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Luvometinib (FCN-159) is an orally bioavailable, highly potent, and selective small molecule inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2). Developed by Fosun Pharma, it targets the MAPK/ERK signaling pathway, which is frequently over-activated in various cancers and genetic disorders due to mutations in BRAF, NRAS, or NF1. Luvometinib is being investigated for the treatment of pediatric low-grade glioma (pLGG), neurofibromatosis type 1 (NF1) associated plexiform neurofibromas, Langerhans cell histiocytosis, and other RAS/MAPK pathway-driven malignancies. It was designed based on the structure of trametinib but demonstrates significantly higher selectivity for activated MEK1/2. The drug has shown promising efficacy in clinical trials, particularly in pediatric populations with BRAF-mutant or NF1-mutant tumors.
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