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Dalpiciclib + pyrotinib is an investigational oral combination therapy for HER2-positive advanced or metastatic breast cancer. Dalpiciclib is a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks cell cycle progression by inhibiting phosphorylation of the retinoblastoma protein, leading to G1 phase arrest. Pyrotinib is an irreversible pan-ErbB receptor tyrosine kinase inhibitor targeting HER1 (EGFR), HER2, and HER4 receptors; it inhibits tumor cell proliferation by blocking downstream signaling pathways critical for cancer growth. The combination has demonstrated promising efficacy and manageable toxicity in clinical trials as a chemotherapy-free regimen for patients with HER2-positive advanced breast cancer—including those with hormone receptor–positive or –negative disease and brain metastases[2][3][4]. It is being studied both as a dual regimen and in triplet combinations with endocrine therapies such as letrozole[1][3][7].
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