pyrotinib + dalpiciclib + letrozole

This is a **chemotherapy-sparing, fully oral combination regimen** consisting of pyrotinib, dalpiciclib, and letrozole, developed for the treatment of **HER2-positive, hormone receptor-positive (HR-positive) metastatic breast cancer**. - **Pyrotinib** is an irreversible tyrosine kinase inhibitor targeting **HER2 (ERBB2)**, as well as EGFR and HER4, blocking downstream signaling and tumor cell growth. - **Dalpiciclib** is a selective **cyclin-dependent kinase 4/6 (CDK4/6) inhibitor**, preventing cell cycle progression from G1 to S phase through inhibition of CDK4/6-mediated phosphorylation of the retinoblastoma protein. - **Letrozole** is a non-steroidal aromatase inhibitor that suppresses estrogen synthesis, providing endocrine therapy in HR-positive malignancies. This triplet is being investigated as a **fully oral chemo-free first-line or second-line treatment** for postmenopausal women with HER2-positive, HR-positive metastatic breast cancer. The regimen demonstrates promising efficacy and manageable toxicity, with most common grade 3-4 adverse events being neutropenia, leukopenia, mucositis, and diarrhea. The combination is currently in Phase II trials[1][3][5].

Brand names

AiRuiNiAiRuiKangFemara

Other names

dalpiciclib + letrozole + pyrotinib