Chemistry and pharmacology of anticancer drugs:
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| Main Author: | |
|---|---|
| Format: | Book |
| Language: | English |
| Published: |
Boca Raton
CRC Press/Taylor & Francis
2007
|
| Subjects: | |
| Online Access: | Table of contents only Publisher description Inhaltsverzeichnis |
| Item Description: | Includes bibliographical references and index |
| Physical Description: | 290 S. Ill. 25 cm |
| ISBN: | 1420008900 0849392195 9780849392191 |
Staff View
MARC
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| 100 | 1 | |a Thurston, David E. |e Verfasser |4 aut | |
| 245 | 1 | 0 | |a Chemistry and pharmacology of anticancer drugs |c David E. Thurston |
| 264 | 1 | |a Boca Raton |b CRC Press/Taylor & Francis |c 2007 | |
| 300 | |a 290 S. |b Ill. |c 25 cm | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 500 | |a Includes bibliographical references and index | ||
| 650 | 4 | |a Anticancéreux | |
| 650 | 4 | |a Antineoplastic agents | |
| 650 | 4 | |a Antineoplastic Agents |x pharmacology | |
| 650 | 4 | |a Antineoplastic Agents |x chemistry | |
| 650 | 0 | 7 | |a Cytostatikum |0 (DE-588)4068347-3 |2 gnd |9 rswk-swf |
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| 856 | 4 | 2 | |m HBZ Datenaustausch |q application/pdf |u http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=016143516&sequence=000014&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |3 Inhaltsverzeichnis |
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Contents
Chapter 1 Introduction to Cancer 1
1.1 Introduction 1
1.2 Terminology 1
1.3 Metastases 2
1.4 Diagnosis and Screening 3
1.5 Formation of Cancer Cells (Tumorigenesis) 4
1.6 Mechanisms of Genomic Damage 5
1.6.1 Internal Factors 5
1.6.1.1 Mutations 5
1.6.1.2 Addition or Loss of Genetic Material 5
1.6.1.3 Epigenetic Changes 5
1.6.1.4 Modified Gene Expression 7
1.6.2 External Factors 7
1.6.2.1 Viruses 7
1.6.2.2 Bacterial Infections 8
1.6.2.3 Chemicals 8
1.6.2.4 Radioactivity 10
1.6.2.5 Electromagnetic Radiation 10
1.6.2.6 Cancer Treatments 11
1.6.3 Hereditary Factors 12
1.7 Treatments 12
1.7.1 Surgery 12
1.7.2 Radiotherapy 13
1.7.3 Photodynamic Therapy (PDT) 14
1.7.4 Biological Response Modifying Agents 14
1.7.5 Chemotherapy 14
1.8 Discovery of Anticancer Drugs and Preclinical Evaluation 15
1.9 Accessibility of Drugs to Tumor Cells 17
1.10 Achieving Selective Toxicity 17
1.11 Limiting the Toxicity of Chemotherapeutic Agents 18
1.11.1 Dose Scheduling and Cell Cycle 18
1.11.2 Use of Adjuvants 20
1.11.3 Novel Formulations and Prodrugs 20
1.11.4 The Cold Cap 20
1.11.5 Pharmacogenomic Markers of Toxicity 20
1.12 Overview of Mechanisms of Action of Chemotherapeutic Agents 21
1.13 Drug Resistance 23
1.14 Combination Chemotherapy 25
1.15 Use of Adjuvants 26
1.16 Infertility Following Cancer Treatments 26
Further Reading 27
Chapter 2 Antimetabolites 29
2.1 Introduction 29
2.2 DHFR Inhibitors (Antifolates) 29
2.2.1 Methotrexate 29
2.3 Purine Antimetabolites 31
2.4 Pyrimidine Antimetabolites 32
2.5 Thymidylate Synthase Inhibition 34
2.6 Adenosine Deaminase Inhibition 35
