Early Drug DevelopmentBringing a Preclinical Candidate to the Clinic
Methods and Principles in Medicinal Chemistry 1. Aufl.
This one-stop reference systematically covers key aspects in early drug development that are directly relevant to the discovery phase and are required for first-in-human studies. Its broad scope brings together critical knowledge from many disciplines, ranging from process technology to pharmacology to intellectual property issues. After introducing the overall early development workflow, the critical steps of early drug development are described in a sequential and enabling order: the availability of the drug substance and that of the drug product, the prediction of pharmacokinetics and -dynamics, as well as that of drug safety. The final section focuses on intellectual property aspects during early clinical development. The emphasis throughout is on recent case studies to exemplify salient points, resulting in an abundance of practice-oriented information that is usually not available from other sources. Aimed at medicinal chemists in industry as well as academia, this invaluable reference enables readers to understand and navigate the challenges in developing clinical candidate molecules that can be successfully used in phase one clinical trials.
Contents to Volume 1 Preface xv A Personal Foreword xix 1 Early Drug Development: Progressing a Candidate Compound to the Clinics 1Fabrizio Giordanetto References 7 Part I Drug Substance 9 2 Early Phase API Process Development Overview 11J. Christopher McWilliams and Mark Guinn 3 The Discovery/Development Transition 31Christopher M. Cimarusti and David R. Kronenthal 4 Active Pharmaceutical Ingredient Cost of Goods: Discovery to Early Development 49Neal G. Anderson and Todd D. Nelson 5 New Technologies in Process Development 73Peter W. Sutton, Joseph P. Adams, Charles Wade, and Katherine Wheelhouse 6 Vortioxetine and Early Drug Development Considerations at the Interface of R&D 125Morten Jørgensen, Kim Christensen, Martin Juhl, and Benny Bang-Andersen 7 Development of a Practical Synthesis of 4?-Azido-2?-Methyl-2?-Desoxycytosine and Its Prodrugs as HCV Chemotherapeutic Agents 145Sébastien Lemaire, Tom Govaerts, and Vittorio Farina Part II Drug Product 169 8 Solubility, Permeability, and Their Interplay 171Avital Beig, Milica Markovic, and Arik Dahan 9 Solid-State Properties 203Si-Wei Zhang, Robert F. Dunn, and Alfred Y. Lee 10 Salt and Cocrystal Screening 229Ann Newman, Cen Chen, and Carlos Sanrame 11 Particle Size Reduction: From Microsizing to Nanosizing 271Dedong Wu and Beth A. Sarsfield 12 Early Drug Development: From a Drug Candidate to the Clinic 305Mark McAllister, Joanne Bennett, John Davis, Brian Henry, and MeiWong 13 A Practical Guide for the Preparation of Drug Nanosuspensions for Preclinical Studies: Including In Vivo Case Studies 333Kalle Sigfridsson, Urban Skantze, Pia Skantze, and Lennart Lindfors Contents to Volume 2 A Personal Foreword xxiii Part III Pharmacokinetics and Pharmacodynamics 365 14 Integration of Pharmacokinetic and Pharmacodynamic Reasoning and Its Importance in Drug Discovery 367Johan Gabrielsson and Stephan Hjorth 15 Prediction of Human Pharmacokinetics and Pharmacodynamics 399Ulf Bredberg 16 Translational Modeling and Simulation for Molecularly Targeted Small Molecule Anticancer Agents: Case Studies of Multiple Tyrosine Kinase Inhibitors, Crizotinib and Lorlatinib 433Shinji Yamazaki 17 Informing Decisions in Discovery and Early Development Research Through Quantitative and Translational Modeling 467Tjerk Bueters, Christopher R. Gibson, Prajakti A. Kothare,Mallika Lala, Eric M. Parker,Matthew L. Rizk, Daniel Tatosian, Maria E. Trujillo, Pavan Vaddady, and Sandra A.G. Visser Contents to Volume 2 Part IV Toxicology 497 18 Preclinical Toxicology Evaluation 499Sara Moses, Ulf Andersson, and Martin Billger 19 Nonclinical Safety Pharmacology 527Bruce H. Morimoto 20 Early Drug Development 549Luis G. Valerio Jr. 21 Addressing Genotoxicity Risk in Lead Optimization: A PDE10A Inhibitor Case Study 581Bie M. P. Verbist, Marjolein Crabbe, Freddy Van Goethem, and Hinrich W. H. Göhlmann 22 The Integrated Optimization of Safety and DMPK Properties Enabling Preclinical Development: A Case History with S1P1 Agonists 603Simon Taylor 23 From TRAIL to ONC201: Case Study on the Safety Benefit of Developing Targeted Agents Against Cancer-selective Pathways 631Christina Leah B. Kline, JessicaWagner, Amriti Lulla,Marie D. Ralff, Avital Lev, Lanlan Zhou, Varun V. Prabhu, Martin Stogniew, Lee Schalop,Wolfgang Oster, Joshua E. Allen, andWafik S. El-Deiry Part V Intellectural Property 647 24 Patent Law Relevant to Early Drug Development 649Joanna T. Brougher Esq.,MPH and Audrey Ogurchak 25 Patent Protection Strategy 667Mark A. Borsos 26 Intellectual Property: The Patent Landscape Viewed from Generic and Originator Perspectives 691Jonathan D.M. Atkinson D.Phil; EPA; C Chem. FRSC 27 Patent Considerations in Collaborative Drug Development 721Mary Anne Armstrong Index 749
Fabrizio Giordanetto graduated in Medicinal Chemistry (Genoa, Italy) followed by his Ph.D. (London, UK) while working for the chemistry unit of Pharmacia – Pfizer (Italy). After positions at AstraZeneca (Sweden) as Principal Scientist and Project Leader and at Taros (Germany) as Head of Medicinal Chemistry, he has recently joined DE Shaw Research LLC (New York, USA) where he leads medicinal chemistry activities and drug discovery projects. During his career, he worked on several drug discovery programs resulting in multiple clinical candidates spanning oncology, CNS, inflammation, metabolic and cardiovascular indications and >100 international patents, peer–reviewed publications and book chapters.
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