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binimetinib + buparlisib
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Binimetinib + buparlisib is an investigational combination therapy consisting of two small molecule inhibitors targeting key signaling pathways in cancer. Binimetinib is a MEK inhibitor, which blocks the mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase (ERK) pathway, while buparlisib is a phosphatidylinositol 3-kinase (PI3K) inhibitor that targets the PI3K/AKT/mTOR pathway. This dual inhibition strategy aims to overcome resistance mechanisms and enhance antitumor activity in patients with advanced solid tumors harboring RAS or RAF mutations. The combination has been studied primarily in phase Ib clinical trials for patients with advanced solid tumors, including ovarian cancer and non-small cell lung cancer with specific genetic alterations[1][2][3].
- Brand names
- MektoviBuparlisib
- Other names
- BKM120 + MEK162
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CA (Phosphoinositide 3-kinase alpha)mTOR (Mammalian target of rapamycin kinase)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3C3 (PI3K class III)
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