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Triple Analysis: The Drug Target Atlas of Apoptopic Drugs in Oncology and Special Focus on Breast and Prostate Cancer
Bioseeker, Feb 2008, Pages: 450
1 Executive Summary
2 Methodologies
3 Table of Contents
List of Tables
3.1 List of Boxes
3.2 List of Figures
4 Introduction to Apoptotic Drugs in Oncology
5 Apoptopic Drug Compound Types and Sub-cellular Localizations of Targets
6 The Cancer Genome Project and Apoptopic Drug Targets
6.1 Apoptopic Drug Targets Present in the Cancer Gene Census and in the Catalogue of Somatic Mutations in Cancer
7 Protein Expression Profiles of Apoptopic Drug Targets in Human
7.1 Expression in Normal Tissues and Cancer Tissues
7.2 Expression in Human Cancer Cell Lines and Primary Cells
8 Pathway Analysis of Drug Targets of Apoptopic Drugs
9 Protein-Protein Interactions Between Identified Apoptopic Drug Targets
10 Available Biological Structure Data on Apoptopic Drug Targets
11 Drug Target Profiles of Apoptopic Drug Targets in Oncology
11.1.1 Auxiliary transport protein activity
11.1.2 Carboxy-lyase activity
11.1.3 Catalytic activity
11.1.4 Cell adhesion molecule activity
11.1.5 Chaperone activity
11.1.6 Complement activity
11.1.7 Cysteine-type peptidase activity
11.1.8 Cytokine activity
11.1.9 DNA topoisomerase activity
11.1.10 Glutathione transferase activity
11.1.1.1 Hormone activity
11.1.1.2 Hydrolase activity
11.1.1.3 Intracellular ligand-gated ion channel activity
11.1.1.4 Kinase activity
11.1.1.5 Kinase regulator activity
11.1.1.6 Ligase activity
11.1.1.7 Lipid kinase activity
11.1.1.8 Metallopeptidase activity
11.1.1.9 Molecular function unknown
11.1.2.0 Motor activity
11.1.2.1 Oxidoreductase activity
11.1.2.2 Peptide hormone
11.1.2.3 Peroxidase activity
11.1.2.4 Protein binding
11.1.2.5 Protein serine/threonine kinase activity
11.1.2.6 Protein threonine/tyrosine kinase activity
11.1.2.7 Protein-tyrosine kinase activity
11.1.2.8 Receptor activity
11.1.2.9 Receptor binding
11.1.3.0 Receptor signaling complex scaffold activity
11.1.3.1 Receptor signaling protein serine/threonine kinase activity
11.1.3.2 RNA binding
11.1.3.3 Structural constituent of cytoskeleton
11.1.3.4 Superoxide dismutase activity
11.1.3.5 T cell receptor activity
11.1.3.6 Transcription factor activity
11.1.3.7 Transcription regulator activity
11.1.3.8 Transferase activity
11.1.3.9 Translation regulator activity
11.1.4.0 Transmembrane receptor activity
11.1.4.1 Transmembrane receptor protein tyrosine kinase activity
11.1.4.2 Transporter activity
12 Apoptopic Drug Target Mix by Development Stage
13 Apoptopic Drug Target Mix by Cancer Indication
13.1 Basal Cell Cancer
13.2 Biliary Cancer
13.3 Bladder Cancer
13.4 Bone Cancer
13.5 Brain Cancer
13.6 Breast Cancer
13.7 Carcinoid Tumor
13.8 Cervical Cancer
13.9 Chemotherapy-induced Neutropenia
13.10 Colorectal Cancer
13.11 Endometrial Cancer
13.12 Fallopian Tube Cancer
13.13 Gastrointestinal Cancer
13.13.1 Gastrointestinal Stomach Cancer
13.13.2 Gastrointestinal Stromal Cancer
13.14 Head and Neck Cancer
13.15 Leukemia
13.15.1 Acute Lymphocytic Leukemia
13.15.2 Acute Myelogenous Leukemia
13.15.3 Chronic Lymphocytic Leukemia
13.15.4 Chronic Myelogenous Leukemia
13.16 Liver Cancer
13.17 Lung Cancer
13.17.1 Non-Small Cell Lung Cancer
13.17.2 Small Cell Lung Cancer
13.18 Lymphoma
13.18.1 B-cell Lymphoma
13.18.2 Hodgkin's Lymphoma
13.18.3 non-Hodgkin's Lymphoma
13.18.4 T-cell Lymphoma
13.19 Melanoma
13.20 Mesothelioma
13.21 Myelodysplastic Syndrome
13.22 Myeloma
13.23 Nasopharyngeal Cancer
13.24 Oesophageal Cancer
13.25 Oral Cancer
13.26 Ovarian Cancer
13.27 Pancreatic Cancer
1328 Peritoneal Cancer
13.29 Prostate Cancer
13.30 Renal Cancer
13.31 Sarcoma
13.31.1 Leiomyo Sarcoma
13.32 Squamous Cell Cancer
13.33 Testicular Cancer
13.34 Thymoma Cancer
13.35 Thyroid Cancer
14 Apoptopic Drugs and their Targets by Companies
14.1 Australia
