CPSA Shanghai 2011
Changing Paradigm in Drug Discovery & Development:
East Meets West
April 13 - 16, 2011
Renaissance Shanghai Pudong Hotel
Shanghai, China
Abstract
Thursday PM - Parallel Session I
Blood-Brain Barrier Transporters: Friend or Enemy for CNS Drug Discovery and Development
Zack Cheng
Drug Metabolism and Pharmacokinetics, GlaxoSmithKline R&D China, Shanghai
The Blood-brain Barrier (BBB) is essential to protect the CNS from potentially harmful agents in the peripheral circulation; however it presents great challenges to CNS drug discovery and development. CNS penetration of therapeutic drugs is influenced by uptake and efflux transporters expressed on the BBB. Pgp is the mostly investigated efflux transporter and BCRP has gained increasing attention in limiting drug transport across BBB. Role of BCRP in CNS drug discovery will be discussed. Contrary to the efflux pumps, uptake transporter may provide a solution for CNS drug delivery across the BBB. We have established a robust high throughput BacMam2-OATP1A2 transduced HEK293 system to investigate the role of OATP1A2 for CNS marketed drug brain penetration. Interplay between uptake and efflux transport defines the extent of exposure of many drugs and their CNS action.
Ziqiang “Zack” Cheng is an Associate Director leading in vitro and in vivo teams in the Drug Metabolism and Pharmacokinetics (DMPK) Department at GlaxoSmithKline (GSK) R&D China in Shanghai. After earning his B.S. in China in 1994, he went to US for graduate school. He received M.S. in Molecular Biology from Purdue University in 1996 and Ph.D in Pharmacology/Drug Metabolism from University of Iowa in 2000. After graduation, he started his career as a Research Scientist I, Research Scientist II, and Team Leader at Cardinal Health (2000-2003), Research Triangle Park (RTP), NC, followed by an Investigator and Principal Scientist at DMPK department at GSK, RTP, NC (2003-2008). He returned to China in 2008 and is the founding member and has built up the DMPK department at GSK R&D China while growing his career as Principal Scientist, Manager and Associate Director. Besides leading DMPK team, he has over 8 years of experience in multidisciplinary project teams and closely worked with Biology, Medicinal Chemistry, Safety Assessment, Pharmaceutical Development, Process Chemistry and Clinical and Commercial. His research interest include drug transporters on Blood-brain Barrier, drug CNS penetration in neurological diseases, and free drug target engagement for in vivo biology study.