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palbociclib + tamoxifen
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Palbociclib + tamoxifen is a combination therapy consisting of the cyclin-dependent kinase 4/6 inhibitor, palbociclib, and the selective estrogen receptor modulator, tamoxifen. This regimen is used for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative (HR+/HER2-) advanced or metastatic breast cancer. Palbociclib inhibits CDK4/6 to block cell cycle progression from G1 to S phase, thereby suppressing tumor proliferation. Tamoxifen acts as an antagonist at estrogen receptors in breast tissue, blocking estrogen-driven tumor growth. Preclinical studies have shown synergistic anti-cancer effects with this combination, including efficacy in models of acquired resistance to endocrine therapy. Clinical trials have demonstrated that this combination improves progression-free survival compared to endocrine therapy alone and offers a new treatment option for both premenopausal and postmenopausal patients with HR+/HER2− advanced breast cancer[1][4][5][6].
- Other names
- palbociclib and tamoxifenpalbociclib plus tamoxifen
02
Targets
ESR2 (ERβ)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)ESR1 (ERα)
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