BEZ235 is an orally administered inhibitor of the PI3K pathway, for which no drugs currently exist. BEZ235 is under development by Novartis. The PI3K pathway has been identified as relevant to GISTs in numerous studies, contributing to tumor cell proliferation (tumor growth).
In 2007 BEZ235 entered a Phase I/II clinical trial at the Nevada Cancer Institute for patients with advanced solid malignancies. The principal investigator is Sunil Sharma, MD.
BEZ235 is also in trial at Sarah Cannon Research Institute in Nashville, Tennessee, as described at this link.
At the June 2008 ASCO meeting the following paper was presented about BEZ235 activity in pre-clinical models (link to abstract).
Pharmacodynamic (PD) endpoints and cellular proliferation effects of NVP-BEZ235, a dual PI3K/mTOR inhibitor, in breast cancer cells and xenografts with wild-type (WT) and activating PI3K mutations. (2008 ASCO Annual Meeting Abstract 14508)