Palbociclib is an oral CDK4/6 inhibitor primarily used to treat hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. It inhibits cyclin-dependent kinases 4/6 (CDK4/6), blocking cancer cell proliferation. It is often used in combination with endocrine-based therapies (such as letrozole and fulvestrant) to prolong progression-free survival.
I. Mechanism of Action and Indications
Palbociclib selectively inhibits CDK4/6 protein kinases, preventing cancer cells from transitioning from the G1 phase to the S phase, thereby inhibiting tumor growth. Its indications are as follows:
HR+/HER2- breast cancer: Patients must be confirmed to be hormone receptor-positive and HER2-negative by testing. 1.
Advanced or metastatic stage: Indicated for patients with inoperable or metastatic breast cancer. 2.
Combination therapy: Typically used in combination with endocrine-based therapies (such as aromatase inhibitors) as first- or second-line treatment.
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