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buparlisib + erlotinib
- Development stage
- Discontinued
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Buparlisib + erlotinib is a combination therapy investigated for the treatment of advanced non-small cell lung cancer (NSCLC). Buparlisib (BKM120) is an oral, pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor that targets all four catalytic isoforms (p110α, p110β, p110δ, and p110γ). Erlotinib is an oral small molecule tyrosine kinase inhibitor that specifically targets the epidermal growth factor receptor (EGFR). The combination was evaluated by SCRI Development Innovations, LLC (Sarah Cannon Research Institute) in Phase II clinical trials to address resistance to EGFR-targeted therapies. The therapeutic rationale is that buparlisib can down-modulate the PI3K-Akt signaling pathway, which is often upregulated as a resistance mechanism in EGFR-mutant lung cancers, thereby restoring or enhancing the anti-tumor activity of erlotinib.
- Brand names
- Tarceva
- Other names
- BKM120 + erlotinibbuparlisib + erlotinib
02
Targets
PIK3CA (Phosphoinositide 3-kinase alpha)TUBB (Tubulin (alpha and beta subunits))PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)EGFR T790M (Epidermal growth factor receptor T790M mutant)
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