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Early ADME and DMPK Predictions for Better Lead Optimization - Header

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12:30 pm Registration

Predictive Adme and Dmpk Assessments

1:55 Chairperson’s Opening Remarks

Alan G.E. Wilson, Ph.D., Vice President, Drug Metabolism, Pharmacokinetics, Toxicology and Pathology, Lexicon Pharmaceuticals     

2:00 Transforming Drug Discovery and Development: The Strategic Role of ADME, PK and Toxicology 

Alan G.E. Wilson, Ph.D., Vice President, Drug Metabolism, Pharmacokinetics, Toxicology and Pathology, Lexicon Pharmaceuticals

Over the past decade, or so, we have seen the implementation of early screening for ADME and PK become a standard approach in the drug discovery armamentarium. In addition, there is growing interest in the earlier application of predictive PK and PK/PD modeling. More recently, we have seen and increasing focus on improving the screening approaches for toxicity. This presentation will discuss our strategy for the early application of ADME/PK and toxicology screening and the application of this data to the rapid transition from Discovery into Development.

2:30 Pharmacokinetic Drivers of Toxicity for Small Molecules

Dolores Diaz, Ph.D., DABT, Investigative Toxicology, Genentech, Inc.

Plasma drug exposures are routinely used in the interpretation of animal toxicity data, but target tissue exposures can be much higher than plasma exposures, which could have implications in the understanding of in vivo toxicities and in the determination of in vivo-in vitro correlations. Examples will be presented in which in vitro-in vivo correlations and differences in species sensitivity can be better understood by considering target organ exposures. Systematic analysis of tissue drug levels for a group of structurally diverse small molecules and consideration of their pharmacokinetic parameters indicates that tissue distribution can be roughly predicted from the volume of distribution (Vss) and the clearance (CLp) of a particular molecule. These findings suggest that consideration of these pharmacokinetic parameters could help provide relevant and translatable information.      

3:00 Sponsored Presentation (Opportunity Available)

3:30 Networking Refreshment Break in the Exhibit Hall

4:30 Strategies for Transporter Studies in Discovery and Development     

Praveen Balimane, Ph.D., Senior Research Investigator, Metabolism and Pharmacokinetics Group, Bristol-Myers Squibb Co.  

In addition to CYP’s, membrane transporters have been demonstrated to be major determinants of pharmacokinetics, efficacy and safety profiles of drugs. Appropriate use of in vitro/in vivo transporter tools for assessing the risk of transporter-mediated clinical effects has the potential to significantly reduce the attrition rates and help progress the right compounds through development. The talk will highlight current industry strategies for transporter studies- which transporters, which models, timing of the studies, result/interpretations, translation of data etc. A few case studies underscoring the impact of these transporter strategies will also be discussed.    

5:00 Predicting in vivo Drug Interactions from in vitro Data     

Brooke VandenBrink, Ph.D., Scientist, Pharmacokinetics and Drug Metabolism, Amgen, Inc. 

Early assessment of the potential for metabolism-based drug-drug interactions (DDI) is critical for designing safer therapeutics and reducing clinical attrition rates. This presentation will focus on identifying the key features that influence experimental design for in vitro DDI experiments, comparing DDI assay design in the discovery and development environments, interpreting DDI results according to regulatory guidance, and predicting the magnitude of in vivo DDIs based upon in vitro data.

5:30 End of Day


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