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buparlisib + fulvestrant + ribociclib
- Development stage
- Discontinued
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
A triple combination therapy consisting of buparlisib (a pan-class I phosphoinositide 3-kinase inhibitor), fulvestrant (a selective estrogen receptor degrader), and ribociclib (a CDK4/6 inhibitor). This combination was investigated for the treatment of hormone receptor-positive (HR+), HER2-negative advanced breast cancer. The combination targets multiple pathways involved in cancer progression but was not advanced to phase II studies due to unexpected toxicity.
- Brand names
- Kisqali
- Other names
- buparlisib + ribociclib + fulvestrantribociclib + buparlisib + fulvestrant
02
Targets
ESR2 (ERβ)CDK4 (Cyclin-dependent kinase 4)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)TUBB (Tubulin (alpha and beta subunits))CDK6 (Cyclin-dependent kinase 6)PIK3CD (Phosphatidylinositol 3-kinase delta)ESR1 (ERα)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)
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