<p><b>Contents to Volume 1</b></p> <p>Preface xv</p> <p>A Personal Foreword xix</p> <p>1 Early Drug Development: Progressing a Candidate Compound to the Clinics 1<br /><i>Fabrizio Giordanetto</i></p> <p>References 7</p> <p><b>Part I Drug Substance 9</b></p> <p>2 Early Phase API Process Development Overview 11<br /><i>J. Christopher McWilliams and Mark Guinn</i></p> <p>3 The Discovery/Development Transition 31<br /><i>Christopher M. Cimarusti and David R. Kronenthal</i></p> <p>4 Active Pharmaceutical Ingredient Cost of Goods: Discovery to Early Development 49<br /><i>Neal G. Anderson and Todd D. Nelson</i></p> <p>5 New Technologies in Process Development 73<br /><i>Peter W. Sutton, Joseph P. Adams, Charles Wade, and Katherine Wheelhouse</i></p> <p>6 Vortioxetine and Early Drug Development Considerations at the Interface of R&D 125<br /><i>Morten Jørgensen, Kim Christensen, Martin Juhl, and Benny Bang-Andersen</i></p> <p>7 Development of a Practical Synthesis of 4′-Azido-2′;;-Methyl-2′-Desoxycytosine and Its Prodrugs as HCV Chemotherapeutic Agents 145<br /><i>Sébastien Lemaire, Tom Govaerts, and Vittorio Farina</i></p> <p><b>Part II Drug Product 169</b></p> <p>8 Solubility, Permeability, and Their Interplay 171<br /><i>Avital Beig, Milica Markovic, and Arik Dahan</i></p> <p>9 Solid-State Properties 203<br /><i>Si-Wei Zhang, Robert F. Dunn, and Alfred Y. Lee</i></p> <p>10 Salt and Cocrystal Screening 229<br /><i>Ann Newman, Cen Chen, and Carlos Sanrame</i></p> <p>11 Particle Size Reduction: From Microsizing to Nanosizing 271<br /><i>Dedong Wu and Beth A. Sarsfield</i></p> <p>12 Early Drug Development: From a Drug Candidate to the Clinic 305<br /><i>Mark McAllister, Joanne Bennett, John Davis, Brian Henry, and MeiWong</i></p> <p>13 A Practical Guide for the Preparation of Drug Nanosuspensions for Preclinical Studies: Including In Vivo Case Studies 333<br /><i>Kalle Sigfridsson, Urban Skantze, Pia Skantze, and Lennart Lindfors</i></p> <p><b>Contents to Volume 2</b></p> <p>A Personal Foreword xxiii</p> <p><b>Part III Pharmacokinetics and Pharmacodynamics 365</b></p> <p>14 Integration of Pharmacokinetic and Pharmacodynamic Reasoning and Its Importance in Drug Discovery 367<br /><i>Johan Gabrielsson and Stephan Hjorth</i></p> <p>15 Prediction of Human Pharmacokinetics and Pharmacodynamics 399<br /><i>Ulf Bredberg</i></p> <p>16 Translational Modeling and Simulation for Molecularly Targeted Small Molecule Anticancer Agents: Case Studies of Multiple Tyrosine Kinase Inhibitors, Crizotinib and Lorlatinib 433<br /><i>Shinji Yamazaki</i></p> <p>17 Informing Decisions in Discovery and Early Development Research Through Quantitative and Translational Modeling 467<br /><i>Tjerk Bueters, Christopher R. Gibson, Prajakti A. Kothare,Mallika Lala, Eric M. Parker,Matthew L. Rizk,</i> <i>Daniel Tatosian, Maria E. Trujillo, Pavan Vaddady, and Sandra A.G. Visser</i></p> <p><b>Contents to Volume 2</b></p> <p><b>Part IV Toxicology 497</b></p> <p>18 Preclinical Toxicology Evaluation 499<br /><i>Sara Moses, Ulf Andersson, and Martin Billger</i></p> <p>19 Nonclinical Safety Pharmacology 527<br /><i>Bruce H. Morimoto</i></p> <p>20 Early Drug Development 549<br /><i>Luis G. Valerio Jr.</i></p> <p>21 Addressing Genotoxicity Risk in Lead Optimization: A PDE10A Inhibitor Case Study 581<br /><i>Bie M. P. Verbist, Marjolein Crabbe, Freddy Van Goethem, and Hinrich W. H. Göhlmann</i></p> <p>22 The Integrated Optimization of Safety and DMPK Properties Enabling Preclinical Development: A Case History with S1P1 Agonists 603<br /><i>Simon Taylor</i></p> <p>23 From TRAIL to ONC201: Case Study on the Safety Benefit of Developing Targeted Agents Against Cancer-selective Pathways 631<br /><i>Christina Leah B. Kline, JessicaWagner, Amriti Lulla,Marie D. Ralff, Avital Lev, Lanlan Zhou, Varun V.</i> <i>Prabhu, Martin Stogniew, Lee Schalop,Wolfgang Oster, Joshua E. Allen, andWafik S. El-Deiry</i></p> <p><b>Part V Intellectural Property 647</b></p> <p>24 Patent Law Relevant to Early Drug Development 649<br /><i>Joanna T. Brougher Esq.,MPH and Audrey Ogurchak</i></p> <p>25 Patent Protection Strategy 667<br /><i>Mark A. Borsos</i></p> <p>26 Intellectual Property: The Patent Landscape Viewed from Generic and Originator Perspectives 691<br /><i>Jonathan D.M. Atkinson D.Phil; EPA; C Chem. FRSC</i></p> <p>27 Patent Considerations in Collaborative Drug Development 721<br /><i>Mary Anne Armstrong</i></p> <p>Index 749</p>