Drug Selectivity

An Evolving Concept in Medicinal Chemistry

Handler, Norbert / Buschmann, Helmut (Editor)

Methods and Principles in Medicinal Chemistry

1. Edition January 2018
XVI, 520 Pages, Hardcover
40 tables
Handbook/Reference Book

ISBN: 978-3-527-33538-1

Wiley-VCH, Weinheim

Wiley Online Library Content Sample Chapter Index

Short Description

Does the medicinal chemist's magic bullet have to be aimed more broadly? The necessity to reach several targets at once has led to a new paradigm in drug development that emphasizes non-selective drugs over single drug/single target systems.

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The book "Drug Selectivity - An Evolving Concept in Medicinal Chemistry" provides a current overview and comprehensive compilation for medicinal chemists that discusses the effects of aiming for multiple targets on the entire drug development process.
The result is a broad survey of current and future strategies for drug selectivity in medicinal chemistry with theoretical but also practical aspects. Different strategies are presented and evaluated, such as various design approaches, merged multiple ligands, discovery technologies and a broad range of successful examples of unselective drugs taken from all major disease areas. With its wide-ranging view of an emerging new paradigm in drug development, this handbook is of prime importance for every medicinal and pharmaceutical chemist.

PART I. INTRODUCTION
Polypharmacology in Drug Discovery

PART II. SELECTIVITY OF MARKTETED DRUGS
Kinase Inhibitors
New Indications for Marketed Drugs
Discovery Technologies of New Indications

PART III. FIXED-DOSE COMBINATIONS
The Growing Market of Fixed-Dose Combinations

PART IV. UNSELECTIVE DRUGS IN DRUG DISCOVERY
The Growing Importance of Individualising Drugs
Drug Discovery Strategies for the Generation of Multi-Target Ligands against Neglected Tropical Diseases
Designing-In Approach
The Linker Approach (Drug-Conjugates)
Merged Multiple Ligands
Pharmacophore Generation of Multiple Ligands
Cellular Assays

PART V. THERAPEUTIC AREAS FOR DESIGNED MULTIPLE LIGANDS
5HT Transporter-Based Multiple Ligands for Depression
Multiple Ligands Targeting the Angiotensin System for Hypertension
PPAR-Based Multiple Ligands for Metabolic Disease
Antibiotics
Multiple Ligands in Cancer Therapy
Multiple Ligands in Neurodegenerative Diseases

Norbert Handler holds a PhD in Medicinal Chemistry from the University of Vienna, where he worked for several years as a postdoc scientist in the field of Medicinal Chemistry. He received an Erwin-Schrödinger-Scholarship and moved to ETH Zürich where he joined Professor Schubigers Group at the Center of Radiopharmaceutical Sciences. After his return to Vienna, he managed the technology transfer office at the University of Vienna before he joined Savira pharmaceuticals, Vienna, as Head of Drug Discovery and Development. Together with Helmut Buschmann he founded RD&C Research, Development & Consulting in Vienna, where he currently is working as Managing Partner. He contributed to more than 25 scientific papers and several patent applications.

Helmut Buschmann has a PhD in organic chemistry from Aachen University and extensive industrial experience in medicinal chemistry, drug discovery and development, scale-up, pharmaceutical development, CMC, patent filing and prosecution. Helmut has over 25 years of international experience in drug discovery research and drug development in the pharmaceutical/biotechnology sectors, both in industry and academia. During his career he worked with a broad range of different targets in different therapeutic areas from pain research to anti-infectives. He has a long publication and patent record, being an author/co-author in more than 150 scientific publications, editor of various reference books and is a named inventor/co-inventor in more than 250 patent applications.
As a result of his research activities more than 15 NCEs within different therapeutic areas have entered the clinical phase (e.g. Rosonabant, Cizorlitine, Dulopetine, Axamadol,). Some of them have reached clinical phase III or are marketed (e.g. Tapentadol: Nucynta® Palexia®). Currently, he is Head of Chemistry, Pharmaceutical Development and Patent A_ airs at AiCuris, Wuppertal and cofounder and co-owner of RD&C Research, Development & Consulting in Vienna.

N. Handler, RD&C Research, Development & Consulting, Vienna, Austria; H. Buschmann, Pharma Consulting Aachen, Germany