Digital Course: Dealing with the Blood-Brain Barrier
CONFERENCE SERIES: Technology and Tools for Life Sciences
Recorded at: World Pharma Congress
June 14, 2010
About this Product: Achieving blood-brain barrier (BBB) penetration remains a significant hurdle for successfully prosecuting CNS targets. Decades of research have failed to yield a single “sure-fire” approach to ensure CNS penetration. The current state of CNS drug discovery suggests that a more holistic approach is necessary, one that considers a balance of ADME and physicochemical properties. This course will examine the physiological basis for the barrier and some of the in vitro and in vivo experiments available.
Agenda At A Glance:
You will obtain a perspective on the variety of factors necessary to make informed decisions regarding blood-brain barrier.
The physiological basis for the “barrier” nature of the BBB
Experimental approaches (in vitro/in vivo) that are available for screening for brain penetration
Medicinal chemistry perspective on in vitro/in silico approaches for optimizing CNS penetration
Multi-parameter optimization (MPO) for CNS penetration
In vivo examples where all these concepts are applied together, e.g., consideration of free fractions in various compartments in relation to in vitro pharmacology values
Projecting human receptor occupancies considering species differences in affinity, free fraction
Exposure targeting for biomarker studies
Douglas Spracklin, Ph.D., Director, Pharmacokinetics, Dynamics and Metabolism, Pfizer, Inc.
Douglas Spracklin graduated from the University of Toronto with a B.Sc. in Chemistry. He obtained a Ph.D. in chemistry from the University of British Columbia in Vancouver, where his thesis work covered a range of topics including natural product synthesis, conformational modelling to predict stereochemical outcomes, and the use of antibodies that catalyze chemical reactions. Subsequently, he “moved south of the border” to do a postdoctoral fellowship with Evan Kharasch at the University of Washington, examining the metabolism of volatile anesthetic compounds. Following that, Dr. Spracklin spent two years at Abbott Labs where the position covered the entire spectrum of drug metabolism responsibilities from Discovery through Development. Upon joining Pfizer, he worked within the CNS therapeutic area for over 8 years, having the opportunity to work on several CNS programs in both the Psychotherapeutics and Neurodegeneration areas, as well as serve as the drug metabolism representative for several development teams. Currently, Dr. Spracklin is the Director of the Biotransformation & Enzymology group within Pfizer (Groton) drug metabolism.
Christopher L. Shaffer, Ph.D., Associate Research Fellow, Pharmacokinetics, Dynamics & Metabolism, Pfizer, Inc.
Christopher Shaffer obtained his B.S. (High Honors) in chemistry from The College of William and Mary (1994). Following two years of employment as an analytical chemist for Whitehall-Robins Healthcare, Inc., he attended the University of Kansas earning a M.S. (1999) and Ph.D. (Honors, 2001) in medicinal chemistry under the mentorship of Professor Robert P. Hanzlik. Subsequently, he joined the department of Pharmacokinetics, Pharmacodynamics and Metabolism within Pfizer Global Research and Development where he is currently an Associate Research Fellow associated with the Neuroscience Research Unit. His research interests include: the discovery and development of drug candidates for CNS-related targets; translational pharmacology for neuroscience-centric behavioral, electrophysiological and PET imaging assays; mechanistic studies in drug metabolism and metabolite structure elucidation; and, the development and implementation of nascent analytical technologies. Dr. Shaffer is a member of the American Chemical Society and its Medicinal Chemistry Division, the International Society for the Study of Xenobiotics, and the Society for Neuroscience.
Travis T. Wager, Ph.D., Associate Research Fellow, Neuroscience Discovery Medicinal Chemistry, Pfizer, Inc.
Travis Wager received his B.S. Professional Chemistry degree at the University of Wisconsin, Oshkosh in 1993. At the University of Utah he took up graduate studies in Chemistry with Professor Gary E. Keck and earned his Ph.D. in 1998. During his research at the University of Utah, he received the Cheves T. Walling Award for the outstanding scientific contribution to the natural product synthesis field. After earning his Ph.D., he accepted a Postdoctoral Fellowship at University of Utah with Prof. Gary E. Keck where he investigated the Julia Coupling and its application towards the total synthesis of Rhizoxin. He began his industrial career as a Research Scientist at Pfizer Inc. and was promoted to Associate Research Fellow in 2009. During his time at Pfizer he has received numerous awards; the most notable was the W.E. Upjohn Award for innovation. His main interest is a broad picture of Neuroscience drug discovery, acquired through the management of multiple disciplined project teams. As a Neuroscience Medicinal Chemist he focuses on early safety de-risking strategies and alignment of attributes (potency, ADME, CNS penetration, and safety) in one molecule which he believes will deliver high quality products to the clinic and ultimately to the market.
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About the Conference:
CHI’s World Pharmaceutical Congress encompasses a broad spectrum of topics that are very important to scientists in the pharmaceutical and biotechnology industry. This event focuses mainly on the pre-clinical aspects of drug discovery and development and consists of three separate Summits (Drug Safety Summit; Drug Discovery Innovation Summit; Screening and Imaging Summit) each featuring various tracks. The topics offer a broad-based perspective on what's going on in the field, tackling issues relevant to chemists, biologists, pharmacologists, toxicologists and clinicians alike. Each track features presentations, interactive panels and technology talks that cover the very latest on the topic, both on the scientific and the technical side. The World Pharmaceutical Congress also offers attendees and exhibitors ample opportunity to network, brain-storm and collaborate on various fronts.