Drug Detail

Information about Velcade

Generic Name	Bortezomib
IND	PS-341
Brand Name (US)	Velcade
Manufacturer	Millennium
Drug Type	Proteasome inhibitor
Delivery	Intravenous
Approval Status	Approved for a non-GIST cancer
Indications	Multiple Myeloma, Mantle Cell Lymphoma
Overall Strategy	GIST cell based
Strategy	Destroy KIT + Unblock cell death genes
Drug Category	Proteasome inhibitor

Velcade is an inhibitor of the 26S proteasome in cells. The 26S proteasome is a large protein complex that degrades ubiquitinated proteins. The ubiquitin-proteasome pathway plays an essential role in regulating the intracellular concentration of specific proteins, thereby maintaining homeostasis within cells. Inhibition of the 26S proteasome prevents this targeted proteolysis, which can affect multiple signaling cascades within the cell. This disruption of normal homeostatic mechanisms can lead to cell death.
There is preclinical evidence that Velcade can promote cell death in GIST cells in the test tube. There are no trials of Velcade in GIST and as yet there are no reports of GIST patients trying Velcade.