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alpelisib + fulvestrant
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
Alpelisib + fulvestrant is a combination therapy used primarily for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative (HR+, HER2-) advanced or metastatic breast cancer with PIK3CA mutations. Alpelisib is an oral small molecule inhibitor that targets the phosphatidylinositol 3 kinase (PI3K) pathway, specifically inhibiting the PI3K alpha isoform, which plays a key role in cell proliferation and survival. Fulvestrant is an estrogen receptor antagonist administered by intramuscular injection; it binds to estrogen receptors on tumor cells and accelerates their degradation, thereby blocking estrogen-driven tumor growth. This combination has demonstrated significant clinical benefit in progression-free survival for patients whose disease has progressed after prior endocrine therapy[1][3][4].
- Brand names
- Piqray + Faslodex
- Other names
- alpelisib and fulvestrantalpelisib plus fulvestrant
02
Targets
PIK3CA (Phosphoinositide 3-kinase alpha)ESR1 (ERα)
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