2.7 Ribonucleotide Reductase Inhibition 35
Further Reading 36
Chapter 3 DNA Interactive Agents 37
3.1 Introduction 37
3.2 Alkylating Agents 38
3.2.1 Methylating Agents 38
3.2.1.1 Dacarbazine 38
3.2.1.2 Temozolomide 39
3.2.1.3 Procarbazine 43
3.2.2 Ecteinascidin 743 44
3.2.3 Pyrrolobenzodiazepine (PBD) Monomers 45
3.3 Cross Linking Agents 47
3.3.1 Nitrogen Mustards 49
3.3.1.1 Aliphatic Nitrogen Mustards 50
3.3.1.2 Aromatic Nitrogen Mustards 51
3.3.1.3 Oxazaphosphorines 52
3.3.1.4 Conjugated Nitrogen Mustards 54
3.3.2 Aziridines 56
3.3.3 Epoxides 57
3.3.4 Methanesulfonates 57
3.3.5 Nitrosoureas 58
3.3.5.1 Lomustine 59
3.3.5.2 Carmustine 60
3.3.6 Platinum Complexes 61
3.3.6.1 Cisplatin 62
3.3.6.2 Carboplatin 63
3.3.6.3 Oxaliplatin 63
3.3.7 Carbinolamines 63
3.3.8 Cyclopropanes 65
3.3.9 Mitomycin C 65
3.3.10 Sequence Selective DNA Cross Linking Agents 66
3.3.10.1 PBD Dimers (SJG 136) 67
3.3.10.2 Cyclopropanepyrroloindole (CP1) Dimer (Bizelesin) 67
3.4 Intercalating Agents 69
3.4.1 Anthracyclines 71
3.4.1.1 Doxorubicin 71
3.4.1.2 Daunorubicin 73
3.4.1.3 Aclarubicin 73
3.4.1.4 Epirubicin 73
3.4.1.5 Idarubicin 73
3.4.2 Anthracenes 74
3.4.2.1 Mitoxantrone 74
3.4.3 Phenoxazines 74
3.4.3.1 Dactinomycin 75
3.5 Topoisomerase Inhibitors 76
3.5.1 Topoisomerase I Inhibitors 77
3.5.1.1 Topotecan 77
3.5.1.2 Irinotecan 78
3.5.2 Topoisomerase II Inhibitors 79
3.5.2.1 Etoposide 79
3.5.2.2 Teniposide 80
3.5.2.3 Ellipticene 81
3.5.2.4 Amsacrine 81
3.6 DNA Cleaving Agents 81
3.6.1 Bleomycins 82
3.6.2 Enediynes 83
Further Reading 84
Chapter 4 Antitubulin Agents 85
4.1 Introduction 85
4.2 Vinca Alkaloids 87
4.2.1 Vinblastine 89
4.2.2 Vincristine 90
4.2.3 Vindesine 90
4.2.4 Vinorelbine 90
4.3 TheTaxanes 90
4.3.1 Paclitaxel 92
4.3.2 Docetaxel 93
Further Reading 93
Chapter 5 Molecularly Targeted Agents 95
5.1 Introduction 95
5.2 Kinase Inhibitors 96
5.2.1 Classification of Protein Kinases 96
5.2.2 Functions of Protein Kinases 97
5.2.3 Mechanism of Signal Transfer 98
5.2.4 Regulation of Kinase Activity by Drugs 98
5.2.5 Role of Protein Kinases in Cancer 99
5.2.5.1 Mutations in Protein Kinases 99
5.2.5.2 Overexpression of Protein Kinases 100
5.2.6 Development of Inhibitors of Protein and Receptor Kinases 100
5.2.6.1 BCR ABL Inhibition: Imatinib 100
5.2.6.2 HER2/neu Inhibition: Trastuzumab 102
5.2.6.3 EGFR Inhibition: Gefitinib, Erlotinib, and Cetuximab . 103
5.2.6.4 VEGFR Inhibition 109
5.2.6.5 PDGFR Inhibition 110
5.2.6.6 Multiple Target Inhibitors 111
5.2.6.7 Other Potential Targets 112
5.3 Inhibition of Ras Pathway Signaling 114
5.3.1 Introduction 114
5.3.2 Mechanism of Ras Signaling Pathway 115
5.3.3 Classes of Inhibitors of Farnesyltransferase 116
5.3.4 Tipifarnib 117
5.3.5 Lonafarnib 118
5.3.6 BMS 214662 118
5.3.7 Other Novel Ras Pathway Inhibitors 119
5.4 Cell Cycle Inhibitors 119
5.5 Proteasome Inhibitors 120
5.6 mTOR Inhibitors 122
Further Reading 125
Chapter 6 Hormonal Therapies 127
6.1 Introduction 127
6.2 Breast Cancer 127
6.2.1 Early Breast Cancer 127
6.2.2 Advanced Breast Cancer 128
6.2.3 Role of Estrogen in Tumor Growth 128