14.2 Canada
14.3 China
14.4 Denmark
14.5 Germany
14.6 Israel
14.7 Japan
14.8 South Korea
14.9 Spain
14.10 Switzerland
14.11 Taiwan
14.12 United Kingdom
14.13 USA
15 Breast Cancer: An Introduction
15.1 Disease Definitions
15.2 Etiology
15.3 Epidemiology
15.4 Prognosis
16 Current Treatment Strategies of Breast cancer
16.1 Localized Disease
16.2 Advanced Disease
17 Progress in Current Breast Cancer Treatment Strategies
17.1 Hormone Based Therapies
17.2 Antibodies
17.3 Chemotherapy
17.4 Chemotherapy
18 Key Therapeutic Strategies for Future Breast Cancer Therapies
18.1 Therapeutic Type, Targets & Mechanisms
19 Competitive Landscape in Breast Cancer Drug Development: The Late Stage Pipeline
19.1 The Epothilones
19.2 Cell Cycle & Apoptosis
19.3 Protein Kinase Inhibitors
19.4 Immunotherapy
20 Current Drug Development for Breast Cancer: The Early Stage Pipeline 20.1 DNA Targeting
20.2 FTIs
20.3 Antisense
20.4 New Hormone Modulators
20.5 Other
21 Prostate Cancer: An Introduction
21.1 Disease Definitions
21.2 Etiology & Pathophysiology
21.3 Epidemiology
21.4 Prognosis
22 Current Prostate Cancer Treatment Strategies
22.1 Localized Disease
22.1.1 Locally Advanced Prostate Cancer
22.2 Metastatic Prostate Cancer
22.2.1 Hormone-Sensitive Metastatic Prostate Cancer
22.2.2 Hormone-Refractory or Recurrent Metastatic Prostate Cancer
23 Progress in Current Prostate Cancer Treatment Strategies
23.1 Long-Term Follow-up Data not yet Been Published
23.2 Significant Reduced Risk of Distant Metastases
23.3 Adverse Events
23.4 No Difference in Overall Survival
23.5 Cross-over Design an Optimal Option?
23.6 Death due to Liver Failure
23.7 Survival Benefit
23.8 Subdermal Implant
23.9 No FDA Approval
23.10 No Improvement in 5-year Disease-Free Survival
23.11 Effective Secondary Hormonal Therapy?
23.12 Synery in Combination
24 Key Therapeutic Strategies for Future Prostate Cancer Therapies
24.1 Therapeutic Type, Targets & Mechanisms
25 Competitive Landscape in Prostate Cancer Drug Development: The Late Stage Pipeline
25.1 Reduced Prostate Cancer Risk
25.2 High Activity in Metastatic AIPC Patients
25.3 Absence of Severe Toxicities
25.4 Waiting for Data
25.5 Probability of Regulatory Approval?
25.6 Co-development and License Agreement
25.7 Improves Predicted Survival?
25.8 Slow Progress & Development Partners
25.9 Exclusive License Agreement
26 Current Prostate Cancer Drug Development: The Early Stage Pipeline
26.1 New Data?
26.2 Terminated Study
26.3 More Than 50% PSA decline
26.4 Safety and Tolerability
26.5 Terminated?
26.6 Marker of Drug Effect
26.7 Preliminary Results for a Tyrosine Kinase Inhibitor
26.8 No Activity in Monotherapy
26.9 Dramatic Disappearance of Bone Metastatic Lesions
26.10 PSA Response - Anthracycline
27 Disclaimer
28 Drug Index
29 Company Index
List of Tables
Table 1: Compound Type Versus Primary and Alternate Localization of Drug Target
Table 2: Drug Targets of Apoptopic Drugs Present in the Catalogue of Somatic Mutations in Cancer and in the Cancer Gene Census
Table 3: Available Protein Expression Profiles of Apoptopic Drug Targets
Table 4: Pathway Summary
Table 5: Drug Targets Without any Identified Assigned Pathways
Table 6: Pathway Profile According to BioCarta of the Drug Targets Belonging to Apoptopic Drugs
Table 7: Drug Targets Belonging to Apoptopic Pathways According to BioCarta
Table 8: Pathway Profile According to KEGG of the Drug Targets Belonging to Apoptopic Drugs
Table 9: Drug Targets within the Apoptosis Pathway According to KEGG
Table 10: Apoptopic Drugs Targeting Major Singaling Pathways
Table 11: Protein-Protein Interactions Between Identified Apoptopic Drug Targets
Table 12: Targets of Apoptopic Drugs without Protein-Protein Interaction with other Drug Targets
Table 13: Number of Available Biological Structures on Apoptopic Drug Targets
Table 14: Overview of Drug Target Profile Themes
