Target Atlas of Apoptopic Drugs and Focus on Breast & Prostate

Table of Contents

• 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
  • 11.1.11 Hormone activity
  • 11.1.12 Hydrolase activity
  • 11.1.13 Intracellular ligand-gated ion channel activity
  • 11.1.14 Kinase activity
  • 11.1.15 Kinase regulator activity
  • 11.1.16 Ligase activity
  • 11.1.17 Lipid kinase activity
  • 11.1.18 Metallopeptidase activity
  • 11.1.19 Molecular function unknown
  • 11.1.20 Motor activity
  • 11.1.21 Oxidoreductase activity
  • 11.1.22 Peptide hormone
  • 11.1.23 Peroxidase activity
  • 11.1.24 Protein binding
  • 11.1.25 Protein serine/threonine kinase activity
  • 11.1.26 Protein threonine/tyrosine kinase activity
  • 11.1.27 Protein-tyrosine kinase activity
  • 11.1.28 Receptor activity
  • 11.1.29 Receptor binding
  • 11.1.30 Receptor signaling complex scaffold activity
  • 11.1.31 Receptor signaling protein serine/threonine kinase activity
  • 11.1.32 RNA binding
  • 11.1.33 Structural constituent of cytoskeleton
  • 11.1.34 Superoxide dismutase activity
  • 11.1.35 T cell receptor activity
  • 11.1.36 Transcription factor activity
  • 11.1.37 Transcription regulator activity
  • 11.1.38 Transferase activity
  • 11.1.39 Translation regulator activity
  • 11.1.40 Transmembrane receptor activity
  • 11.1.41 Transmembrane receptor protein tyrosine kinase activity
  • 11.1.42 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
  • 13.28 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 ........................................................................................... 202
• 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 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
• 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

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

List of Figures

• Box 37: Quick Facts - GVAX
• Box 38: Quick Facts - Exisulind
• Box 39: Quick Facts - Vapreotide
• Box 40: Quick Facts - DCVax

List of Figures

• Figure 1: Distribution of Compound Types Among Apoptopic Drugs
• Figure 2: Primary Sub-cellular Localization of Drug Targets