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ribociclib + tamoxifen
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Ribociclib + tamoxifen is a combination of two oral small molecule drugs used in the treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer, particularly in premenopausal women. Ribociclib 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. Tamoxifen is a selective estrogen receptor modulator (SERM) that acts as an antagonist on estrogen receptors in breast tissue, thereby blocking estrogen-driven tumor growth. The combination has been studied in clinical trials such as MONALEESA-7 for advanced breast cancer but is not currently indicated due to increased risk of QT interval prolongation and other safety concerns[2][3][5][6][7].
- Other names
- ribociclib + tamoxifen
02
Targets
CDK4 (Cyclin-dependent kinase 4)ESR2 (ERβ)CDK6 (Cyclin-dependent kinase 6)ESR1 (ERα)
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