Die Optimierung pharmakokinetischer Eigenschaften ist mittlerweile der Flaschenhals und deshalb eine der größten Herausforderungen der Wirkstofforschung. Daher war die Nachfrage nach einem Buch, das dieses Gebiet umfassend, zuverlässig, sachlich und grundsätzlich behandelt, beträchtlich. In diesem einmalig breitgefächert und zugleich tiefgründig angelegten Werk stellen international renommierte Fachleute und Praktiker aus Universitäten und Forschungseinrichtungen der Industrie die modernsten biologischen, physikochemischen und computergestützten Strategien vor, um in Versuchsreihen zu…mehr
Die Optimierung pharmakokinetischer Eigenschaften ist mittlerweile der Flaschenhals und deshalb eine der größten Herausforderungen der Wirkstofforschung. Daher war die Nachfrage nach einem Buch, das dieses Gebiet umfassend, zuverlässig, sachlich und grundsätzlich behandelt, beträchtlich. In diesem einmalig breitgefächert und zugleich tiefgründig angelegten Werk stellen international renommierte Fachleute und Praktiker aus Universitäten und Forschungseinrichtungen der Industrie die modernsten biologischen, physikochemischen und computergestützten Strategien vor, um in Versuchsreihen zu optimalen pharmakokinetischen Kenndaten zu gelangen. Gefragt wird dabei nach der Resorption im Verdauungstrakt, der Bindung an Proteine, der Fähigkeit, in Hirngewebe einzudringen, und dem metabolischen Profil. Ebenfalls sehr wichtig sind natürlich toxikologische Aspekte. Zusätzlich zu den 33 Kapiteln des Buches enthält die beiliegende CD-ROM die Haupt- und Kurzvorträge sowie Poster (Vollversionen), die im März 2000 auf dem Zweiten LogP-Symposium (Lipophilie und Wirkstoffverteilung - Praktische und computergestützte Ansätze zur Untersuchung von Moleküleigenschaften, die zur Aufnahme, Verteilung und Verstoffwechselung von Wirkstoffen in Beziehung stehen) an der Universität Lausanne präsentiert wurden.
Han van de Waterbeemd studied Chemistry at the Technival University of Eindhoven and did a Ph.D. in Medicinal Chemistry at the University of Leiden, The Netherlands. In his pharmaceutical career he worked for Roche, Pfizer and Astra-Zeneca. His research interests include the role of molecular properties in drug disposition and modeling of ADMET properties.
Gerd Folkers is professor of pharmaceutical chemistry at the ETH Zürich since 1991. He studied pharmacy at the University of Bonn and earned his Ph.D. on structure-activity relationships of desapurines. He then moved to the University of Tübingen, where he completed his habilitation in pharmaceutical chemistry. During a stay with H.-D. Hoeltje in Bern, he studied new research methods in computer-aided molecular design and expanded this knowledge during other stays with T. Blundell at the Birkbeck College and E. Meyer at Texas A&M University.The focus of his research is the molecular interaction between drugs and their binding sites. Besides his work on the molecular mechanism of "conventional" nucleoside therapeutics against virus infections and cancer, his special interest has shifted to immuno-therapeutics.
