Drug Detail

Information about Imatinib,BKM120

Generic Name
IND	Imatinib,BKM120
Brand Name (US)
Manufacturer	Novartis
Drug Type	Tyrosine Kinase Inhibitor
Delivery	Oral
Approval Status	Gleevec is approved for GIST. This combination is in a phase 1/2 trial for GIST.
Indications
Overall Strategy	KIT Protein Based + Oncogenic Signal Path Based
Strategy	Block KIT + Block related tumor signal paths
Drug Category	KIT/PDGFRA + PI3K Inhibitor

BKM120 is a pan-PI3K inhibitor. PI3K has been shown to be an important signaling protein that is downstream from KIT. Lab experiments suggest that inhibiting KIT and PI3K at the same time may be effective and that combination shows synergistic and long-lasting effects even after treatment withdrawal, which is not the case with drugs routinely used for GIST treatment.
The links below demonstrate significant activity of the combination of PI3K inhibitors (two different inhibitors) and imatinib. Note that neither of these inhibitors was BKM120.