Drug Detail

Information about Midostaurin

Generic Name	Midostaurin
IND	PKC412
Brand Name (US)
Manufacturer	Novartis
Drug Type	Tyrosine Kinase Inhibitor
Delivery	Oral
Approval Status	Phase 3
Indications
Overall Strategy	KIT Protein Based + Oncogenic Signal Path Based
Strategy	Block KIT + Block related tumor signal paths
Drug Category	KIT/PDGFRA inhibitor

PKC412 is a protein kinase C (PKC) inhibitor made by Novartis. It inhibits PKC alpha, beta and gamma. PKC is not a very selective inhibitor; in addition to PKC it also inhibits KIT, including many of the mutations that cause resistance in GIST.
PKC412 also inhibits the D842V mutation in PDGFRA.
Although PKC412 inhibits many of the mutations that cause resistance, it's use in GIST has been limited by drug interactions with Gleevec.