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Dalpiciclib + letrozole is an oral combination therapy used primarily for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Dalpiciclib is a novel, selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor that blocks cell cycle progression by inhibiting phosphorylation of the retinoblastoma protein, thereby preventing cellular proliferation in cancer cells dependent on this pathway[2][3][4]. Letrozole is a third-generation nonsteroidal aromatase inhibitor that suppresses estrogen production by inhibiting the aromatase enzyme (CYP19A1), which converts androgens to estrogens; this reduction in estrogen levels slows or stops the growth of estrogen-dependent breast tumors[6][7]. The combination has demonstrated significant clinical benefit as first-line therapy for HR+/HER2- advanced breast cancer, improving progression-free survival and objective response rates compared to endocrine therapy alone[5]. Dalpiciclib was developed by Jiangsu Hengrui Pharmaceuticals.
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