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fulvestrant + gedatolisib + palbociclib
- Development stage
- Unknown
- Lead developer
- Celcuity
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
A combination therapy consisting of fulvestrant (a selective estrogen receptor degrader), gedatolisib (a pan-PI3K/mTOR inhibitor), and palbociclib (a CDK4/6 inhibitor). This triplet therapy is being investigated for the treatment of hormone receptor-positive (HR+), HER2-negative advanced breast cancer, particularly in patients who have progressed on prior CDK4/6 inhibitor and aromatase inhibitor therapy. Gedatolisib targets all class I PI3K isoforms and mTOR complex 1 (mTORC1)-mTOR complex 2 (mTORC2), potentially reversing resistance to CDK4/6 inhibitors by inhibiting the PI3K/mTOR pathway.
- Brand names
- FaslodexIbrance
02
Targets
ABCB1 (P-glycoprotein)CDK4 (Cyclin-dependent kinase 4)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)ESR1 (ERα)GPER1 (G protein-coupled estrogen receptor 1)CDK6 (Cyclin-dependent kinase 6)mTOR (Mammalian target of rapamycin kinase)PIK3CD (Phosphatidylinositol 3-kinase delta)ABCG2 (Breast cancer resistance protein)ESR2 (ERβ)
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