Core Insights - Arvinas, Inc. announced preclinical data for ARV-806, a PROTAC KRAS G12D degrader, demonstrating significant tumor growth inhibition in models of pancreatic, colorectal, and lung cancer, highlighting its best-in-class potential for KRAS G12D mutated cancers [1][2][5] Group 1: Drug Development and Efficacy - ARV-806 showed robust and durable KRAS G12D degradation, leading to significant tumor growth inhibition in various cancer models [1] - The drug targets both ON and OFF forms of KRAS G12D, which is the most common mutation of the KRAS protein, addressing high unmet needs in solid tumors [1][5] - In vitro studies indicated that ARV-806 degraded KRAS G12D with picomolar potency across multiple cancer cell lines without affecting wild-type and other mutant RAS isoforms [6] - Following a single intravenous dose, ARV-806 achieved over 90% degradation of KRAS G12D for seven days, with sustained effects on c-MYC suppression and BIM induction for at least five days [6] Group 2: Clinical Trials and Future Potential - Arvinas is currently evaluating ARV-806 in a Phase 1 clinical trial for patients with KRAS G12D–mutated advanced solid tumors [3] - The data suggest that ARV-806's sustained pharmacodynamic activity supports intermittent clinical dosing, indicating a potential for effective treatment regimens [3][8] - The drug demonstrated over 25-fold greater potency in reducing cancer cell proliferation and over 40-fold higher potency in degrading KRAS G12D protein compared to other clinical-stage G12D degraders [6] Group 3: Company Overview - Arvinas is a clinical-stage biotechnology company focused on developing protein degradation therapies through its PROTAC platform, targeting various diseases including cancers with KRAS mutations [7] - The company is advancing multiple investigational drugs, including ARV-806 for KRAS G12D, vepdegestrant for ER+/HER2- breast cancer, and ARV-393 for non-Hodgkin lymphoma [7]
Arvinas Presents Preclinical Data for ARV-806 Demonstrating Robust and Differentiated Activity in Models of KRAS G12D-mutated Cancer at the 2025 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics