Drug Selectivity

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.

In summary, this is a very good and valuable book for graduate students as well as medicinal chemists in academia and pharmaceutical companies. Readers will find many interesting chapters, some of which are more oriented to experts, while others are well suited for beginners. I recommend this book to those working in the field of medicinal chemistry, or even pharmacology, who have a particular interest in selective and selectively nonselective drugs. (Prof. Antonio Macchiarulo, ChemMedChem 19/2018)

• PART I. INTRODUCTIONPolypharmacology in Drug Discovery PART II. SELECTIVITY OF MARKTETED DRUGSKinase InhibitorsNew Indications for Marketed DrugsDiscovery Technologies of New Indications PART III. FIXED-DOSE COMBINATIONSThe Growing Market of Fixed-Dose Combinations PART IV. UNSELECTIVE DRUGS IN DRUG DISCOVERYThe Growing Importance of Individualising DrugsDrug Discovery Strategies for the Generation of Multi-Target Ligands against Neglected Tropical DiseasesDesigning-In ApproachThe Linker Approach (Drug-Conjugates)Merged Multiple LigandsPharmacophore Generation of Multiple LigandsCellular Assays PART V. THERAPEUTIC AREAS FOR DESIGNED MULTIPLE LIGANDS5HT Transporter-Based Multiple Ligands for DepressionMultiple Ligands Targeting the Angiotensin System for Hypertension PPAR-Based Multiple Ligands for Metabolic DiseaseAntibioticsMultiple Ligands in Cancer TherapyMultiple Ligands in Neurodegenerative Diseases