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Drug-drug interactions in pharmaceutical development [[electronic resource] /] / edited by Albert P. Li
| Drug-drug interactions in pharmaceutical development [[electronic resource] /] / edited by Albert P. Li |
| Pubbl/distr/stampa | Hoboken, N.J., : Wiley-interscience, c2008 |
| Descrizione fisica | 1 online resource (261 p.) |
| Disciplina |
615.7045
615/.7045 |
| Altri autori (Persone) | LiA. P |
| Collana | Wiley series in drug discovery and development |
| Soggetto topico |
Drug interactions
Drug development |
| ISBN |
1-282-02206-7
9786612022067 0-470-18792-1 0-470-18791-3 |
| Formato | Materiale a stampa  |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
DRUG-DRUG INTERACTIONS IN PHARMACEUTICAL DEVELOPMENT; CONTENTS; Preface; Contributors; 1 In Vitro Evaluation of Metabolic Drug-Drug Interactions: Concepts and Practice; 1.1 Introduction; 1.2 Mechanisms of Adverse Drug-Drug Interactions; 1.2.1 Pharmacological Interactions; 1.2.2 Pharmacokinetic Interactions; 1.3 Drug Metabolism; 1.3.1 Phase I Oxidation; 1.3.2 Phase II Conjugation; 1.4 CYP Isoforms; 1.5 Human In Vitro Experimental Systems for Drug Metabolism; 1.5.1 Hepatocytes; 1.5.2 Liver Postmitochondrial Supernatant (PMS); 1.5.3 Human Liver Microsomes; 1.5.4 Recombinant P450 Isoforms (rCYP)
1.5.5 Cytosol1.6 Mechanisms of Metabolic Drug-Drug Interactions; 1.7 Mechanism-Based Approach for Evaluation of Drug-Drug Interaction Potential; 1.7.1 Metabolic Phenotyping; 1.7.2 Evaluation of Inhibitory Potential for Drug-Metabolizing Enzymes; 1.7.3 Induction Potential for Drug-Metabolizing Enzymes; 1.8 Experimental Approaches for In Vitro Evaluation of Drug-Drug Interaction Potential; 1.8.1 Study 1: Metabolic Phenotyping 1-Metabolite Identification; 1.8.2 Study 2: Metabolic Phenotyping 2-Identification of Major Metabolic Pathways 1.8.3 Study 3: Metabolic Phenotyping 3-Identification of P450 Isoform Pathways (P450 Phenotyping)1.8.4 Study 4: CYP Inhibitory Potential; 1.8.5 Study 5: Enzyme Induction Potential; 1.8.6 Study 6: In Vitro Empirical Drug-Drug Interactions; 1.9 Data Interpretation; 1.9.1 Pathway Evaluation; 1.9.2 P450 Inhibition; 1.9.3 P450 Induction; 1.10 Conclusion; References; 2 In Vitro Approaches to Anticipating Clinical Drug Interactions; 2.1 In Vitro Systems for Human CYP450 Metabolism; 2.1.1 Incubation Buffer (pH and Ionic Strength); 2.1.2 MgCl(2) and Cytochrome b(5); 2.1.3 Nonspecific Binding 2.1.4 Organic Solvents and Excipients2.2 Analysis of Data from In Vitro Systems; 2.2.1 Linear Transformation of Michaelis-Menten Equation (Lineweaver-Burk and Eadie-Hofstee); 2.2.2 Nonlinear Regression Analysis of Hyperbolic Kinetic Data; 2.2.3 Consideration of Non-Michaelis-Menten Kinetics; 2.3 Use of In Vitro Kinetic Data to Predict In Vivo Clearance; 2.3.1 Calculation of In Vitro (Predicted) Hepatic Clearance; 2.3.2 Comparison of In Vitro (Predicted) with In Vivo Hepatic Clearance; 2.4 Use of In Vitro Kinetic Data to Predict Drug-Drug Interactions 2.4.1 Choice of Probe Substrates for Inhibition Studies2.4.2 Determining the Mechanism of CYP450 Inhibition; 2.4.3 Prediction of In Vivo Drug-Drug Inhibition Interactions from In Vitro Data; 2.5 Consideration of Non-CYP Enzymatic Systems; 2.5.1 Flavin-Containing Monooxygenase (FMO); 2.5.2 UDP-glucuronosyltransferase (UGT); 2.5.3 Sulfotransferase (SULT); 2.5.4 N-Acetyltransferase (NAT); 2.5.5 Methyltransferase; 2.5.6 Epoxidase Hydrolase; 2.5.7 Aldehyde Oxidase and Dehydrogenase; 2.5.8 Glutathione-S-transferase (GST); 2.6 Summary; 2.7 Acknowledgments; References 3 Inhibition of Drug-Metabolizing Enzymes and Drug-Drug Interactions in Drug Discovery and Development |
| Record Nr. | UNINA-9910143982103321 |
| Hoboken, N.J., : Wiley-interscience, c2008 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Drug-drug interactions in pharmaceutical development / / edited by Albert P. Li
| Drug-drug interactions in pharmaceutical development / / edited by Albert P. Li |
| Edizione | [1st ed.] |
| Pubbl/distr/stampa | Hoboken, N.J., : Wiley-interscience, c2008 |
| Descrizione fisica | 1 online resource (261 p.) |
| Disciplina |
615.7045
615/.7045 |
| Altri autori (Persone) | LiA. P |
| Collana | Wiley series in drug discovery and development |
| Soggetto topico |
Drug interactions
Drug development |
| ISBN |
1-282-02206-7
9786612022067 0-470-18792-1 0-470-18791-3 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
DRUG-DRUG INTERACTIONS IN PHARMACEUTICAL DEVELOPMENT; CONTENTS; Preface; Contributors; 1 In Vitro Evaluation of Metabolic Drug-Drug Interactions: Concepts and Practice; 1.1 Introduction; 1.2 Mechanisms of Adverse Drug-Drug Interactions; 1.2.1 Pharmacological Interactions; 1.2.2 Pharmacokinetic Interactions; 1.3 Drug Metabolism; 1.3.1 Phase I Oxidation; 1.3.2 Phase II Conjugation; 1.4 CYP Isoforms; 1.5 Human In Vitro Experimental Systems for Drug Metabolism; 1.5.1 Hepatocytes; 1.5.2 Liver Postmitochondrial Supernatant (PMS); 1.5.3 Human Liver Microsomes; 1.5.4 Recombinant P450 Isoforms (rCYP)
1.5.5 Cytosol1.6 Mechanisms of Metabolic Drug-Drug Interactions; 1.7 Mechanism-Based Approach for Evaluation of Drug-Drug Interaction Potential; 1.7.1 Metabolic Phenotyping; 1.7.2 Evaluation of Inhibitory Potential for Drug-Metabolizing Enzymes; 1.7.3 Induction Potential for Drug-Metabolizing Enzymes; 1.8 Experimental Approaches for In Vitro Evaluation of Drug-Drug Interaction Potential; 1.8.1 Study 1: Metabolic Phenotyping 1-Metabolite Identification; 1.8.2 Study 2: Metabolic Phenotyping 2-Identification of Major Metabolic Pathways 1.8.3 Study 3: Metabolic Phenotyping 3-Identification of P450 Isoform Pathways (P450 Phenotyping)1.8.4 Study 4: CYP Inhibitory Potential; 1.8.5 Study 5: Enzyme Induction Potential; 1.8.6 Study 6: In Vitro Empirical Drug-Drug Interactions; 1.9 Data Interpretation; 1.9.1 Pathway Evaluation; 1.9.2 P450 Inhibition; 1.9.3 P450 Induction; 1.10 Conclusion; References; 2 In Vitro Approaches to Anticipating Clinical Drug Interactions; 2.1 In Vitro Systems for Human CYP450 Metabolism; 2.1.1 Incubation Buffer (pH and Ionic Strength); 2.1.2 MgCl(2) and Cytochrome b(5); 2.1.3 Nonspecific Binding 2.1.4 Organic Solvents and Excipients2.2 Analysis of Data from In