Challenges & Opportunities in Drug Development from a Drug Safety and Metabolism Perspective
Dr. Jack H. Dean
Department of Pharmacology and Toxicology
University of Arizona
Dr. Thomas Baillie
School of Pharmacy
University of Washington
The first seminar will review three areas concerning the Biopharmaceutical Industry:
- factors forcing transformation of the industry;
- difficulties and strategies for filling the product gap; and
- use of toxicogenomics as a selection tool for NCEs.
Transformation of large pharma is being driven by increasing R&D costs with declining productivity, wholesale patent expiration of blockbuster drugs, and increasing regulatory demands. These factors will create a dramatic transformation of large and small pharma which will be discussed. Filling the gap with NCEs is the biggest challenge for our industry and will require a renewed effort to find rapid methods to explore both the chemical and biological space to define new targets and select lead NCEs. The use of nano-scale solid phase combinatorial chemistry techniques as a tool to fill the gap will be discussed. The challenge is to rapidly explore the safety of these candidates using in vitro toxicological tools such as toxicogenomics.
The metabolic transformation of a chemically stable molecule to a reactive, electrophilic intermediate generally is considered to be an undesirable feature of a drug candidate, and the phenomenon of “metabolic activation” has attracted widespread attention in drug discovery and development programs. The second half of the seminar series will focus on one aspect of metabolic activation, namely time-dependent inhibition of cytochrome P450 enzymes. Mechanistic studies on time-dependent inhibition can prove valuable in redirecting lead optimization efforts towards analogs that lack such a liability, and this approach will be exemplified in the case of the selective estrogen receptor modulator, raloxifene (Evista).
Space is Limited — Register Early to Guarantee Your Attendance!
|Eric Johnson, Ph.D.
|| Characterization of Substrate/Inhibitor Binding to Drug-Metabolizing Cytochrome P450 Monooxygenases using X-ray Crystallography
||September 30, 2008
|Dr. Kenneth E. Thummel, Ph.D.
|| Regulation Of Intestinal CYP3A By VDR: Implications And Safety Of Oral Therapeutics
||May 7, 2008
|Dr. Anthony Lu, Ph.D.
|| Why Is The Liver Microsomal Cytochrome P450 Such A Versatile And Unique Enzyme?
||September 12, 2007
|Dr. Scott Obach, Ph.D.
|| Leveraging ADME Data In Metabolites In Safety Testing (MIST)
||April 18, 2007
|Dr. Sidney Nelson, Ph.D.
|| Drug Metabolism and Chemical Structural Alerts
||September 27, 2006
|Richard B. Kim, MD
|| Relevance and Utility of Transporters to Drug Discovery and Development
||September 21, 2005
|Dr. Frederick P. Guengerich, Ph.D.
|| Human Cytochrome P450 2A6 as a Case History: Flavors, Smoke, Blue Roses, New Drugs & Basics of a P450
||April 27, 2005
|Dr. Leslie Benet, Ph.D.
||Predicting Drug Disposition via Application of BCS: Transport/Absorption/Elimination Interplay and BDDCS
||September 29, 2004
|Dr. Christopher A. Lipinski, Ph.D.
||ADME/Tox: How Low Can You Go And How Do You Recover?
||April 21, 2004
Our May 2009 meeting is generously sponsored by:
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