Table 15: Fall Out in Terms of the Number of Drug Target Mixes, Drugs, and Developmental Projects by Developmental Stage
Table 16: Apoptopic Drug Target Mixes by Development
Table 17: Number of Unique Apoptopic Drug Target Mixes Reported by Cancer Indication
Table 18: Apoptopic Drug Target Mix for the Treatment of Basal Cell Cancer According to the Compound Type and Developmental Stage of Drug
Table 19: Apoptopic Drug Target Mix for the Treatment of Biliary Cancer According to the Compound Type and Developmental Stage of Drug
Table 20: Apoptopic Drug Target Mix for the Treatment of Bladder Cancer According to the Compound Type and Developmental Stage of Drug
Table 21: Apoptopic Drug Target Mix for the Treatment of Bone Cancer According to the Compound Type and Developmental Stage of Drug
Table 22: Apoptopic Drug Target Mix for the Treatment of Brain Cancer According to the Compound Type and Developmental Stage of Drug
Table 23: Apoptopic Drug Target Mix for the Treatment of Breast Cancer According to the Compound Type and Developmental Stage of Drug
Table 24: Apoptopic Drug Target Mix for the Treatment of Carcinoid Tumor According to the Compound Type and Developmental Stage of Drug
Table 25: Apoptopic Drug Target Mix for the Treatment of Cervical Cancer According to the Compound Type and Developmental Stage of Drug
Table 26: Apoptopic Drug Target Mix for the Treatment of Chemotherapy-induced Neutropenia According to the Compound Type and Developmental Stage of Drug
Table 27: Apoptopic Drug Target Mix for the Treatment of Colorectal Cancer According to the Compound Type and Developmental Stage of Drug
Table 28: Apoptopic Drug Target Mix for the Treatment of Endometrial Cancer According to the Compound Type and Developmental Stage of Drug
Table 29: Apoptopic Drug Target Mix for the Treatment of Fallopian Tube Cancer According to the Compound Type and Developmental Stage of Drug
Table 30: Apoptopic Drug Target Mix for the Treatment of Gastrointestinal Cancer According to the Compound Type and Developmental Stage of Drug
Table 31: Apoptopic Drug Target Mix for the Treatment of Gastrointestinal Stomach Cancer According to the Compound Type and Developmental Stage of Drug
Table 32: Apoptopic Drug Target Mix for the Treatment of Gastrointestinal Stromal Cancer According to the Compound Type and Developmental Stage of Drug
Table 33: Apoptopic Drug Target Mix for the Treatment of Head and Neck Cancer According to the Compound Type and Developmental Stage of Drug
Table 34: Apoptopic Drug Target Mix for the Treatment of Leukemia (general) According to the Compound Type and Developmental Stage of Drug
Table 35: Apoptopic Drug Target Mix for the Treatment of Acute Lymphocytic Leukemia According to the Compound Type and Developmental Stage of Drug
Table 36: Apoptopic Drug Target Mix for the Treatment of Acute Myelogenous Leukemia According to the Compound Type and Developmental Stage of Drug
Table 37: Apoptopic Drug Target Mix for the Treatment of Chronic Lymphocytic Leukemia According to the Compound Type and Developmental Stage of Drug
Table 38: Apoptopic Drug Target Mix for the Treatment of Chronic Myelogenous Leukemia According to the Compound Type and Developmental Stage of Drug
Table 39: Apoptopic Drug Target Mix for the Treatment of Liver Cancer According to the Compound Type and Developmental Stage of Drug
Table 40: Apoptopic Drug Target Mix for the Treatment of Lung Cancer (general) According to the Compound Type and Developmental Stage of Drug
Table 41: Apoptopic Drug Target Mix for the Treatment of Non-Small Cell Lung Cancer According to the Compound Type and Developmental Stage of Drug
Table 42: Apoptopic Drug Target Mix for the Treatment of Small Cell Lung Cancer According to the Compound Type and Developmental Stage of Drug
Table 43: Apoptopic Drug Target Mix for the Treatment of Lymphoma (general) According to the Compound Type and Developmental Stage of Drug
