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ERAS-3490 is an orally available, CNS-penetrant small molecule inhibitor specifically targeting the KRAS G12C mutation. Developed by Erasca, it is designed to overcome limitations of first-generation KRAS G12C inhibitors by achieving robust penetration of the blood-brain barrier and demonstrating both systemic and central nervous system (CNS) anti-tumor activity. Preclinical studies have shown that ERAS-3490 potently inhibits cell proliferation and RAS/MAPK signaling in KRAS G12C mutant cell lines, with significant anti-tumor effects in subcutaneous and intracranial models of non-small cell lung cancer (NSCLC). The drug is being developed primarily for the treatment of solid tumors harboring the KRAS G12C mutation, including NSCLC with a focus on patients at risk for or with CNS metastases[2][3][8].
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