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Ribociclib + capecitabine is a combination therapy consisting of a selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor and a fluoropyrimidine carbamate prodrug. Ribociclib works by inhibiting the CDK4/6-cyclin D complex, which prevents the phosphorylation of the retinoblastoma (Rb) protein, thereby blocking cell cycle progression from G1 to S phase. Capecitabine is an orally administered systemic prodrug of 5-fluorouracil (5-FU), which is converted to 5-FU by thymidine phosphorylase in tumor tissues. The active metabolite 5-FU inhibits DNA synthesis and slows tumor growth by inhibiting thymidylate synthase and incorporating into RNA and DNA. This combination has been investigated primarily for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer, particularly in patients who have progressed on prior endocrine therapies and CDK4/6 inhibitors.
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