Verastem Oncology is focused on developing innovative treatments for cancers driven by RAS pathway mutations, which are associated with aggressive disease and poor patient outcomes. Their primary investigational drug, avutometinib (VS-6766), is a dual RAF/MEK inhibitor designed to target these mutations effectively. The company is committed to exploring novel treatment combinations that include avutometinib, such as its use alongside other agents like defactinib, sotorasib, and standard chemotherapy drugs. This approach aims to enhance therapeutic options for patients with difficult-to-treat cancers, including non-small cell lung cancer, pancreatic cancer, and low-grade serous ovarian cancer.

Verastem's research pipeline includes multiple clinical trials assessing the safety and efficacy of avutometinib in various cancer types, particularly those with specific genetic mutations like KRAS. The company emphasizes the importance of combination therapies to overcome resistance mechanisms and improve patient outcomes. Their ongoing studies aim to establish the effectiveness of these combinations in real-world settings, ultimately striving to provide more hope and options for patients facing challenging cancer diagnoses.

United States

Verastem Oncology (Nasdaq: VSTM) (Verastem, Inc.) is a late-stage development biopharmaceutical company committed to the development and commercialization of new medicines to improve the lives of patients diagnosed with cancer. Our pipeline is focused on novel small molecule drugs that inhibit critical signaling pathways in cancer that promote cancer cell survival and tumor growth, including RAF/MEK inhibition and FAK inhibition. 

Pursuing unexplored pathways demands that we’re purposeful in everything we do. And it’s an endeavor that’s only possible with an experienced team of employees and partners dedicated to a singular purpose: changing and improving the way cancer is treated by delivering novel therapies that address areas of high unmet need in RAS/MAPK pathway-driven cancers. At Verastem Oncology, it takes our diversity of backgrounds, expertise, perspectives, and skills to find the answers that patients need, but don’t have—yet. To join our team or for more information, please visit www.verastem.com.

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Cancer

Verastem Oncology

Low-Grade Serous Ovarian Cancer

Ovarian cancer

About VS-6766
VS-6766 is an oral small molecule inhibitor of the RAF/MEK signaling pathway. In contrast to other MEK inhibitors in development, VS-6766 blocks both MEK kinase activity and the ability of RAF to phosphorylate MEK. This unique mechanism allows VS-6766 to block MEK signaling without the compensatory activation of MEK that appears to limit the efficacy of other inhibitors.
 
About Defactinib
Defactinib (VS-6063) is an oral small molecule inhibitor of FAK and PYK2 that is currently being evaluated as a potential combination therapy for various solid tumors. The Company has received Orphan Drug designation for defactinib in ovarian cancer in the US, EU and Australia. Preclinical research by Verastem Oncology scientists and collaborators at world-renowned research institutions has described the effect of FAK inhibition to enhance immune response by decreasing immuno-suppressive cells, increasing cytotoxic T cells, and reducing stromal density, which allows tumor-killing immune cells to enter the tumor.

Avutometinib (VS-6766) +/- Defactinib (AVMAPKI FAKZYNJA CO-PACK)

Chronic lymphocytic leukemia

Follicular lymphoma

Small lymphocytic lymphoma

Duvelisib is an inhibitor of PI3K with inhibitory activity predominantly against PI3K-δ and PI3K-γ isoforms expressed in normal and malignant B-cells. Duvelisib induced growth inhibition and reduced viability in cell lines derived from malignant B-cells and in primary CLL tumor cells. Duvelisib inhibits several key cell-signaling pathways, including B-cell receptor signaling and CXCR12-mediated chemotaxis of malignant B-cells. Additionally, duvelisib inhibits CXCL12-induced T cell migration and M-CSF and IL-4 driven M2 polarization of macrophages.

 COPIKTRA (duvelisib)

Non-small cell lung carcinoma

About VS-6766
VS-6766 is an oral small molecule inhibitor of the RAF/MEK signaling pathway. In contrast to other MEK inhibitors in development, VS-6766 blocks both MEK kinase activity and the ability of RAF to phosphorylate MEK. This unique mechanism allows VS-6766 to block MEK signaling without the compensatory activation of MEK that appears to limit the efficacy of other inhibitors.

Avutometinib (VS-6766) + LUMAKRAS (sotorasib)

Pancreatic cancer

Avutometinib (VS-6766), + defactinib+gemcitabine/nab-paclitaxel

GFH375 (VS-7375) is a potential best-in-class, potent and selective oral KRAS G12D (ON/OFF) inhibitor, identified as the lead program from the Verastem Oncology discovery and development collaboration with GenFleet Therapeutics.

GFH375 (VS-7375)

About VS-6766
VS-6766 is an oral small molecule inhibitor of the RAF/MEK signaling pathway. In contrast to other MEK inhibitors in development, VS-6766 blocks both MEK kinase activity and the ability of RAF to phosphorylate MEK. This unique mechanism allows VS-6766 to block MEK signaling without the compensatory activation of MEK that appears to limit the efficacy of other inhibitors.
 
About Defactinib
Defactinib (VS-6063) is an oral small molecule inhibitor of the FAK and PYK2 signaling pathways that is currently being evaluated as a potential combination therapy for various solid tumors. Verastem Oncology has received Orphan Drug Designation for defactinib in ovarian cancer in the U.S., EU and Australia. Preclinical research by Verastem Oncology scientists and collaborators at world-renowned research institutions have described the effect of FAK inhibition to enhance immune response by decreasing immuno-suppressive cells, increasing cytotoxic T cells, and reducing stromal density, which allows tumor-killing immune cells to enter the tumor.

Verastem Oncology

Company Details