Successful Drug Discovery

With its focus on drugs so recently introduced that they have yet to be found in any other textbooks or general references, the information and insight found here makes this a genuinely unique handbook and reference.

Following the successful approach of the previous volumes in the series, inventors and primary developers of successful drugs from both industry and academia tell the story of the drug’s discovery and describe the sometimes twisted route from the first drug candidate molecule to the final marketed drug. The 11 case studies selected describe recent drugs ranging across many therapeutic fields and provide a representative cross-section of present-day drug developments. Backed by plenty of data and chemical information, the insight and experience of today’s top drug creators makes this one of the most useful training manuals that a junior medicinal chemist may hope to find.

The International Union of Pure and Applied Chemistry has endorsed and sponsored this project because of its high educational merit.

PART I: GENERAL ASPECTS
New Trends in Drug Discovery
Patenting Small and Large Pharmaceutical Molecules
 
PART II: DRUG CLASSES
Kinase Inhibitor Drugs
Evolution of Nonsteroidal Androgen Receptor Antagonists
 
PART III: CASE HISTORIES
Development of T-Cell-Engaging Bispecific Antibody Blinatumomab (Blincyto) for Treatment of B-Cell Malignancies
Ceritinib: A Potent ALK Inhibitor for the Treatment of Crizotinib-Resistant Non-Small Cell Lung Cancer Tumors
Discovery, Development, and Mechanisms of Action of the Human CD38 Antibody Daratumumab
The Discovery of Obeticholic Acid (Ocaliva), First in Class FXR Agonist
Discovery and Development of Obinutuzumab (Gazyva, Gazyvaro), a Glycoengineered Type II Anti-CD20 Antibody for the Treatment of Non-Hodgkin Lymphoma and Chronic Lymphotic Leukemia
Omarigliptin (Marizev, MK-3102)
Opicapone, a Novel Catechol-O-Methyltransferase Inhibitor (COMT) to Manage the Symptoms of Parkinson's Disease
The Discovery of Osimertinib (Tagrisso): An Irreversible Inhibitor of Activating and 1790M Resistant Forms of the Epidermal Growth Factor Receptor Tyrosine Kinase for the Treatment of Non-Small Cell Lung Cancer
Discovery of Pitolisant, the First Marketed Histamine H3-Receptor Inverse Agonist/Antagonist for Treating Narcolepsy
Discovery and Development of Safinamide, a New Drug for the Treatment of Parkinson's Disease
Discovery and Development of Trifluridine/Tipiracil (Lonsurf)

• Edited by János Fischer
• Edited by Christian Klein
• Edited by Wayne E. Childers