Discovering and Developing Molecules with Optimal Drug-Like Properties, 2015 AAPS Advances in the Pharmaceutical Sciences Series, Vol. 15

This authoritative volume provides a contemporary view on the latest research in molecules with optimal drug-like properties. It is a valuable source to access current best practices as well as new research techniques and strategies. Written by leading scientists in their fields, the text consists of fourteen chapters with an underlying theme of early collaborative opportunities between pharmaceutical and discovery sciences. The book explores the practical realities of performing physical pharmaceutical and biopharmaceutical research in the context of drug discovery with short timelines and low compound availability. Chapters cover strategies and tactics to enable discovery as well as predictive approaches to establish, understand and communicate risks in early development. It also examines the detection, characterization, and assessment of risks on the solid state properties of advanced discovery and early development candidates, highlighting the link between solid state propertiesand critical development parameters such as solubility and stability. Final chapters center on techniques to improve molecular solubilization and prevent precipitation, with particularly emphasis on linking physiochemical properties of molecules to formulation selection in preclinical and clinical settings.

1 Developability Assessment and Risk Management During Drug Discovery.- 2 Discovery Formulations – Approaches and Practices in Early Preclinical Development.- 3 Enabling Discovery Through Leveraging and Miniaturizing Pharmaceutical Principles and Processes.- 4 Diagnosing Biopharmaceutical Limitations.- 5 The Importance of Molecular Design Principles in Delivering High Quality Pharmaceutical Candidates.- 6 Predictive Approaches to Establishing, Understanding, and Communicating Risk with Emphasis on Early Development.- 7 Strategies and Methods for Drug Candidate Phase Optimization in Discovery Space.- 8 Efficient Laboratory Methods to Assess Risk and Design Formulations.- 9 Advanced X-ray Analytical Methods to Understand Structure, Properties and Risk.- 10 Performance and Characterization of Amorphous Solid Dispersions: An Overview.- 11 Hot-Melt Extrusion: The Process-Product-Performance Interplay.- 12 Practical Considerations for Spray Dried Formulation and Process Development.- 13 Nanosizing: “End-to-End” Formulation Strategy for Poorly-Water- Soluble Molecules.- 14 Leveraging Solid State Form and Physiochemical Properties for Early Clinical Formulation Efforts: Opportunities and Challenges during Telcagepant Liquid Capsule Development.

Dr. Allen C. Templeton is executive director of the Analytical Sciences organization within Merck Research Laboratories. He is responsible for the managing staff in the pursuit of scientific problem-solving for pharmaceutical product development. Before assuming his current position, Dr. Templeton held positions of increasing responsibility within Merck, including leadership roles in preformulation and formulation. Dr. Templeton earned his Ph.D. in analytical chemistry from the University of North Carolina at Chapel Hill. His research experience has been in the area of analytical and materials chemistry. He has published more than fifty articles, served as co-inventor on eleven patents and authored more than 120 presentations in the area of pharmaceutical analysis. He has organized a number of symposia and training courses on diverse topics within the field of pharmaceutical characterization. Dr. Templeton is an active member in a number of professional organizations, including the American Association of Pharmaceutical Scientists (AAPS) and the American Chemical Society (ACS). He has served in a number of roles for AAPS and is most recently the secretary/treasurer of the Physical Pharmacy and Biopharmaceutics section. He was elected to the United States Pharmacopeia (USP) expert committee on physical analysis and has worked to revise a number of USP standard chapters.  He is also currently serving on the Analytical Leadership Group for the International Consortium for Innovation & Quality in Pharmaceutical Development (IQ).  He is on the editorial advisory boards for the Journal of Pharmaceutical Sciences, American Pharmaceutical Review and Current Drug Delivery.  

Dr. Stephen R. Byrnis Charles B. Jordan Professor of Medicinal Chemistry in the Department of Industrial and Physical Pharmacy, Purdue University.  Dr. Byrn set in motion the development of the field ofsolid