Inhaltsangabe
Preface (B. Testa) SETTING THE SCENE Pharmacokinetic Challenges in Lead Optimization (G. Gaviraghi, R.J. Barnaby and M. Pellegatti) Modelling in Preclinical and Clinical Drug Development (L.P. Balant and M. Gex-Fabry) MOLECULAR AND BIOLOGICAL BACKGROUND Structure of Liposomal Membranes in Relation to Permeation (O.G. Mouritsen, H.K. Andersen, J.S. Andersen, J. Davidsen, L.K. Nielsen and K. Jørgensen) Relations of Molecular Properties with Drug Disposition: The Cases of Gastrointestinal Absorption and Brain Penetration (H. van de Waterbeemd and D.A. Smith) Structure-Metabolism Relations, and the Challenge of redicting Biotransformation (B. Testa and G. Cruciani) Concepts in Prodrug Design to Overcome Pharmacokinetic Problems (B. Testa and J.M. Mayer) BIOLOGICAL STRATEGIES Methodologies in Cell Culture (H. Wunderli-Allenspach) Biological Models to Assess Drug Bioavailability (R.T. Borchardt) Biological Models to Study Blood-Brain Barrier Permeation (S.D. Krämer, N.J. Abbott and D.J. Begley) Biological Models to Study Skin Permeation (N. Sekkat and R.H. Guy) Biopharmaceutical Aspects of Nasal and Pulmonary Drug Delivery (P. Colombo, D. Cocconi, P. Santi, R. Bettini, G. Massimo, P.L. Catellani and C. Terzano) Significance of Plasma Protein Binding in Drug Research (S. Urien, J.-P. Tillement and J. Barré) High-Throughput ADE Screening (O. Kretz and A. Probst) In Vitro Models for Early Studies of Drug Metabolism (J.H. Lin and A.D. Rodrigues) Addressing Toxicological Issues in the Lead Optimization Phase of Drug Discovery and Evelopment (P. Bentley) PHYSICOCHEMICAL STRATEGIES Physicochemical Parameters as Tools in Drug Discovery and Lead Optimization (B. Faller and F. Wohnsland) Lipophilicity profiles: theory and measurement (J. Comer and K. Tam) High-Throughput Measurements of Solubility Profiles (A. Avdeef) Cyclic voltammetry as a new tool to study the partitioning and proton transport behaviour of ionized drugs (F. Reymond, G. Bouchard and H. Girault) Biolipid pKas and the Lipophilicity of Ampholytes and Ion Pairs (R.A. Scherrer) Recent Advances in Reversed-Phase-HPLC Techniques to Determine Lipophilicity (C. Yamagami) Liposome / Water Partitioning: Theory, Techniques and Applications (S.D. Krämer) Importance of the Mobile Phase in Immobilized Artificial Membrane Chromatography (K.L. Hauer and C. Pidgeon) High-Throughput Artificial Membrane Permeability Studies In Early Lead Discovery and Development (M. Kansy, H. Fischer, K. Kratzat, F. Senner, B. Wagner and I. Parrilla) NMR Spectroscopy for the Study of Drug-Phospholipid Interactions (R. Fruttero) COMPUTATIONAL STRATEGIES Virtual Screening of Molecular Properties: A Comparison of Log P Calculators (M.E. Duban, M.G. Bures, J. DeLazzer and Y.C. Martin) Quantitative Structure-Absorption Relationships (H.van de Waterbeemd) Hydrogen Bonding, the Last Mystery in Drug Design? (H. Kubinyi) Molecular Hydrogen-Bonding Potentials (MHBPs) in Structure-Permeation Relations (G. Caron, S. Rey, G. Ermondi, P. Crivori, P. Gaillard, P.-A. Carrupt and B. Testa) VolSurf and its Interest in Structure-Disposition Relationships (G. Cruciani, S. Clementi, P. Crivori, P.-A. Carrupt and B. Testa) Molecular Modeling Approaches to Predict Metabolism and Toxicity (A.M. ter Laak and N.P.E. Vermeulen) CONCLUSION Molecular Biology, Drug Design and Drug Delivery: Bringing It All Together (V.H.L. Lee, S.K. Wu and C. Chu) Pharmacokinetic lead optimization: fine art vs. blind technology (B. Testa)
