GIST Support Wiki19 Apr 2008
From: Marina Symcox
Subject: Clinical trial for BGT226 a PI3K inhibitor by Novartis
Hello everyone,
PI3K (Pee Eye three KYE-nase) is a very important signaling protein in many types of cancer including GIST, and common cancers as well. PI3K is potentially a HUGE target for drug development, as is HSP90.
The importance of PI3K in driving tumor growth has been known for years, but we were lacking drugs that could block PI3K in a patient--there were drugs that could block PI3K in a test tube setting, but which were not suitable to give to a patient. Now, there seem to be several investigational drugs in clinical trial that block PI3K. George Demetri mentioned such a drug called BEZ 235 by Novartis in the show, "The truth about cancer."
BEZ-235 can be found at clinicaltrials.gov--and is available at Sarah Cannon Cancer Center in Nashville and in Nevada. BEZ235 as the PI3K inhibitor listed below (BGT226) started out in phase I trial at Nevada with Sunil Sharma as PI.
Is PI3K a good target in GIST? Probably..though KIT or PDGFRA are likely still likely the best targets for most pts because KIT and PDGFRA sit on the top zennith position of a pyramid of signaling into the cancer cell. Meanwhile, PI3K is an important hub inside the cell but is more like the second layer down from KIT signaling. PI3K tells the cancer cell to stay alive. PI3K also helps the cancer cell important glucose for fast fuel.
For me as a pt, blocking PI3K may seem something to try if KIT inhibitors are no longer working because my tumor load has too many different types of secondary mutations in them...or if I have a wild type GIST that is not responding to the KIT inhibitors. A combination of a PI3K inhibitor and GLeevec seems like an attractive idea...
For those interested in trying a PI3K inhibitor, the protocol for BGT226 is listed below...I don't know if BEZ235 or BGT226 is better...don't know...
http://clinicaltrials.gov/ct2/show/NCT00600275?term=PI3+Kinase&recr=Open&rank=1