SUCCESSFUL DRUG DISCOVERY, VOLUME 4

• Part I General Aspects 1
1 Trends in Peptide Therapeutics 3
2 Physicochemical Parameters of Recently Approved Oral Drugs 35
• Part II Drug Class Studies 55
3 Antibody–Drug Conjugates: Empowering Antibodies for the Fight Against Cancer 57
4 Dopamine D2 Partial Agonists – Discovery, Evolution, and Therapeutic Potential 83
• Part III Case Studies 131
5 Discovery of Etelcalcetide for the Treatment of Secondary Hyperparathyroidism in Patients with Chronic Kidney Disease 133
6 Development of Lenvatinib Mesylate, an Angiogenesis Inhibitor Targeting VEGF and FGF Receptors 155
7 Ocrelizumab: A New Generation of anti CD20 mAb for Treatment of Multiple Sclerosis 169
8 The Story of Rucaparib (Rubraca) 201
9 Discovery and Development of Venetoclax, a Selective Antagonist of BCL 2 225

In this fourth volume in the series, inventors and primary developers of drugs that made it to the market continue telling the story of the drugs? discovery and development, and discuss the sometimes twisted route from the first drug candidate molecule to the final marketed one. Beginning with a general section addressing overarching topics for drug discovery, the book offers seven chapters that feature selected case studies describing recently introduced drugs or drug classes. These include small molecule drugs as well as biopharmaceuticals and range across different therapeutic fields. Together, they provide a representative cross-section of the present-day drug development effort.

Successful Drug Discovery: Volume 4 covers trends in peptide-based drug discovery and the physicochemical properties of recently approved oral drugs. The section on drug class studies looks at antibody-drug conjugates and the discovery, evolution, and therapeutic potential of dopamine partial agonists. Featured case studies examine the discovery of Etelcalcetide for the treatment of secondary hyper-parathyroidism in patients with chronic kidney disease; the development of Lenvatinib Mesylate; the discovery and development of Venetoclax; and more.

-Focuses on recently introduced drugs that have not been featured in any textbooks or general references, including Ocrelizumab, a new generation of anti-CD-20 mAb for the treatment of multiple sclerosis, and Venetoclax, a selective antagonist of BCL-2
-Features personal experiences of successful drug developers from industry and academia
-Endorsed and supported by the International Union of Pure and Applied Chemistry (IUPAC)

Successful Drug Discovery: Volume 4 provides a fascinating and informative look into the process of drug discovery and would be a great reference for those in the pharmaceutical industry, organic and pharmaceutical chemists, and lecturers in pharmacy.

AUTHORS
• János Fischer, PhD, is a Senior Research Scientist at Richter Plc., Budapest, Hungary, and is Member of the Subcommittee on Drug Discovery and Development of IUPAC.
• Christian Klein, PhD, is Department Head Cancer Immunotherapy Discovery 3 and Site Head at the Roche Innovation Center Zurich, specialized in the discovery, validation, and preclinical development of antibody based cancer immunotherapies and bispecific antibodies.
• Wayne E. Childers, PhD, is Associate Professor of Pharmaceutical Sciences at Temple University School of Pharmacy, Philadelphia, USA.