Preface (B. Testa) SETTING THE SCENE Pharmacokinetic Challenges in Lead Optimization (G. Gaviraghi, R.J. Barnaby and M. Pellegatti) Modelling in Preclinical and Clinical Drug Development (L.P. Balant and M. Gex-Fabry) MOLECULAR AND BIOLOGICAL BACKGROUND Structure of Liposomal Membranes in Relation to Permeation (O.G. Mouritsen, H.K. Andersen, J.S. Andersen, J. Davidsen, L.K. Nielsen and K. Jørgensen) Relations of Molecular Properties with Drug Disposition: The Cases of Gastrointestinal Absorption and Brain Penetration (H. van de Waterbeemd and D.A. Smith) Structure-Metabolism Relations, and the Challenge of redicting Biotransformation (B. Testa and G. Cruciani) Concepts in Prodrug Design to Overcome Pharmacokinetic Problems (B. Testa and J.M. Mayer) BIOLOGICAL STRATEGIES Methodologies in Cell Culture (H. Wunderli-Allenspach) Biological Models to Assess Drug Bioavailability (R.T. Borchardt) Biological Models to Study Blood-Brain Barrier Permeation (S.D. Krämer, N.J. Abbott and D.J. Begley) Biological Models to Study Skin Permeation (N. Sekkat and R.H. Guy) Biopharmaceutical Aspects of Nasal and Pulmonary Drug Delivery (P. Colombo, D. Cocconi, P. Santi, R. Bettini, G. Massimo, P.L. Catellani and C. Terzano) Significance of Plasma Protein Binding in Drug Research (S. Urien, J.-P. Tillement and J. Barré) High-Throughput ADE Screening (O. Kretz and A. Probst) In Vitro Models for Early Studies of Drug Metabolism (J.H. Lin and A.D. Rodrigues) Addressing Toxicological Issues in the Lead Optimization Phase of Drug Discovery and Evelopment (P. Bentley) PHYSICOCHEMICAL STRATEGIES Physicochemical Parameters as Tools in Drug Discovery and Lead Optimization (B. Faller and F. Wohnsland) Lipophilicity profiles: theory and measurement (J. Comer and K. Tam) High-Throughput Measurements of Solubility Profiles (A. Avdeef) Cyclic voltammetry as a new tool to study the partitioning and proton transport behaviour of ionized drugs (F. Reymond, G. Bouchard and H. Girault) Biolipid pKas and the Lipophilicity of Ampholytes and Ion Pairs (R.A. Scherrer) Recent Advances in Reversed-Phase-HPLC Techniques to Determine Lipophilicity (C. Yamagami) Liposome / Water Partitioning: Theory, Techniques and Applications (S.D. Krämer) Importance of the Mobile Phase in Immobilized Artificial Membrane Chromatography (K.L. Hauer and C. Pidgeon) High-Throughput Artificial Membrane Permeability Studies In Early Lead Discovery and Development (M. Kansy, H. Fischer, K. Kratzat, F. Senner, B. Wagner and I. Parrilla) NMR Spectroscopy for the Study of Drug-Phospholipid Interactions (R. Fruttero) COMPUTATIONAL STRATEGIES Virtual Screening of Molecular Properties: A Comparison of Log P Calculators (M.E. Duban, M.G. Bures, J. DeLazzer and Y.C. Martin) Quantitative Structure-Absorption Relationships (H.van de Waterbeemd) Hydrogen Bonding, the Last Mystery in Drug Design? (H. Kubinyi) Molecular Hydrogen-Bonding Potentials (MHBPs) in Structure-Permeation Relations (G. Caron, S. Rey, G. Ermondi, P. Crivori, P. Gaillard, P.-A. Carrupt and B. Testa) VolSurf and its Interest in Structure-Disposition Relationships (G. Cruciani, S. Clementi, P. Crivori, P.-A. Carrupt and B. Testa) Molecular Modeling Approaches to Predict Metabolism and Toxicity (A.M. ter Laak and N.P.E. Vermeulen) CONCLUSION Molecular Biology, Drug Design and Drug Delivery: Bringing It All Together (V.H.L. Lee, S.K. Wu and C. Chu) Pharmacokinetic lead optimization: fine art vs. blind technology (B. Testa)
Rezensionen
Erwähnung in dem Artikel "Hürdenlauf im Körper" von Michael Breu auf: Tagesberichte: ETH Life - ETH Zurich's weekly web journal in English
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