6.2.4 Anti Estrogens 130
6.2.4.1 Tamoxifen 130
6.2.4.2 Toremifene 132
6.2.4.3 Novel Selective ER Modulators 132
6.2.5 Aromatase Inhibitors 134
6.2.5.1 Aminoglutethimide 136
6.2.5.2 Anastrozole 137
6.2.5.3 Letrozole 137
6.2.5.4 Vorozole 138
6.2.5.5 Exemestane 139
6.3 Prostatic Cancer 139
6.3.1 Gonadorelin Analogs (LH RH Analogs; Agonists and
Antagonists) 142
6.3.1.1 Buserelin 143
6.3.1.2 Goserelin 144
6.3.1.3 Leuprorelin Acetate 144
6.3.1.4 Triptorelin 144
6.3.2 LH RH Receptor Antagonists 145
6.3.3 Anti Androgens 146
6.3.3.1 Cyproterone Acetate 148
6.3.3.2 Flutamide 149
6.3.3.3 Bicalutamide 150
6.3.3.4 Nilutamide 150
6.4 Neuroendocrine Tumors: Somatostatin Analogs 151
6.4.1 Octreotide 152
6.4.2 Lanreotide 152
6.5 Estrogen Therapy 153
6.5.1 Diethylstilbestrol 153
6.5.2 Ethinylestradiol 153
6.6 Progestogen Therapy 154
6.6.1 Gestonorone Caproate 154
6.6.2 Medroxyprogesterone Acetate 155
6.6.3 Megestrol Acetate 155
6.6.4 Norethisterone 156
Further Reading 156
Chapter 7 Tumor Targeting Strategies 157
7.1 Introduction 157
7.2 Antibody Based Approaches 158
7.2.1 Antibodies as Single Agents 159
7.2.2 Antibody Drug Conjugates 160
7.2.2.1 Gemtuzumab Ozogamicin 160
7.2.3 Antibody Radionuclide Conjugates 161
7.2.3.1 Pemtumomab 161
7.3 Vascular Targeting Strategies 162
7.3.1 Anti Angiogenic Agents 164
7.3.1.1 Bevacizumab 164
7.3.2 Vascular Disruptive Agents (VDAs) 165
7.3.2.1 Combretastatins 165
7.3.2.2 Combretastatin Prodrugs: CA4P and Oxi4503 168
7.3.2.3 Flavone 8 Acetic Acid (FAA) and DMXAA 168
7.3.3 Bioreductive Agents 170
7.3.3.1 AQ4N 171
7.3.4 Polymer Drug Conjugates 172
7.4 X DEPT (Biphasic) Strategies 173
7.4.1 ADEPT 174
7.4.2 GDEPT (or VDEPT) 176
7.4.3 PDEPT 178
7.5 Enzymatic Targeting 179
7.5.1 Prodrug Activation by Constitutively Overexpressed Tumor
Enzymes 179
7.5.2 Cosubstrate Mediated Prodrug Therapy 180
7.5.3 Asparaginase 182
7.6 Photoactivated Drugs (Photodynamic Therapy) 182
7.6.1 Porfimer Sodium 183
7.6.2 Temoporfin 184
7.7 Boron Neutron Capture Therapy (BNCT) 184
7.8 Novel Drug Delivery Approaches 187
7.8.1 Gene Therapy 187
7.8.2 Nanotechnology Based Drug Delivery 188
7.8.3 Intracranial Delivery 189
7.8.4 Ultrasound Targeting 189
Further Reading 191
Chapter 8 Biological Agents 193
8.1 Introduction 193
8.2 Biological Response Modifiers (BRMs) 194
8.2.1 Monoclonal Antibodies (MAbs) 194
8.2.1.1 Rituximab 194
8.2.1.2 Alemtuzumab 194
8.2.2 Interferons 195
8.2.2.1 Interferon Alpha 195
8.2.3 Interleukins 196
8.2.3.1 Interleukin 2 196
8.3 Immunotherapy 196
8.3.1 BCG Bladder Instillation 197
8.4 Enzyme Based Therapies 197
8.4.1 Asparaginase 198
8.5 Vaccines 198
8.5.1 The Immune System 199
8.5.2 Types of Cancer Vaccines 199
8.5.3 Strategies for Stimulating the Immune System 200
8.5.3.1 Direct Use of Tumor Antigens 200
8.5.3.2 Enhancement of Immunogenicity of Tumor Antigens 200
8.5.3.3 Primed APCs 201
8.5.3.4 Anti Idiotype Antibodies 201
8.5.4 Manufacture of Vaccines 201
8.5.5 Activity of Vaccines 202
8.5.6 Examples of Vaccines in Development 202
8.5.6.1 Non Hodgkin's Lymphoma 202
8.5.6.2 Non Small Cell Lung Cancer (NSCLC) 203
8.5.6.3 Melanoma 203
