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Drug intelligence / Profile preview
palbociclib + fulvestrant
- Development stage
- Phase 4
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
Palbociclib + fulvestrant is a combination therapy used primarily for the treatment of hormone receptor–positive (HR+), human epidermal growth factor receptor 2–negative (HER2-) advanced or metastatic breast cancer. Palbociclib is an oral small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression from G1 to S phase by preventing phosphorylation of the retinoblastoma protein. Fulvestrant is an estrogen receptor antagonist that binds, blocks, and accelerates degradation of the estrogen receptor, thereby inhibiting estrogen signaling in breast cancer cells. This combination is indicated for patients whose disease has progressed following endocrine therapy[1][5][6][8]. Palbociclib was developed by Pfizer and marketed as Ibrance; fulvestrant was developed by AstraZeneca and marketed as Faslodex.
- Brand names
- Faslodex + Ibrance
- Other names
- fulvestrant and palbociclib
02
Targets
CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)ESR1 (ERα)ESR2 (ERβ)
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