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Time to lose our inhibitions? Future directions in CYP inhibition 

This webinar will give an overview of future directions of CYP inhibition and will cover molecular mechanisms, in vitro assessment and clinical impact.

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Agenda

• Introduction to current CYP inhibition – competitive (or reversible) inhibition & time-dependent inactivation 
  • General introduction to competitive and time-dependent enzyme inhibition including molecular mechanisms, clinical impact etc.
• How do we measure enzyme inhibition? 
  • How do we measure enzyme inhibition in vitro and in vivo in the clinic? 
  • Theoretical and practical aspects of the methods
• Future directions 
  • How can we use numerical methods to analyse atypical (non-Michaelis-Menten) kinetics and time-dependent inactivation CYP inhibition data to estimate clinical impact and improve clinical DDI predictions

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Moderated by: Simon Taylor - Vice President DMPK, Drug Discovery at Pharmaron

Speakers

Barry Jones, Ph.D. - Chief Scientist, Global DMPK at Pharmaron

Dr. Barry Jones is the chief scientist for Pharmaron global DMPK based at Hoddesdon and Rushden in the UK. Prior to this, Barry worked in the pharmaceutical industry firstly at Pfizer Global Research & Development in Sandwich from 1990 to 2011 before joining Astrazeneca in 2011 until 2019.

Throughout his industrial career he has focused on setting strategic direction, identifying new opportunities for research/development programs and adding significant insight/expertise and value to drug discovery and development projects with a focus in the area of in vitro DMPK science and drug-drug interactions. Barry gained his Ph. D. from the University of Surrey following research into cytochrome P450-mediated N-dealkylation 1990. He is a long standing member of the Xenobiotica editorial board and has authored or co-authored more than 80 publications.

Jing Lai, Ph.D. - Associate Director, in vitro ADME at Pharmaron

Jing achieved her Doctorate degree from the China Agricultural University, major in veterinary pharmacology and toxicology in 2013. She has worked in the in vitro ADME department at Pharmaron for the last 9 years. At Pharmaron she previously managed in vitro ADME screening projects for ~ 200 clients, participated in integrated service for 5 different target projects, provided scientific ADME input and assay service to clients. This has given Jing experience in screening stage in vitro ADME assays including CYP induction, CYP inhibition, nuclear receptor activation, non-CYP enzyme phenotyping, transporter and permeability assays. Currently Jing is leading the Pharmaron in vitro ADMET innovation team. Her team is responsible for assay harmonization and optimization, and setting-up of new assay platforms.

Ken Korzekwa, Ph.D. -  Professor, Department of Pharmaceutical Sciences at Temple University School of Pharmacy

Dr. Ken Korzekwa is a Professor in the Department of Pharmaceutical Sciences at Temple University School of Pharmacy. Ken received his B.S. in Chemical Engineering from New Mexico State University and his PhD in Medicinal Chemistry from the University of Washington. He received a PRAT Fellowship from the NIH and worked as a Staff Fellow and Senior Staff Fellow in the areas of drug metabolism and enzymology. He joined the University of Pittsburgh as an Associate Professor in the Department of Clinical Pharmacology and continued his research in drug metabolism and pharmacokinetics. Some of the predictive technologies developed by Ken and his colleague Jeff Jones were licensed to Camitro Corporation, a startup company based in California. Ken joined Camitro Corporation as Vice President of Research in 1998. Ken moved to the Philadelphia area in 2004 and worked as a Director and Distinguished Senior Investigator in Drug Metabolism at Merck. After some time at another start-up company, Ken joined Temple University School of Pharmacy in July 2010, and teaches Pharm D and graduate pharmacokinetics. Ken’s laboratory is currently working in the areas of in vitro and in vivo drug metabolism, models for drug absorption, drug transport, time dependent inhibition, and human pharmacokinetics prediction.