8.5.6.4 Prostate Cancer 203
8.5.6.5 Cervical Cancer 203
8.5.6.6 Head and Neck and Cervical Cancer 203
8.5.7 Conclusion 204
Further Reading 204
Chapter 9 The Future 205
9.1 Introduction 205
9.2 Novel Biological Targets and Therapeutic Strategies 205
9.2.1 Novel Therapeutic Targets 205
9.2.1.1 Resistance Inhibitors 205
9.2.1.2 Telomerase Inhibitors 209
9.2.1.3 Epigenetic Based Therapies 211
9.2.1.4 Antimetastatic Agents 216
9.2.1.5 Heat Shock Protein (HSP) Inhibitors 219
9.2.1.6 Thioredoxin Reductase Inhibitors 222
9.2.1.7 HDM2 p53 Binding Inhibitors 223
9.2.1.8 Radiosensitizing Agents 226
9.2.2 New Biological Agents 227
9.2.2.1 Growth Factors 227
9.2.2.2 Tumor Necrosis Factor 228
9.2.2.3 Immunomodulation 228
9.2.3 Novel Drug Delivery Systems 229
9.2.3.1 Near Infrared Activated Nanoshells 230
9.2.3.2 Radioactive Glass Beads (Microspheres) 231
9.2.4 Nucleic Acid Targeting 231
9.2.4.1 Antigene Strategy 233
9.2.4.2 Antisense Strategy 235
9.2.4.3 Ribozymes 236
9.2.4.4 Zinc Finger Proteins (ZFPs) 237
9.2.4.5 GenelCE™ Technology 238
9.2.4.6 Decoy Strategies 239
9.2.4.7 RNA Interference (RNAi) 239
9.2.5 Gene Therapy 241
9.2.6 Cancer Stem Cells 242
9.3 New Research Tools and Methodologies 244
9.3.1 Gene Hunting and DNA Sequencing 245
9.3.2 Genomics and Proteomics 245
9.3.3 Protein Structural Studies 247
9.3.4 Chemical Technologies 247
9.3.5 Screening Methodologies 249
9.3.6 In Vivo Models 249
9.3.7 Sources of New Lead Molecules 250
9.4 Chemopreventive Agents 252
9.4.1 Resveratrol 254
9.4.2 Phytoestrogens 255
9.4.3 Curcumin 256
9.4.4 Sulforaphane 257
9.4.5 COX 2 Inhibitors 258
9.4.6 Antioxidants 260
9.4.6.1 Ascorbic Acid (Vitamin C) 260
9.4.6.2 Ergothioneine 261
9.4.7 Olive Oil (The "Mediterranean Diet") 261
9.4.7.1 Oleic Acid 262
9.4.7.2 Oleocanthal 262
9.4.7.3 Lycopene 263
9.4.8 The KEAP1 Gene 264
Further Reading 265
Chapter 10 Personalized Treatments 267
10.1 Introduction 268
10.2 Screening for Risk of Disease Development 269
10.3 Prognosis and Staging 271
10.4 Screening for Risk of Recurrence of Disease 272
10.5 Selecting Best Treatments for Patients 272
10.5.1 Genomic and Proteomic Tests 272
10.5.2 Chemosensitivity Testing 273
10.6 Predicting Side Effects of Chemotherapeutic Agents 273
10.7 Pharmacogenomics in Clinical Trials 275
Further Reading 276
Chapter 11 Adjunct Therapies 279
11.1 Introduction 279
11.2 Anti Emetic Agents 279
11.2.1 Oral and Parenteral Dosing 279
11.2.2 Sublingual Dosing 281
11.3 Steroidal Agents 282
11.3.1 Prednisolone and Dexamethasone 282
11.4 Adjuvent Enzymes 282
11.4.1 Chemophase™ 282
11.5 Other Therapies 283
11.5.1 Razoxane 283
Further Reading 283
Index 285 |
| adam_txt |
Contents
Chapter 1 Introduction to Cancer 1
1.1 Introduction 1
1.2 Terminology 1
1.3 Metastases 2
1.4 Diagnosis and Screening 3
1.5 Formation of Cancer Cells (Tumorigenesis) 4
1.6 Mechanisms of Genomic Damage 5
1.6.1 Internal Factors 5
1.6.1.1 Mutations 5
1.6.1.2 Addition or Loss of Genetic Material 5
1.6.1.3 Epigenetic Changes 5
1.6.1.4 Modified Gene Expression 7
1.6.2 External Factors 7
1.6.2.1 Viruses 7
1.6.2.2 Bacterial Infections 8
1.6.2.3 Chemicals 8
