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BGB-53038 is a novel, orally administered pan-KRAS inhibitor (second generation) developed by BeiGene for the treatment of advanced or metastatic solid tumors harboring KRAS mutations or amplifications. Its mechanism of action involves inhibiting the KRAS protein, a GTPase that plays a critical role in cell signaling pathways driving cancer growth. The drug is currently being evaluated in first-in-human Phase 1 clinical trials as both monotherapy and in combination with other agents such as tislelizumab (an anti-PD-1 antibody) and cetuximab (an EGFR inhibitor). Indications under investigation include non-small cell lung cancer, colorectal cancer, esophageal cancer, pancreatic ductal carcinoma, gastrointestinal cancers, adenocarcinoma, squamous cell carcinoma, and other solid tumors with KRAS alterations.
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