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Nuvalent Announces Publication in Cancer Discovery Detailing Design and Characterization of ROS1-selective inhibitor NVL-520
Publication provides comprehensive assessment of NVL-520's activity spanning preclinical characterization and preliminary clinical case studies CAMBRIDGE,
About this update from Nuvalent, Inc.
[{"type":"text","content":"Publication provides comprehensive assessment of NVL-520's activity spanning preclinical characterization and preliminary clinical case studies\nCAMBRIDGE, Mass., Dec. 13, 2022 /PRNewswire/ -- Nuvalent, Inc. (Nasdaq: NUVL), a clinical-stage biopharmaceutical company focused on creating precisely targeted therapies for clinically proven kinase targets in cancer, today announced the publication of a manuscript in Cancer Discovery, a journal of the American Association for Cancer Research, which describes the design and characterization of NVL-520 and details Nuvalent's approach to rationally targeting ROS1. NVL-520 is currently being studied in the ongoing ARROS-1 Phase 1/2 clinical trial for patients with advanced ROS1-positive non-small cell lung cancer (NSCLC) and other solid tumors.\n\n \n \n \n \n \n \n\n \nThe paper, entitled \"NVL-520 is a selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations,\" is published online and can be accessed here: https://aacrjournals.org/cancerdiscovery/article/doi/10.1158/2159-8290.CD-22-0968/\n\"The ROS1 kinase is a clinically validated target for the treatment of NSCLC, and ROS1 tyrosine kinase inhibitors (TKIs) are established as an important treatment option for ROS1-driven lung cancers. However, limitations do exist with available ROS1 TKIs, including treatment-emergent drug resistance, off-target neurological adverse events, and inadequate control or prevention of brain metastases,\" said senior author Jessica J. Lin, M.D., Thoracic Oncologist at Mass General Cancer Center, Assistant Professor of Medicine at Harvard Medical School, and investigator in the ARROS-1 trial. \"As described in this paper and earlier this year at the EORTC-NCI-AACR Symposium, preclinical characterization and preliminary clinical data support the opportunity for NVL-520 to overcome these limitations as a potential best-in-class ROS1 kinase inhibitor and provide compelling rationale for its ongoing evaluation in patients with TKI-experienced ROS1 fusion-positive cancers and planned evaluation in treatment-naïve patients.\"\nThe paper details the design principles underlying the activity of NVL-520 against ROS1 and its most commonly occurring resistance mutation, ROS1 G2032R, and a molecular rationale for the selectivity of NVL-520 for ROS1 over the structurally-rel...