Ridaforolimus (Deforolimus AP23573) BEZ235 SF1126 XL418 XL765 XL147 Everolimus (RAD001) PX-866 XL281 Perifosine XL228 RDEA119 GDC-0941 bismesylate PF-04691502 GDC-0973 Sirolimus (Rapamune) GDC-0980 Temsirolimus (Torisel, CCI-779) Selumetinib (AZD6244)

GDC-0941 bismesylate

GDC-0941, bismesylate, is a potent, selective, orally bioavailable inhibitor of PI3K currently being developed by Genentech and being evaluated in human clinical trials for the treatment of cancer.

Definition from NCI Drug Dictionary: PI3K inhibitor GDC-0941, bismesylate, is the orally bioavailable bismesylate salt of a potent small-molecule thieno[3,2-d]pyrimidine inhibitor of the class I phosphatidylinositol 3 kinase (PI3K) isoforms p100alpha and p100delta with potential antineoplastic activity. PI3K inhibitor GDC-0941 selectively binds to PI3K isoforms in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway; inhibition of tumor cell growth, motility and survival in susceptible tumor cell populations may result. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis; dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents

Mode of action:  ATP-competitive inhibitor of PI3K

Manufacturer: Genentech  For specific information at Genentech website click here.

Current clinical trials relevant to GIST:

NCT00876109:  An Open-Label, Phase I, Dose-Escalation Study Evaluating Two Dosing Schedules of PI3-Kinase Inhibitor (GDC-0941) in Patients With Locally Advanced or Metastatic Solid Tumors for Which Standard Therapy Either Does Not Exist or Has Proven Ineffective or Intolerable.

NCT00876122: A Study of GDC-0941 in Patients With Locally Advanced or Metastatic Solid Tumors or Non-Hodgkin's Lymphoma for Which Standard Therapy Either Does Not Exist or Has Proven Ineffective or Intolerable

Related papers in PubMed:

Link here to see paper abstracts at the PubMed website.