Optimizing the “Drug-Like” Properties of Leads in Drug Discovery

1. Strategic Use of Preclinical Pharmacokinetic Studies and In Vitro Models in Optimizing ADME Properties of Lead Compounds
Dhiren R. Thakker

2. Role of Mechanistic Transport Studies in Lead Optimization
Jerome Hochman, Qin Mei, Masayo Yamazaki, Cuyue Tang, Thomayant Prueksaritanont, Mark Bock, Sookhee Ha, Jiunn Lin

3. Metabolic Activation-Role in Toxicity and Idiosyncratic Reactions
John S. Walsh

4. Case History — Use of ADME Studies for Optimization of Drug Candidates
Liang-Shang Gan, Frank W. Lee, Nelamangala Nagaraja, Ping Li, Jason Labutti, Wei Yin, Cindy Xia, Hua Yang, Vinita Uttamsingh, Chuang Lu, Sandeepraj Pusalkar, J. Scott Daniels, Ron Huang, Mark Qian, Jing-Tao Wu, Kym Cardoza, Suresh K. Balani, Gerald T. Miwa

5. Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization
Michael J. Hageman

6. Lipid-based Systems, Drug Exposure and Lead Optimization
William N. Charman, Susan A. Charman, Christopher J. H. Porter

7. Biopharmaceutics Modeling and the Role of Dose and Formulation on Oral Exposure
Brian R. Rohrs

8. Application of Physicochemical Data to Support Lead Optimization by Discovery Teams
Li Di, Edward H. Kerns

9. Computational Models Supporting Lead Optimization in Drug Discovery
Philip S. Burton, Italo Poggesi, Massimiliano Germani, Jay T. Goodwin

10. Prodrug Strategies for Improving Drug-Like Properties
Valentino J. Stella

11. The Application of Multivariate Data Analysis to Compound Property Optimization
John W. Ellingboe

12. Case History: Toxicology Biomarker Development Using Toxicogenomics
David E. Watson, Timothy P. Ryan, James L. Stevens

13. Predicting Idiosyncratic Drug Reactions
Alastair Cribb

14. Elementary Predictive Toxicology for Advanced Applications
Constantine Kreatsoulas, Stephen K. Durham, Laura L. Custer, Greg M. Pearl

15. The Application of PK/PD Modeling and Simulations During Lead Optimization
Stuart Friedrich, Evelyn Lobo, Karen Zimmerman, Anthony Borel, Carlos O. Garner

16. Early Preclinical Evaluation of Brain Exposure in Support of Hit Identification and Lead Optimization
Thomas J. Raub, Barry S. Lutzke, Paula K. Andrus, Geri A. Sawada, Brian A. Staton

17. Optimizing Biomarker Development for Clinical Studies at the Lead Optimization Stage of Drug Development
Geoffrey S Ginsburg, Julie Lekstrom-Himes, William Trepicchio

18. The Relevance of Transporters in Determining Drug Disposition
Hartmut Glaeser, Richard B. Kim

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Keywords: TECHNOLOGY & ENGINEERING / Biomedical TEC059000