Vitro Systems; 2.2.1 Linear Transformation of Michaelis-Menten Equation (Lineweaver-Burk and Eadie-Hofstee); 2.2.2 Nonlinear Regression Analysis of Hyperbolic Kinetic Data; 2.2.3 Consideration of Non-Michaelis-Menten Kinetics; 2.3 Use of In Vitro Kinetic Data to Predict In Vivo Clearance; 2.3.1 Calculation of In Vitro (Predicted) Hepatic Clearance; 2.3.2 Comparison of In Vitro (Predicted) with In Vivo Hepatic Clearance; 2.4 Use of In Vitro Kinetic Data to Predict Drug-Drug Interactions 2.4.1 Choice of Probe Substrates for Inhibition Studies2.4.2 Determining the Mechanism of CYP450 Inhibition; 2.4.3 Prediction of In Vivo Drug-Drug Inhibition Interactions from In Vitro Data; 2.5 Consideration of Non-CYP Enzymatic Systems; 2.5.1 Flavin-Containing Monooxygenase (FMO); 2.5.2 UDP-glucuronosyltransferase (UGT); 2.5.3 Sulfotransferase (SULT); 2.5.4 N-Acetyltransferase (NAT); 2.5.5 Methyltransferase; 2.5.6 Epoxidase Hydrolase; 2.5.7 Aldehyde Oxidase and Dehydrogenase; 2.5.8 Glutathione-S-transferase (GST); 2.6 Summary; 2.7 Acknowledgments; References 3 Inhibition of Drug-Metabolizing Enzymes and Drug-Drug Interactions in Drug Discovery and Development |
| Record Nr. | UNINA-9910818381003321 |
| Hoboken, N.J., : Wiley-interscience, c2008 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Enzyme inhibition in drug discovery and development [[electronic resource] ] : the good and the bad / / edited by Chuang Lu, Albert P. Li
| Enzyme inhibition in drug discovery and development [[electronic resource] ] : the good and the bad / / edited by Chuang Lu, Albert P. Li |
| Pubbl/distr/stampa | Hoboken, NJ, : John Wiley, c2010 |
| Descrizione fisica | 1 online resource (878 p.) |
| Disciplina |
615.35
615/.19 |
| Altri autori (Persone) |
LuChuang
LiA. P |
| Soggetto topico |
Enzyme inhibitors
Drug development Drugs - Metabolism |
| ISBN |
1-282-49134-2
9786612491344 0-470-53895-3 0-470-53894-5 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
ENZYME INHIBITION IN DRUG DISCOVERY AND DEVELOPMENT; CONTENTS; PREFACE; CONTRIBUTORS; PART I. DRUG DISCOVERY APPROACHES AND TECHNOLOGIES; 1. The Drug Discovery Process; 2. Medicinal Chemistry of the Optimization of Enzyme Inhibitors; 3. Bioanalytical Technologies in Drug Discovery; 4. Safety Biomarkers in Drug Development: Emerging Trends and Implications; 5. The Role of Drug Metabolism in Drug Discovery; 6. Applied Pharmacokinetics in Drug Discovery and Development; PART II. INHIBITION OF THE DRUG METABOLIZING ENZYMES-THE UNDESIRABLE INHIBITION
7. Enzyme Inhibition and Inactivation: Cytochrome P450 Enzymes8. Cytochrome P450 Induction; 9. Inhibition of Drug-Metabolizing Enzymes in the Gastrointestinal Tract and Its Influence on the Drug-Drug Interaction Prediction; 10. Enzyme Inhibition in Various In Vitro Systems; 11. Cytochrome P450 Degradation and Its Clinical Relevance; 12. Complexities of Working with UDP-Glucuronosyltransferases (UGTs): Focus on Enzyme Inhibition; 13. Evaluation of Inhibitors of Drug Metabolism in Human Hepatocytes; 14. Grapefruit Juice and Its Constituents as New Esterase Inhibitors 15. Transporter-Xenobiotic