1.6.2.4 Radioactivity 10
1.6.2.5 Electromagnetic Radiation 10
1.6.2.6 Cancer Treatments 11
1.6.3 Hereditary Factors 12
1.7 Treatments 12
1.7.1 Surgery 12
1.7.2 Radiotherapy 13
1.7.3 Photodynamic Therapy (PDT) 14
1.7.4 Biological Response Modifying Agents 14
1.7.5 Chemotherapy 14
1.8 Discovery of Anticancer Drugs and Preclinical Evaluation 15
1.9 Accessibility of Drugs to Tumor Cells 17
1.10 Achieving Selective Toxicity 17
1.11 Limiting the Toxicity of Chemotherapeutic Agents 18
1.11.1 Dose Scheduling and Cell Cycle 18
1.11.2 Use of Adjuvants 20
1.11.3 Novel Formulations and Prodrugs 20
1.11.4 The Cold Cap 20
1.11.5 Pharmacogenomic Markers of Toxicity 20
1.12 Overview of Mechanisms of Action of Chemotherapeutic Agents 21
1.13 Drug Resistance 23
1.14 Combination Chemotherapy 25
1.15 Use of Adjuvants 26
1.16 Infertility Following Cancer Treatments 26
Further Reading 27
Chapter 2 Antimetabolites 29
2.1 Introduction 29
2.2 DHFR Inhibitors (Antifolates) 29
2.2.1 Methotrexate 29
2.3 Purine Antimetabolites 31
2.4 Pyrimidine Antimetabolites 32
2.5 Thymidylate Synthase Inhibition 34
2.6 Adenosine Deaminase Inhibition 35
2.7 Ribonucleotide Reductase Inhibition 35
Further Reading 36
Chapter 3 DNA Interactive Agents 37
3.1 Introduction 37
3.2 Alkylating Agents 38
3.2.1 Methylating Agents 38
3.2.1.1 Dacarbazine 38
3.2.1.2 Temozolomide 39
3.2.1.3 Procarbazine 43
3.2.2 Ecteinascidin 743 44
3.2.3 Pyrrolobenzodiazepine (PBD) Monomers 45
3.3 Cross Linking Agents 47
3.3.1 Nitrogen Mustards 49
3.3.1.1 Aliphatic Nitrogen Mustards 50
3.3.1.2 Aromatic Nitrogen Mustards 51
3.3.1.3 Oxazaphosphorines 52
3.3.1.4 Conjugated Nitrogen Mustards 54
3.3.2 Aziridines 56
3.3.3 Epoxides 57
3.3.4 Methanesulfonates 57
3.3.5 Nitrosoureas 58
3.3.5.1 Lomustine 59
3.3.5.2 Carmustine 60
3.3.6 Platinum Complexes 61
3.3.6.1 Cisplatin 62
3.3.6.2 Carboplatin 63
3.3.6.3 Oxaliplatin 63
3.3.7 Carbinolamines 63
3.3.8 Cyclopropanes 65
3.3.9 Mitomycin C 65
3.3.10 Sequence Selective DNA Cross Linking Agents 66
3.3.10.1 PBD Dimers (SJG 136) 67
3.3.10.2 Cyclopropanepyrroloindole (CP1) Dimer (Bizelesin) 67
3.4 Intercalating Agents 69
3.4.1 Anthracyclines 71
3.4.1.1 Doxorubicin 71
3.4.1.2 Daunorubicin 73
3.4.1.3 Aclarubicin 73
3.4.1.4 Epirubicin 73
3.4.1.5 Idarubicin 73
3.4.2 Anthracenes 74
3.4.2.1 Mitoxantrone 74
3.4.3 Phenoxazines 74
3.4.3.1 Dactinomycin 75
3.5 Topoisomerase Inhibitors 76
3.5.1 Topoisomerase I Inhibitors 77
3.5.1.1 Topotecan 77
3.5.1.2 Irinotecan 78
3.5.2 Topoisomerase II Inhibitors 79
3.5.2.1 Etoposide 79
3.5.2.2 Teniposide 80
3.5.2.3 Ellipticene 81
3.5.2.4 Amsacrine 81
3.6 DNA Cleaving Agents 81
3.6.1 Bleomycins 82
3.6.2 Enediynes 83
Further Reading 84
Chapter 4 Antitubulin Agents 85
4.1 Introduction 85
4.2 Vinca Alkaloids 87
4.2.1 Vinblastine 89
4.2.2 Vincristine 90
4.2.3 Vindesine 90
4.2.4 Vinorelbine 90
4.3 TheTaxanes 90
4.3.1 Paclitaxel 92
4.3.2 Docetaxel 93
Further Reading 93
Chapter 5 Molecularly Targeted Agents 95
5.1 Introduction 95
5.2 Kinase Inhibitors 96
5.2.1 Classification of Protein Kinases 96
5.2.2 Functions of Protein Kinases 97
5.2.3 Mechanism of Signal Transfer 98
