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BKM120 + vemurafenib
- Development stage
- Phase 2
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
BKM120 (also known as buparlisib) is an oral pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor. Vemurafenib is a small molecule inhibitor of mutated BRAF-serine-threonine kinase, particularly effective against the BRAF V600E mutation. The combination of BKM120 and vemurafenib has been investigated in clinical trials for patients with metastatic melanoma harboring the BRAFV600 mutation. This dual pathway inhibition strategy targets both the MAPK pathway (via BRAF inhibition by vemurafenib) and the PI3K/AKT/mTOR pathway (via PI3K inhibition by BKM120), aiming to overcome resistance mechanisms to single-agent therapy in advanced melanoma[1][2][3][4]. However, studies have reported that this combination can be poorly tolerated due to overlapping toxicities[3].
- Other names
- buparlisib + vemurafenib
02
Targets
BRAF V600EPI3K (Phosphoinositide-3-kinase regulatory subunit 6)
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