Short Courses  |  Day 1 | Day 2 |  Day3 |  Download Brochure

Pre-Conference Short Courses*

Tuesday, February 2

9:00 AM – 12:00 PM

(SC6) Dealing with the 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

9:00 Douglas Spracklin, Ph.D., Director, Pharmacokinetics, Dynamics and Metabolism, Pfizer, Inc.

9:45 Christopher L. Shaffer, Ph.D., Associate Research Fellow, Pharmacokinetics, Dynamics & Metabolism, Pfizer, Inc.

10:30 Coffee Break

11:00 Travis T. Wager, Ph.D., Associate Research Fellow, Neuroscience Discovery Medicinal Chemistry, Pfizer, Inc.

11:45 Q&A

12:00 End of Course

(SC9) Fragment-Inspired Medicinal Chemistry

• Fragment-based approaches as platforms for medicinal chemistry
• Fragment-based methods that inspire fresh approaches to lead generation
• Optimization of fragment hits
• Combining technology with fragment-based methods to advance medicinal chemistry
• Facing the challenge of applying fragment-based approaches when structural information is not available
• Promises and pitfalls of surface plasmon resonance (SPR) for fragment methods

2:00 Michelle Arkin, Ph.D., Associate Director, Biology, Small Molecule Discovery Center, Pharmaceutical Chemistry, University of California, San Francisco

3:15 Refreshment Break

3:45 Daniel A. Erlanson, Ph.D., Cofounder, Carmot Therapeutics, Inc.

5:00 End of Course

(SC10) Transporter-mediated Drug-Drug Interaction Potential: Strategies for in vitro Characterization

• Clinical relevance of transporter DDI’s 
• In vitro, cell based models for evaluating transporter interactions of substrates and inhibitors 
• Case study: Minimizing p-glycoprotein interactions as a barrier to CNS penetration 

2:00 Introductory Comments

Phil Burton, Ph.D., Chief Executive Officer & Chief Scientific Officer, ADMETRx, Inc.

2:05 Joseph A. Ware, Ph.D., Senior Scientist, Clinical Pharmacokinetics and Pharmacodynamics, Development Sciences, Genentech, Inc.

3:00 Phil Burton, Ph.D., Chief Executive Officer & Chief Scientific Officer, ADMETRx, Inc.

3:50 Refreshment Break

4:15 XingRong Liu, Ph.D., Senior Scientist, DMPK, Genentech, Inc.

4:45 Q&A

5:00 End of Course

*Separate Registration Required

Short Courses  |  Day 1 | Day 2 |  Day3 |  Download Brochure