Table 44: Apoptopic Drug Target Mix for the Treatment of B-cell Lymphoma According to the Compound Type and Developmental Stage of Drug
Table 45: Apoptopic Drug Target Mix for the Treatment of Hodgkin’s Lymphoma According to the Compound Type and Developmental Stage of Drug
Table 46: Apoptopic Drug Target Mix for the Treatment of non-Hodgkin’s Lymphoma According to the Compound Type and Developmental Stage of Drug
Table 47: Apoptopic Drug Target Mix for the Treatment of T-cell Lymphoma According to the Compound Type and Developmental Stage of Drug
Table 48: Apoptopic Drug Target Mix for the Treatment of Melanoma According to the Compound Type and Developmental Stage of Drug
Table 49: Apoptopic Drug Target Mix for the Treatment of Mesothelioma According to the Compound Type and Developmental Stage of Drug
Table 50: Apoptopic Drug Target Mix for the Treatment of Myelodysplastic Syndrome According to the Compound Type and Developmental Stage of Drug
Table 51: Apoptopic Drug Target Mix for the Treatment of Myeloma According to the Compound Type and Developmental Stage of Drug
Table 52: Apoptopic Drug Target Mix for the Treatment of Nasopharyngeal Cancer According to the Compound Type and Developmental Stage of Drug
Table 53: Apoptopic Drug Target Mix for the Treatment of Oesophageal Cancer According to the Compound Type and Developmental Stage of Drug
Table 54: Apoptopic Drug Target Mix for the Treatment of Oral Cancer According to the Compound Type and Developmental Stage of Drug
Table 55: Apoptopic Drug Target Mix for the Treatment of Ovarian Cancer According to the Compound Type and Developmental Stage of Drug
Table 56: Apoptopic Drug Target Mix for the Treatment of Pancreatic Cancer According to the Compound Type and Developmental Stage of Drug
Table 57: Apoptopic Drug Target Mix for the Treatment of Peritoneal Cancer According to the Compound Type and Developmental Stage of Drug
Table 58: Apoptopic Drug Target Mix for the Treatment of Prostate Cancer According to the Compound Type and Developmental Stage of Drug
Table 59: Apoptopic Drug Target Mix for the Treatment of Renal Cancer According to the Compound Type and Developmental Stage of Drug
Table 60: Apoptopic Drug Target Mix for the Treatment of Sarcoma (general) According to the Compound Type and Developmental Stage of Drug
Table 61: Apoptopic Drug Target Mix for the Treatment of Leiomyo Sarcoma According to the Compound Type and Developmental Stage of Drug
Table 62: Apoptopic Drug Target Mix for the Treatment of Squamous Cell Cancer According to the Compound Type and Developmental Stage of Drug
Table 63: Apoptopic Drug Target Mix for the Treatment of Testiculat Cancer According to the Compound Type and Developmental Stage of Drug
Table 64: Apoptopic Drug Target Mix for the Treatment of Thymoma Cancer According to the Compound Type and Developmental Stage of Drug
Table 65: Apoptopic Drug Target Mix for the Treatment of Thyroid Cancer According to the Compound Type and Developmental Stage of Drug
Table 66: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Australia
Table 67: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Canada
Table 68: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in China
Table 69: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Denmark
Table 70: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Germany
Table 71: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Israel
Table 72: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Japan
Table 73: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in South Korea 242
Table 74: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Spain
Table 75: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Switzerland
Table 76: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Taiwan
Table 77: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in United Kingdom