Interactions: An Important Aspect of Drug Development Studies16. Polymorphisms of Drug Transporters and Their Clinical Implications; 17. Clinical Drug Interactions Due to Metabolic Inhibition: Prediction, Assessment, and Interpretation; 18. Predicting Interindividual Variability of Metabolic Drug-Drug Interactions: Identifying the Causes and Accounting for Them Using a Systems Approach; PART III. INHIBITION OF THE DRUG TARGET ENZYMES-THE DESIRABLE INHIBITION; 19. NF-κB: Mechanism, Tumor Biology, and Inhibitors; 20. G-Protein-Coupled Receptors as Drug Targets 21. Pharmacological Modulation of Ion Channels for the Treatment of Chronic Pain22. Targeting the mTOR Pathway for Tumor Therapeutics; 23. HIV-1 Protease Inhibitors as Antiretroviral Agents; INDEX |
| Record Nr. | UNINA-9910139522703321 |
| Hoboken, NJ, : John Wiley, c2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Enzyme inhibition in drug discovery and development [[electronic resource] ] : the good and the bad / / edited by Chuang Lu, Albert P. Li
| Enzyme inhibition in drug discovery and development [[electronic resource] ] : the good and the bad / / edited by Chuang Lu, Albert P. Li |
| Pubbl/distr/stampa | Hoboken, NJ, : John Wiley, c2010 |
| Descrizione fisica | 1 online resource (878 p.) |
| Disciplina |
615.35
615/.19 |
| Altri autori (Persone) |
LuChuang
LiA. P |
| Soggetto topico |
Enzyme inhibitors
Drug development Drugs - Metabolism |
| ISBN |
1-282-49134-2
9786612491344 0-470-53895-3 0-470-53894-5 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
ENZYME INHIBITION IN DRUG DISCOVERY AND DEVELOPMENT; CONTENTS; PREFACE; CONTRIBUTORS; PART I. DRUG DISCOVERY APPROACHES AND TECHNOLOGIES; 1. The Drug Discovery Process; 2. Medicinal Chemistry of the Optimization of Enzyme Inhibitors; 3. Bioanalytical Technologies in Drug Discovery; 4. Safety Biomarkers in Drug Development: Emerging Trends and Implications; 5. The Role of Drug Metabolism in Drug Discovery; 6. Applied Pharmacokinetics in Drug Discovery and Development; PART II. INHIBITION OF THE DRUG METABOLIZING ENZYMES-THE UNDESIRABLE INHIBITION
7. Enzyme Inhibition and Inactivation: Cytochrome P450 Enzymes8. Cytochrome P450 Induction; 9. Inhibition of Drug-Metabolizing Enzymes in the Gastrointestinal Tract and Its Influence on the Drug-Drug Interaction Prediction; 10. Enzyme Inhibition in Various In Vitro Systems; 11. Cytochrome P450 Degradation and Its Clinical Relevance; 12. Complexities of Working with UDP-Glucuronosyltransferases (UGTs): Focus on Enzyme Inhibition; 13. Evaluation of Inhibitors of Drug Metabolism in Human Hepatocytes; 14. Grapefruit Juice and Its Constituents as New Esterase Inhibitors 15. Transporter-Xenobiotic Interactions: An Important Aspect of Drug Development Studies16. Polymorphisms of Drug Transporters and Their Clinical Implications; 17. Clinical Drug Interactions Due to Metabolic Inhibition: Prediction, Assessment, and Interpretation; 18. Predicting Interindividual Variability of Metabolic Drug-Drug Interactions: Identifying the Causes and Accounting for Them Using a Systems Approach; PART III. INHIBITION OF THE DRUG TARGET ENZYMES-THE DESIRABLE INHIBITION; 19. NF-κB: Mechanism, Tumor Biology, and Inhibitors; 20. G-Protein-Coupled Receptors as Drug Targets 21. Pharmacological Modulation of Ion Channels for the Treatment of Chronic Pain22. Targeting the mTOR Pathway for Tumor Therapeutics; 23. HIV-1 Protease Inhibitors as Antiretroviral Agents; INDEX |