5.2.4 Regulation of Kinase Activity by Drugs 98
5.2.5 Role of Protein Kinases in Cancer 99
5.2.5.1 Mutations in Protein Kinases 99
5.2.5.2 Overexpression of Protein Kinases 100
5.2.6 Development of Inhibitors of Protein and Receptor Kinases 100
5.2.6.1 BCR ABL Inhibition: Imatinib 100
5.2.6.2 HER2/neu Inhibition: Trastuzumab 102
5.2.6.3 EGFR Inhibition: Gefitinib, Erlotinib, and Cetuximab . 103
5.2.6.4 VEGFR Inhibition 109
5.2.6.5 PDGFR Inhibition 110
5.2.6.6 Multiple Target Inhibitors 111
5.2.6.7 Other Potential Targets 112
5.3 Inhibition of Ras Pathway Signaling 114
5.3.1 Introduction 114
5.3.2 Mechanism of Ras Signaling Pathway 115
5.3.3 Classes of Inhibitors of Farnesyltransferase 116
5.3.4 Tipifarnib 117
5.3.5 Lonafarnib 118
5.3.6 BMS 214662 118
5.3.7 Other Novel Ras Pathway Inhibitors 119
5.4 Cell Cycle Inhibitors 119
5.5 Proteasome Inhibitors 120
5.6 mTOR Inhibitors 122
Further Reading 125
Chapter 6 Hormonal Therapies 127
6.1 Introduction 127
6.2 Breast Cancer 127
6.2.1 Early Breast Cancer 127
6.2.2 Advanced Breast Cancer 128
6.2.3 Role of Estrogen in Tumor Growth 128
6.2.4 Anti Estrogens 130
6.2.4.1 Tamoxifen 130
6.2.4.2 Toremifene 132
6.2.4.3 Novel Selective ER Modulators 132
6.2.5 Aromatase Inhibitors 134
6.2.5.1 Aminoglutethimide 136
6.2.5.2 Anastrozole 137
6.2.5.3 Letrozole 137
6.2.5.4 Vorozole 138
6.2.5.5 Exemestane 139
6.3 Prostatic Cancer 139
6.3.1 Gonadorelin Analogs (LH RH Analogs; Agonists and
Antagonists) 142
6.3.1.1 Buserelin 143
6.3.1.2 Goserelin 144
6.3.1.3 Leuprorelin Acetate 144
6.3.1.4 Triptorelin 144
6.3.2 LH RH Receptor Antagonists 145
6.3.3 Anti Androgens 146
6.3.3.1 Cyproterone Acetate 148
6.3.3.2 Flutamide 149
6.3.3.3 Bicalutamide 150
6.3.3.4 Nilutamide 150
6.4 Neuroendocrine Tumors: Somatostatin Analogs 151
6.4.1 Octreotide 152
6.4.2 Lanreotide 152
6.5 Estrogen Therapy 153
6.5.1 Diethylstilbestrol 153
6.5.2 Ethinylestradiol 153
6.6 Progestogen Therapy 154
6.6.1 Gestonorone Caproate 154
6.6.2 Medroxyprogesterone Acetate 155
6.6.3 Megestrol Acetate 155
6.6.4 Norethisterone 156
Further Reading 156
Chapter 7 Tumor Targeting Strategies 157
7.1 Introduction 157
7.2 Antibody Based Approaches 158
7.2.1 Antibodies as Single Agents 159
7.2.2 Antibody Drug Conjugates 160
7.2.2.1 Gemtuzumab Ozogamicin 160
7.2.3 Antibody Radionuclide Conjugates 161
7.2.3.1 Pemtumomab 161
7.3 Vascular Targeting Strategies 162
7.3.1 Anti Angiogenic Agents 164
7.3.1.1 Bevacizumab 164
7.3.2 Vascular Disruptive Agents (VDAs) 165
7.3.2.1 Combretastatins 165
7.3.2.2 Combretastatin Prodrugs: CA4P and Oxi4503 168
7.3.2.3 Flavone 8 Acetic Acid (FAA) and DMXAA 168
7.3.3 Bioreductive Agents 170
7.3.3.1 AQ4N 171
7.3.4 Polymer Drug Conjugates 172
7.4 X DEPT (Biphasic) Strategies 173
7.4.1 ADEPT 174
7.4.2 GDEPT (or VDEPT) 176
7.4.3 PDEPT 178
7.5 Enzymatic Targeting 179
7.5.1 Prodrug Activation by Constitutively Overexpressed Tumor
Enzymes 179
7.5.2 Cosubstrate Mediated Prodrug Therapy 180
7.5.3 Asparaginase 182
7.6 Photoactivated Drugs (Photodynamic Therapy) 182
7.6.1 Porfimer Sodium 183
7.6.2 Temoporfin 184
7.7 Boron Neutron Capture Therapy (BNCT) 184
