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Rineterkib is an orally available small molecule inhibitor targeting extracellular signal-regulated kinases 1 and 2 (ERK1/2), key components of the MAPK signaling pathway. It is being developed primarily for the treatment of cancers characterized by activating mutations in the MAPK pathway, including myelofibrosis, malignant melanoma, and other advanced solid tumors. Rineterkib has been studied both as a monotherapy and in combination with other agents such as ruxolitinib (a JAK inhibitor) or RAF inhibitors. Its mechanism involves direct inhibition of ERK-mediated signal transduction, thereby blocking cell proliferation signals downstream of RAS/RAF/MEK activation[1][2][3][4][5][6]. The drug was originally developed by Novartis.
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