Table 78: Apoptopic Drugs with Target Mix and Developmental Projects by Company in USA
Table 64: The Stage System
Table 65: Risk Factors
Table 66: List of Approved Drugs and Their Mechanisms of Action
Table 67: Hormonal Treatment Strategies
Table 68: Adjuvant Systemic Treatment Options for Women With Axillary Node-Negative Breast Cancer
Table 69: Treatment Options for Women With Axillary Node-Positive Breast Cancer
Table 70: Chemotherapy Drugs and Regimen
Table 71: Summay of Drugs Involved in Breast Cancer Therapy
Table 72: Short Facts Tamoxifen
Table 73: Short Facts Anastrozole
Table 74: Short Facts Letrozole
Table 75: Short Facts Exemestane
Table 76: Short Facts Goserelin
Table 77: Short Facts Fulvestrant
Table 78: Short Facts Trastuzumab
Table 79 Cancer Immunotherapy Strategies
Table 80: Progress on Ixabepilone
Table 81: Progress on CCI-779
Table 82: Progress on Fenretinide
Table 83: Progress on Lapatinib
Table 84: Progress on Bevacizumab
Table 85: Progress on Theratope
Table 86: Summary of Mid-Stage to Late stage Investigational Agents Under Development
Table 87: Summary of Breast Cancer Early Stage Pipeline
Table 88: The TNM System
Table 89: Lifestyle factors
Table 90: Historical Summary of Clinical Studies on Patients with Late Stage Disease
Table 91: Short Facts Abarelix
Table 92: Short Facts Bicalutamide
Table 93: Short Facts Carboplatin
Table 94: Short Facts Docetaxel
Table 95: Short Facts Mitoxantrone
Table 96: Short Facts Flutamide
Table 97: Short Facts Goserelin
Table 98: Short Facts Histrelin
Table 99: Short Facts Lanreotide
Table 100: Short Facts Leuprolide
Table 101: Short Facts Nilutamide
Table 102: Short Facts Estramustine
Table 103: Summary of Recent Clinical Studies on Patients with Late Stage Disease
Table 104: Ongoing Late Stage Clinical Studies
Table 105: Cancer Immunotherapy Strategies
Table 106: Near Term Progress Toremifene
Table 107: Near Term Progress Bevacizumab
Table 108: Near Term Progress Oblimersen
Table 109: Near Term Progress R-flurbiprofen
Table 110: Near Term Progress APC8015
Table 111: Near Term Progress Satraplatin
Table 112: Near Term Progress GVAX
Table 113: Near Term Progress Exisulind
Table 114: Summary of Prostate Cancer Late Stage Pipeline
Table 115: Paclitaxel
Table 116: Epothilone
Table 117: Ixabepilone
Table 118: PTK/ZK
Table 119: Arsenic trioxide
Table 120: Retinoic Acid
Table 121: Imatinib
Table 122: Bortezomib
Table 123: Sorafenib
Table 124: Doxorubicin
Table 125: Summary of Prostate Cancer Early Stage Pipeline
31 List of Boxes
Box 1: Ongoing Phase III Studies Anastrozole
Box 2: Ongoing Phase III Studies Letrozole
Box 3: Ongoing Phase III Studies Exemestane
Box 4: Ongoing Phase III Studies Goserelin
Box 5: Ongoing Phase III Studies Fulvestrant
Box 6: Ongoing Phase III Studies Trastuzumab
Box 7: The TRAIL Receptor family
Box 8: The Bcl-2 family of proteins
Box 9: Quick Facts - BMS-247550
Box 10: Quick Facts - Temsirolimus
Box 11: Quick Facts - SDX-105
Box 12: Quick Facts - 4HPR
Box 13: Quick Facts - Lapatinib
Box 14: Quick Facts - Bevacizumab
Box 15: Quick Facts - Theratope
Box 16: Erlotinib
Box 17: Gefitinib
Box 18: Imatinib
Box 19: Pemetrexed
Box 20: NX473
Box 21: Lonafarnib
Box 22: Tipifarnib
Box 23: Bortezomib
Box 24: Arzoxifene
Box 25: Patupilone
Box 26: KOS-862
Box 27: Southwest Oncology Group Study 99-16 Design
Box 28: TAX 327 Study Design
Box 29: The TRAIL Receptor family
Box 30: The Bcl-2 family of proteins
Box 31: Quick Facts - Toremifene
Box 32: Quick Facts - Bevacizumab
Box 33: Quick Facts - Genasense
Box 34: Quick Facts - R-flurbiprofen
Box 35: Quick Facts - Provenge
Box 36: Quick Facts - Satraplatin
Box 37: Quick Facts - GVAX
Box 38: Quick Facts - Exisulind
Box 39: Quick Facts - Vapreotide
Box 40: Quick Facts - DCVax
32 List of Figures
Figure 1: Distribution of Compound Types Among Apoptopic Drugs
Figure 2: Primary Sub-cellular Localization of Drug Targets
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