7.8 Novel Drug Delivery Approaches 187
7.8.1 Gene Therapy 187
7.8.2 Nanotechnology Based Drug Delivery 188
7.8.3 Intracranial Delivery 189
7.8.4 Ultrasound Targeting 189
Further Reading 191
Chapter 8 Biological Agents 193
8.1 Introduction 193
8.2 Biological Response Modifiers (BRMs) 194
8.2.1 Monoclonal Antibodies (MAbs) 194
8.2.1.1 Rituximab 194
8.2.1.2 Alemtuzumab 194
8.2.2 Interferons 195
8.2.2.1 Interferon Alpha 195
8.2.3 Interleukins 196
8.2.3.1 Interleukin 2 196
8.3 Immunotherapy 196
8.3.1 BCG Bladder Instillation 197
8.4 Enzyme Based Therapies 197
8.4.1 Asparaginase 198
8.5 Vaccines 198
8.5.1 The Immune System 199
8.5.2 Types of Cancer Vaccines 199
8.5.3 Strategies for Stimulating the Immune System 200
8.5.3.1 Direct Use of Tumor Antigens 200
8.5.3.2 Enhancement of Immunogenicity of Tumor Antigens 200
8.5.3.3 Primed APCs 201
8.5.3.4 Anti Idiotype Antibodies 201
8.5.4 Manufacture of Vaccines 201
8.5.5 Activity of Vaccines 202
8.5.6 Examples of Vaccines in Development 202
8.5.6.1 Non Hodgkin's Lymphoma 202
8.5.6.2 Non Small Cell Lung Cancer (NSCLC) 203
8.5.6.3 Melanoma 203
8.5.6.4 Prostate Cancer 203
8.5.6.5 Cervical Cancer 203
8.5.6.6 Head and Neck and Cervical Cancer 203
8.5.7 Conclusion 204
Further Reading 204
Chapter 9 The Future 205
9.1 Introduction 205
9.2 Novel Biological Targets and Therapeutic Strategies 205
9.2.1 Novel Therapeutic Targets 205
9.2.1.1 Resistance Inhibitors 205
9.2.1.2 Telomerase Inhibitors 209
9.2.1.3 Epigenetic Based Therapies 211
9.2.1.4 Antimetastatic Agents 216
9.2.1.5 Heat Shock Protein (HSP) Inhibitors 219
9.2.1.6 Thioredoxin Reductase Inhibitors 222
9.2.1.7 HDM2 p53 Binding Inhibitors 223
9.2.1.8 Radiosensitizing Agents 226
9.2.2 New Biological Agents 227
9.2.2.1 Growth Factors 227
9.2.2.2 Tumor Necrosis Factor 228
9.2.2.3 Immunomodulation 228
9.2.3 Novel Drug Delivery Systems 229
9.2.3.1 Near Infrared Activated Nanoshells 230
9.2.3.2 Radioactive Glass Beads (Microspheres) 231
9.2.4 Nucleic Acid Targeting 231
9.2.4.1 Antigene Strategy 233
9.2.4.2 Antisense Strategy 235
9.2.4.3 Ribozymes 236
9.2.4.4 Zinc Finger Proteins (ZFPs) 237
9.2.4.5 GenelCE™ Technology 238
9.2.4.6 Decoy Strategies 239
9.2.4.7 RNA Interference (RNAi) 239
9.2.5 Gene Therapy 241
9.2.6 Cancer Stem Cells 242
9.3 New Research Tools and Methodologies 244
9.3.1 Gene Hunting and DNA Sequencing 245
9.3.2 Genomics and Proteomics 245
9.3.3 Protein Structural Studies 247
9.3.4 Chemical Technologies 247
9.3.5 Screening Methodologies 249
9.3.6 In Vivo Models 249
9.3.7 Sources of New Lead Molecules 250
9.4 Chemopreventive Agents 252
9.4.1 Resveratrol 254
9.4.2 Phytoestrogens 255
9.4.3 Curcumin 256
9.4.4 Sulforaphane 257
9.4.5 COX 2 Inhibitors 258
9.4.6 Antioxidants 260
9.4.6.1 Ascorbic Acid (Vitamin C) 260
9.4.6.2 Ergothioneine 261
9.4.7 Olive Oil (The "Mediterranean Diet") 261
9.4.7.1 Oleic Acid 262
9.4.7.2 Oleocanthal 262
9.4.7.3 Lycopene 263
9.4.8 The KEAP1 Gene 264
Further Reading 265
Chapter 10 Personalized Treatments 267
10.1 Introduction 268
10.2 Screening for Risk of Disease Development 269
10.3 Prognosis and Staging 271
