buparlisib

Ligand id: 7878

Name: buparlisib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 8
Hydrogen bond donors 1
Rotatable bonds 4
Topological polar surface area 89.63
Molecular weight 410.17
XLogP 1.4
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Buparlisib is being assessed in clinical trials, including Phase II trials for metastatic transitional cell carcinoma of the urothelium (NCT01551030) and untreated squamous non-small cell lung cancer (NCT01820325). Click here to link to ClinicalTrials.gov's complete listing of buparlisib trials.
Mechanism Of Action and Pharmacodynamic Effects
Activation/dysregulation of PI3K signaling may contribute to tumorigenesis and tumor resistance to a many of the currently used antineoplastic agents. Buparlisib selectively inhibits class I PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations.