Press release
Verastem Oncology Announces Multiple Presentations Focused on RAS/MAPK Pathway Inhibition at AACR Annual Meeting 2025
VS-7375, a potential best-in-class oral KRAS G12D (ON/OFF) inhibitor more potent than other KRAS G12D inhibitors in preclinical models VS-7375, when combined
About this update from Verastem, Inc.
[{"type":"text","content":"\nVS-7375, a potential best-in-class oral KRAS G12D (ON/OFF) inhibitor more potent than other KRAS G12D inhibitors in preclinical models\n\nVS-7375, when combined with cetuximab, demonstrated strong tumor regressions in preclinical KRAS G12D models, including complete responses in a colorectal cancer model\n\nIn a patient-derived LGSOC xenograft model, an FAK inhibitor addition to avutometinib augmented tumor regression with stronger inhibition of MAPK, PI3K and YAP/TEAD signaling than either agent alone\n\nThe combination of avutometinib, a RAF/MEK clamp, with a pan-RAF inhibitor led to strong tumor regressions in multiple NRAS- and BRAF-driven tumor models corresponding with nearly complete shutdown of RAS/MAPK pathway signaling\n\n BOSTON--(BUSINESS WIRE)--\nVerastem Oncology (Nasdaq: VSTM), a biopharmaceutical company committed to advancing new medicines for patients with RAS/MAPK pathway-driven cancers, announced today multiple oral and poster presentations at the American Association for Cancer Research (AACR) Annual Meeting 2025 to be held on April 25-30 in Chicago, Illinois. These presentations will highlight clinical and preclinical data from the Company’s development programs, including VS-7375 (GFH375), an oral KRAS G12D (ON/OFF) inhibitor and avutometinib, an oral RAF/MEK clamp, and defactinib, an oral FAK inhibitor.\n\n“At this year’s AACR annual meeting, we show that VS-7375, our oral KRAS G12D (ON/OFF) inhibitor, was found to be more potent than other KRAS G12D inhibitors in preclinical models. In addition, using a patient-derived LGSOC xenograft model, we and our collaborators further explored the mechanism by which our FAK inhibitor increases the anti-tumor efficacy of avutometinib. The results demonstrate that compared to avutometinib alone, the FAK inhibitor/avutometinib combination inhibits RAS/MAPK pathway signaling more deeply while also blocking key adaptive resistance mechanisms including PI3K and YAP/TEAD signaling,” said Jonathan Pachter, Ph.D., Chief Scientific Officer of Verastem Oncology.\n\nKey Data Presentations:\n\nOral Presentation: Minisymposium\n\n\nTitle: Correlative preclinical studies to elucidate mechanisms of synergy of the combination of the RAF/MEK clamp avutometinib and the FAK inhibitor defactinib in low-grade serous ovarian cancer\n\n\nAbstract #: 6368\n\n\nPresenter: Udai Banerji, M....