10.4 Screening for Risk of Recurrence of Disease 272
10.5 Selecting Best Treatments for Patients 272
10.5.1 Genomic and Proteomic Tests 272
10.5.2 Chemosensitivity Testing 273
10.6 Predicting Side Effects of Chemotherapeutic Agents 273
10.7 Pharmacogenomics in Clinical Trials 275
Further Reading 276
Chapter 11 Adjunct Therapies 279
11.1 Introduction 279
11.2 Anti Emetic Agents 279
11.2.1 Oral and Parenteral Dosing 279
11.2.2 Sublingual Dosing 281
11.3 Steroidal Agents 282
11.3.1 Prednisolone and Dexamethasone 282
11.4 Adjuvent Enzymes 282
11.4.1 Chemophase™ 282
11.5 Other Therapies 283
11.5.1 Razoxane 283
Further Reading 283
Index 285 |
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| id | DE-604.BV022938818 |
| illustrated | Illustrated |
| index_date | 2024-07-02T18:57:32Z |
| indexdate | 2025-02-09T19:00:37Z |
| institution | BVB |
| isbn | 1420008900 0849392195 9780849392191 |
| language | English |
| lccn | 2006008937 |
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| physical | 290 S. Ill. 25 cm |
| publishDate | 2007 |
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| spelling | Thurston, David E. Verfasser aut Chemistry and pharmacology of anticancer drugs David E. Thurston Boca Raton CRC Press/Taylor & Francis 2007 290 S. Ill. 25 cm txt rdacontent n rdamedia nc rdacarrier Includes bibliographical references and index Anticancéreux Antineoplastic agents Antineoplastic Agents pharmacology Antineoplastic Agents chemistry Cytostatikum (DE-588)4068347-3 gnd rswk-swf Cytostatikum (DE-588)4068347-3 s DE-604 http://www.loc.gov/catdir/toc/ecip0610/2006008937.html Table of contents only http://www.loc.gov/catdir/enhancements/fy0654/2006008937-d.html Publisher description HBZ Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=016143516&sequence=000014&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Thurston, David E. Chemistry and pharmacology of anticancer drugs Anticancéreux Antineoplastic agents Antineoplastic Agents pharmacology Antineoplastic Agents chemistry Cytostatikum (DE-588)4068347-3 gnd |
| subject_GND | (DE-588)4068347-3 |
| title | Chemistry and pharmacology of anticancer drugs |
| title_auth | Chemistry and pharmacology of anticancer drugs |
| title_exact_search | Chemistry and pharmacology of anticancer drugs |
| title_exact_search_txtP | Chemistry and pharmacology of anticancer drugs |
| title_full | Chemistry and pharmacology of anticancer drugs David E. Thurston |
| title_fullStr | Chemistry and pharmacology of anticancer drugs David E. Thurston |
| title_full_unstemmed | Chemistry and pharmacology of anticancer drugs David E. Thurston |
| title_short | Chemistry and pharmacology of anticancer drugs |
| title_sort | chemistry and pharmacology of anticancer drugs |
| topic | Anticancéreux Antineoplastic agents Antineoplastic Agents pharmacology Antineoplastic Agents chemistry Cytostatikum (DE-588)4068347-3 gnd |
| topic_facet | Anticancéreux Antineoplastic agents Antineoplastic Agents pharmacology Antineoplastic Agents chemistry Cytostatikum |
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