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Verastem Oncology Announces Preclinical Presentations for New Oral G12D Inhibitor and for Avutometinib and Defactinib Combination as a Backbone of Therapy for RAS/MAPK Driven Cancers at AACR Annual Meeting 2024

GFH375 (VS-7375), a potential best-in-class oral KRAS G12D (ON/OFF) inhibitor, demonstrated potent anti-tumor activity in pancreatic and colorectal cancer

articleVerastem, Inc.March 5, 20245/company/verastem-inc/news/verastem-oncology-announces-preclinical-presentations-for-new-oral-g12d-inhibitor-and
Verastem Oncology Announces Preclinical Presentations for New Oral G12D Inhibitor and for Avutometinib and Defactinib Combination as a Backbone of Therapy for RAS/MAPK Driven Cancers at AACR Annual Meeting 2024

About this update from Verastem, Inc.

[{"type":"text","content":"\n GFH375 (VS-7375), a potential best-in-class oral KRAS G12D (ON/OFF) inhibitor, demonstrated potent anti-tumor activity in pancreatic and colorectal cancer models; Partner GenFleet plans to submit IND in H1 2024\n\n\nPreclinical data demonstrate strong anti-tumor activity of avutometinib with FAK inhibitor combination with standard-of-care chemotherapy in pancreatic cancer models; supports the scientific rationale for ongoing RAMP 205 Phase 1/2 trial\n\n\nAvutometinib with FAK inhibitor combination overcomes resistance to BRAF and MEK inhibitors and to immunotherapy in patient-derived melanoma models\n\n\n BOSTON--(BUSINESS WIRE)--\nVerastem Oncology (Nasdaq: VSTM), a biopharmaceutical company committed to advancing new medicines for patients, today announced that preclinical data will be presented in five posters at the American Association for Cancer Research (AACR) Annual Meeting 2024 to be held on April 5-10 in San Diego, California. The presentations will highlight anti-tumor efficacy of GFH375 (VS-7375), a potent and selective orally bioavailable KRAS G12D (ON/OFF) inhibitor, and will also show data of RAF/MEK clamp plus FAK inhibition in pancreatic ductal adenocarcinoma (PDAC) models supporting the ongoing RAMP 205 trial. Additional presentations will support the use of avutometinib and FAK inhibitor combination in cutaneous melanoma models to overcome resistance to BRAF and MEK inhibitors, resistance to immunotherapy, and brain metastasis.\n\n\n“For the first time, GenFleet and Verastem will present potency, selectivity, anti-tumor efficacy, and bioavailability data on GFH375 (VS-7375), a potential best-in-class orally active KRAS G12D (ON/OFF) inhibitor. We look forward to an IND submission by GenFleet in China in H1 2024,” said Jonathan Pachter, Ph.D., chief scientific officer of Verastem Oncology. “Additionally, preclinical data will be presented demonstrating that the combination of avutometinib and a FAK inhibitor with standard-of-care chemotherapy can induce tumor regressions in pancreatic cancer models, providing the scientific rationale for the ongoing RAMP 205 Phase 1/2 study evaluating the combination of avutometinib, defactinib, gemcitabine, and nab-paclitaxel in first-line metastatic pancreatic ductal adenocarcinoma. Collectively, these data from the five posters build on our desire to advance treatments th...

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