Volume 4
Edited by
Editors
János Fischer
Richter Co., Plc.
Gyömröi ut 19/21
1103 Budapest
Hungary
Christian Klein
Roche Innovation Center Zürich
Cancer Immunotherapy Division
Wagistrasse 10
8952 Schlieren
Switzerland
Wayne E. Childers
Temple University School of Pharmacy
Moulder Ctr. for Drug Discovery Res.
3307 N Broad Street
Philadelphia, PA 19140
United States
Cover
Supported by the international Union of Pure and Applied Chemistry (IUPAC)
Chemistry and Human Health Division
PO Box 13757
Research Triangle Park, NC 2770‐3757
USA
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Print ISBN: 978‐3‐527‐34468‐0
ePDF ISBN: 978‐3‐527‐81470‐1
ePub ISBN: 978‐3‐527‐81471‐8
oBook ISBN: 978‐3‐527‐81469‐5
Magid Abou‐Gharbia
(Temple University, USA)
Jagath R. Junutula
(Cellerant Therapeutics, Inc., USA)
Kazumi Kondo
(Otsuka, Japan)
John A. Lowe
(JL3Pharma LLC, USA)
Gerd Schnorrenberg
(Boehringer Ingelheim, Germany)
The fourth volume of Successful Drug Discovery continues to follow the structure of the previous volumes, consisting of three parts: General Aspects, Drug Class Studies, and Case Studies. The book series focuses on new discoveries of small‐molecule drugs and biologics.
The editors thank the advisory board members: Magid Abou‐Gharbia (Temple University, USA), Jagath R. Junutula (Cellerant Therapeutics, Inc., USA), Kazumi Kondo (Otsuka), John A. Lowe (JL3Pharma LLC, USA), and Gerd Schnorrenberg (Boehringer Ingelheim, Germany), and the following reviewers who helped both the authors and the editors: Jonathan Baell, Gabriele Costantino, György Domány, John M. Beals, Stephen Hauser, Jagath R. Junutula, Béla Kiss, Paul Leeson, Gábor Mező, Tomi Sawyer, Malcolm Stevens, Michael Wagner, Peng Wu. Special thanks are due to Juergen Stohner for his review from the viewpoints of the IUPAC Interdivisional Committee on Terminology, Nomenclature and Symbols (ICTNS).
John P. Mayer and coworkers give a comprehensive survey on the recent progress in peptide therapeutics. Remarkable achievements in various therapeutic fields and several orally administered peptides are summarized in this chapter.
Andreas Ritzén and coworker investigate the physicochemical parameters of recently approved drugs. A significant fraction of non‐CNS oral drugs violate two or more of the Lipinski parameters.
Nicolas Joubert and coworkers give an overview on antibody–drug conjugates in cancer‐targeted chemotherapy. Over the last decade, they have been improved by the choice of better drugs, linkers, and mAb targets.
Wayne E. Childers and coworkers evaluate three decades in the discovery of D2 partial agonist drugs. Progress has been made in treating the negative and cognitive symptoms of schizophrenia.
Derek Maclean and coworker report on the discovery of etelcalcetide, which affords a suitable therapy for hemodialysis patients with secondary hyperparathyroidism.
Akihiko Tsuruoka and coworkers describe how lenvatinib mesylate was discovered to give a new drug for the treatment of differentiated thyroid cancer.
Andrew C. Chan and coworkers describe the discovery and development of ocrelizumab, which represents a new generation of anti‐CD20 mAb for the treatment of multiple sclerosis.
Bernard T. Golding has prepared a chapter on the discovery and development of rucaparib, a new PARP‐1 inhibitor anticancer drug for the treatment of ovarian cancer. It also represents an example of a good cooperation of academia and industry.
Wayne J. Fairbrother and coworkers describe how venetoclax, a selective antagonist of B cell lymphoma 2 (Bcl‐2), was discovered for the treatment of leukemia.
The editor and authors thank Wiley‐VCH, and personally Dr. Frank Weinreich for the excellent cooperation.
Budapest
Philadelphia
Zurich
8 November 2018
János Fischer
Wayne E. Childers
Christian Klein