly Aggressive Disease In Vivo
Malignant mesothelioma is a highly aggressive, asbestos-related cancer frequently marked by mutations in tumor suppressor genes Neurofibromatosis 2 (NF2) and p16/ARF. Inactivation of NF2 results in the absence of its protein product, merlin. Merlin loss is a critical driver of mesothelioma tumorigenesis and correlates with FAK inhibitor sensitivity in preclinical models. p16 and ARF are tumor suppressors, which bind to and regulate proteins involved in cell cycle progression and apoptosis. NF2 and p16/ARF are frequently co-inactivated in mesothelioma. The study results demonstrated in vivo that inactivation of NF2 and p16/ARF cooperate to drive the development of highly aggressive mesothelioma characterized by enhanced disease progression and an increase in cancer stem cells.
Verastem’s lead compound is VS-6063, an orally available agent that targets cancer stem cells through potent inhibition of focal adhesion kinase (FAK), a critical signaling pathway in the development and survival of cancer stem cells. Cancer stem cells are an underlying cause of tumor resistance to chemotherapy, recurrence, and ultimate disease progression.
“These findings provide strong genetic evidence for the cooperativity
between merlin and p16/ARF loss of function in driving the development
of highly aggressive malignant mesothelioma marked by an enhanced
presence of cancer stem cells that drive tumor progression,” said
"The ongoing COMMAND trial is designed to evaluate the effect of VS-6063
in patients with mesothelioma,” said Dr.
About Malignant Pleural Mesothelioma
Malignant pleural mesothelioma is an aggressive form of cancer that
occurs in the mesothelium, the thin layer of tissue that covers the
lungs. Mesothelioma is associated with exposure to asbestos in most
cases. According to the
VS-6063 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 by
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.
About Verastem, Inc.
This press release includes forward-looking statements about the
Company’s strategy, future plans and prospects, including statements
regarding the development of the Company’s compounds, including VS-6063,
VS-4718, VS-6062 and the Company’s FAK inhibition program, the timeline
for clinical development and regulatory approval of the Company’s
compounds, the expected timing for the reporting of data from ongoing
trials, and the structure of the Company’s planned or pending clinical
trials, and potential indications for clinical development. The words
“anticipate,” “appear,” “believe,” “estimate,” “expect,” “intend,”
“may,” “plan,” “predict,” “project,” “target,” “potential,” “will,”
“would,” “could,” “should,” “continue,” and similar expressions are
intended to identify forward-looking statements, although not all
forward-looking statements contain these identifying words. Each
forward-looking statement is subject to risks and uncertainties that
could cause actual results to differ materially from those expressed or
implied in such statement. Applicable risks and uncertainties include
the risks that the preclinical testing of the Company’s compounds and
preliminary data from clinical trials may not be predictive of the
results or success of ongoing or later clinical trials, that data may
not be available when we expect it to be, that the Company will be
unable to successfully complete the clinical development of its
compounds, including VS-6063 and VS-4718, that the development of the
Company’s compounds will take longer or cost more than planned, and that
the Company’s compounds will not receive regulatory approval or become
commercially successful products. Other risks and uncertainties include
those identified under the heading “Risk Factors” in the Company’s
Annual Report on Form 10-K for the year ended
|You may automatically receive Verastem Oncology™ financial information by e-mail. To choose your options for e-mail notification, please enter your e-mail address below and click Submit. On the next page you will be able to choose from the following options:|
To change your e-mail options at any time, re-enter your e-mail address and click Submit, then adjust your form entries.