-5%
Palbociclib inhibits Cyclin-dependent kinases (CDK) 4 and 6, which are key regulators of cellular proliferation. It works by:
- Blocking the transition from the G1 phase to the S phase in the cell cycle reduces the proliferation of estrogen receptor (ER)-positive breast cancer cells.
- Decreasing retinoblastoma (RB) protein phosphorylation, leads to reduced E2F signaling and enhanced cell growth arrest when combined with antiestrogens.
- Inducing sustained cell senescence when used alongside antiestrogens, greater effects were observed when antiestrogen treatment continued after Palbokin discontinuation.
- Demonstrating stronger tumor growth inhibition in combination with letrozole compared to either drug alone in patient-derived ER-positive breast cancer models.
Palbokin is a kinase inhibitor used to treat hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. It is prescribed in combination with:
- An aromatase inhibitor was the first endocrine-based therapy for postmenopausal women.
- Fulvestrant for women whose disease has progressed after prior endocrine therapy.