Journal Blood: Pyk2 promotes tumor progression in multiple myeloma

On November 7, 2014, Verastem, Inc., a company focused on discovering and developing drugs to treat cancer by the targeted killing of cancer stem cells, announced that a paper, titled “PYK2 Promotes Tumor Progression in Multiple Myeloma,” has been published in Blood (2014 Oct 23;124(17):2675-86), a peer-reviewed medical journal published by the American Society of Hematology. “These data demonstrate that PYK2 is a promising therapeutic target in multiple myeloma,” said Jonathan Pachter, Ph.D., Verastem Head of Research. “These results build upon prior scientific findings demonstrating the activity of dual FAK/PYK2 inhibitors across multiple types of cancer and support the ongoing clinical development of VS-4718.” The paper describes the finding that patients with multiple myeloma have a higher expression of proline-rich tyrosine kinase 2 (PYK2), a member of the focal adhesion kinase (FAK) family, compared to healthy individuals, and that PYK2 plays a tumor-promoting role in myeloma progression. The FAK family is composed of just two members, FAK and PYK2, which are highly homologous. In the published study, it was demonstrated that inhibition of PYK2 led to reduction of myeloma tumor growth in vivo as well as decreased cell proliferation, cell cycle progression, and adhesion ability in vitro. In contrast, overexpression of PYK2 was shown to promote the malignant phenotype, as evidenced by enhanced tumor growth and reduced survival. The paper further describes how administration of Verastem’s FAK/PYK2 inhibitor, VS-4718, effectively inhibited myeloma cell growth in both in vitro and in vivo models. “In addition to this work recently published by our collaborators at the Dana Farber Cancer Institute, we have been conducting further research and collaborating with scientific leaders to understand the potential of cancer stem cell inhibitors in hematological malignancies”, continued Dr. Pachter. “We believe that inhibitors of FAK and PYK2, such as VS-4718, may be useful in the treatment of many types of cancer, particularly where there is minimal residual disease with enrichment of cancer stem cells following chemotherapy. We and our collaborators will be presenting additional research at the upcoming American Society of Hematology in December.” “VS-4718 is currently being evaluated in a Phase 1 dose escalation clinical trial in patients with advanced solid tumors,” said Robert Forrester, President and Chief Executive Officer of Verastem. “A new Phase 1 trial of VS-4718 in hematological malignancies is currently planned to begin in the first quarter of 2015.” The full publication can be accessed online here. 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 solid tumors. About Verastem, Inc. Verastem, Inc. (NASDAQ:VSTM) is discovering and developing drugs to treat cancer by the targeted killing of cancer stem cells. Cancer stem cells are an underlying cause of tumor recurrence and metastasis. Verastem is developing small molecule inhibitors of signaling pathways that are critical to cancer stem cell survival and proliferation: FAK, PI3K/mTOR and Wnt. For more information, please visit www.verastem.com.