CZ415, a highly selective mTOR inhibitor showing in vivo efficacy in a collagen induced arthritis (CIA) model

6^th World Congress on Medicinal Chemistry and Drug Design

June 07-08, 2017 Milan, Italy

Giovanna Bergamini

GSK Company, Germany

Scientific Tracks Abstracts: Med Chem (Los Angeles)

Abstract :

CZ415, a potent ATP-competitive mTOR inhibitor with unprecedented selectivity over other kinases will be presented here. It�s in vivo pharmacokinetic profile will be reported, in addition to a comprehensive characterization of its in vitro activities and ADME data. The suitability of this inhibitor for studying in vivo mTOR biology is shown by the inhibition of target-dependent phosphorylation signaling observed in a mechanistic mouse model following oral administration. The compound reported here is the first ATP-competitive mTOR inhibitor described to show efficacy in a semi-therapeutic collagen induced arthritis (CIA) mouse model.

Biography :

Giovanna Bergamini has completed her PhD in Virology at the University of Bologna. She was a Post-doctoral Researcher at the European Molecular Biology Laboratory in Heidelberg, Germany. At Cellzome in Heidelberg, she leads Drug Discovery Programs in the Immuno-inflammation Therapeutic area. As a Director of Discovery Biology following acquisition of Cellzome from GSK, she oversees numerous activities on the investigation of drug mode of action across the GSK portfolio. She has published more than 20 papers in high impact journals.

Email: giovanna.2.bergamini@gsk.com