| Record Nr. | UNINA-9910830438803321 |
| Hoboken, NJ, : John Wiley, c2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Enzyme inhibition in drug discovery and development : the good and the bad / / edited by Chuang Lu, Albert P. Li
| Enzyme inhibition in drug discovery and development : the good and the bad / / edited by Chuang Lu, Albert P. Li |
| Pubbl/distr/stampa | Hoboken, NJ, : John Wiley, c2010 |
| Descrizione fisica | 1 online resource (878 p.) |
| Disciplina |
615.35
615/.19 |
| Altri autori (Persone) |
LuChuang
LiA. P |
| Soggetto topico |
Enzyme inhibitors
Drug development Drugs - Metabolism |
| ISBN |
1-282-49134-2
9786612491344 0-470-53895-3 0-470-53894-5 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
ENZYME INHIBITION IN DRUG DISCOVERY AND DEVELOPMENT; CONTENTS; PREFACE; CONTRIBUTORS; PART I. DRUG DISCOVERY APPROACHES AND TECHNOLOGIES; 1. The Drug Discovery Process; 2. Medicinal Chemistry of the Optimization of Enzyme Inhibitors; 3. Bioanalytical Technologies in Drug Discovery; 4. Safety Biomarkers in Drug Development: Emerging Trends and Implications; 5. The Role of Drug Metabolism in Drug Discovery; 6. Applied Pharmacokinetics in Drug Discovery and Development; PART II. INHIBITION OF THE DRUG METABOLIZING ENZYMES-THE UNDESIRABLE INHIBITION
7. Enzyme Inhibition and Inactivation: Cytochrome P450 Enzymes8. Cytochrome P450 Induction; 9. Inhibition of Drug-Metabolizing Enzymes in the Gastrointestinal Tract and Its Influence on the Drug-Drug Interaction Prediction; 10. Enzyme Inhibition in Various In Vitro Systems; 11. Cytochrome P450 Degradation and Its Clinical Relevance; 12. Complexities of Working with UDP-Glucuronosyltransferases (UGTs): Focus on Enzyme Inhibition; 13. Evaluation of Inhibitors of Drug Metabolism in Human Hepatocytes; 14. Grapefruit Juice and Its Constituents as New Esterase Inhibitors 15. Transporter-Xenobiotic Interactions: An Important Aspect of Drug Development Studies16. Polymorphisms of Drug Transporters and Their Clinical Implications; 17. Clinical Drug Interactions Due to Metabolic Inhibition: Prediction, Assessment, and Interpretation; 18. Predicting Interindividual Variability of Metabolic Drug-Drug Interactions: Identifying the Causes and Accounting for Them Using a Systems Approach; PART III. INHIBITION OF THE DRUG TARGET ENZYMES-THE DESIRABLE INHIBITION; 19. NF-κB: Mechanism, Tumor Biology, and Inhibitors; 20. G-Protein-Coupled Receptors as Drug Targets 21. Pharmacological Modulation of Ion Channels for the Treatment of Chronic Pain22. Targeting the mTOR Pathway for Tumor Therapeutics; 23. HIV-1 Protease Inhibitors as Antiretroviral Agents; INDEX |
| Record Nr. | UNINA-9910877182103321 |
| Hoboken, NJ, : John Wiley, c2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||