- The phosphoinositide 3-kinase (P13K) signaling pathway is deregulated in a wide variety of cancers. GDC-0941 is a potent and selective pan-inhibitor of class I P13K. It demonstrates excellent in vivo activity in tumor xenograft models and is currently in clinical drug development.
- GDC-0941 is in multiple clinical trials for various cancers (e.g. BC, mBC, NSCLC).
- Based on its physiochemical properties – high permeability and poor solubility at physiologically relevant pH values 9 4- 7.5), GDC-0941 classfies as BCS class II drug, GDC-0941 belongs to the group of compounds known for their highly variable absorption that is dictated by their solubility vs. pH profile characteristics.
- Because of the steep pH-dependent solubility profile in vitro, a Phase I, randomized, open-label study was conducted in healthy volunteers to investigate the effect of food and porton pump inhibitor (PPI) on GDC-0941.
By Grace Fraczkiewicz
ASCPT 115th Annual Meeting in Atlanta, Georgia, March 18-22, 2014,