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buparlisib + letrozole
- Development stage
- Unknown
- Lead developer
- Adlai Nortye
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Buparlisib is an oral, reversible inhibitor of all class I phosphoinositide-3-kinases (PI3K), and letrozole is a nonsteroidal aromatase inhibitor. The combination has been investigated for the treatment of hormone receptor-positive (HR+), HER2-negative breast cancer, particularly in patients with metastatic disease refractory to endocrine therapy. The combination aims to overcome resistance to endocrine therapy by targeting both estrogen synthesis and the PI3K pathway, which is frequently activated in HR+ breast cancer[1][2][10].
02
Targets
TUBB (Tubulin (alpha and beta subunits))PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)CYP19A1 (Aromatase)PIK3CA (Phosphoinositide 3-kinase alpha)
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