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Successful Drug Discovery, Volume 1

Janos Fischer (Editor), David P. Rotella (Editor)
ISBN: 978-3-527-67845-7
256 pages
January 2015
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Description

The first volume of the book series "Successful Drug Discovery" is focusing on new drug discoveries during the last decade, from established drugs to recently introduced drugs of all kinds: small-molecule-, peptide-, and protein-based drugs.
The role of serendipity is analyzed in some very successful drugs where the research targets of the lead molecule and the drug are different. Phenotypic and target-based drug discovery approaches are discussed from the viewpoint of pioneer drugs and analogues.
This volume gives an excellent overview of insulin analogues including a discussion of the properties of rapid-acting and long-acting formulations of this important hormone.
The major part of the book is devoted to case histories of new drug discoveries described by their key inventors. Eight case histories range across many therapeutic fields.
The goal of this book series is to help the participants of the drug research community with a reference book series and to support teaching in medicinal chemistry with case histories and review articles of new drugs.
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Table of Contents

GENERAL ASPECTS
Serendipitious Target-based Drug Discoveries
Drug Discoveries and Molecular Mechanism of Action
DRUG CLASSES
Insulin Analogues Improving the Therapy of Diabetes
CASE HISTORIES
The Discovery of StendraTM (Avanafil) for the Treatment of Erectile Dysfunction
Dapagliflozin, a Selective SGLT2 Inhibitor for Treatment of Diabetes
Elvitegravir, a New HIV-1 Integrase Inhibitor for Antiretrovial Therapy
Discovery of Linagliptin for the Treatment of Type 2 Diabetes Mellitus
The Discovery of Alimta (Pemetrexed)
Perampanel: a Novel, Non-competitive AMPA Receptor Antagonist for the Treatment of Epilepsy
Discovery and Development of Telaprevir (IncivekTM) - a Protease Inhibitor to Treat Hepatitis C Infection
Antibody-Drug Conjugates: Design and Development of Trastuzumab Emtansine (T-DM1)
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Author Information

JŠnos Fischer is a Senior Research Scientist at Richter Plc., Budapest, Hungary. He received his MSc and PhD degrees in organic chemistry from the Eotvos University of Budapest under Professor A. Kucsman. Between 1976 and 1978, he was a Humboldt Fellow at the University of Bonn under Professor W. Steglich. He has worked at Richter Plc. since 1981 where he participated in the research and development of leading cardiovascular drugs in Hungary. He is the author of some 100 patents and scientific publications. In 2004, he was elected as a Titular member of the Chemistry and Human Health Division of IUPAC. He received an honorary professorship at the Technical University of Budapest.

David Rotella is the Margaret and Herman Sokol Professor of Medicinal Chemistry at Montclair State University. He earned a B.S. Pharm. degree at the University of Pittsburgh (1981) and a Ph.D. (1985) at The Ohio State University with Donald. T. Witiak. After postdoctoral studies in organic chemistry at Penn State University with Ken S. Feldman, he became an assistant professor at the University of Mississippi. Before accepting his current position he worked at Cephalon, Bristol-Myers, Lexicon and Wyeth where he was involved in neurodegeneration, schizophrenia, cardiovascular and metabolic disease drug discovery projects.
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Reviews

“In summary, this book provides a diverse set of insights into successful drug discovery cases and concepts. It is highly valuable both to support teaching and as a motivating read for medicinal chemists in academia and industry.”  (ChemMedChem, 1 October 2015)

Because of the manner in which this book combines
basic broad concepts (Section I), a detailed
overview of an class of molecules (Section II), and narrowly
focused case studies (Section III), it would be
a valuable addition to the library of any group doing
drug discovery and development.

"Because of the manner in which this book combines basic broad concepts (Section I), a detailedoverview of an class of molecules (Section II), and narrowly focused case studies (Section III), it would be a valuable addition to the library of any group doing drug discovery and development." (Chemistry International 2016)

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