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Antibody Drug Target Atlas in Oncology

Published by: BioSeeker Group AB

Published: Jun. 12, 2007 - 172 Pages


Table of Contents


1 Executive Summary

2 About Cancer Highlights

3 Methodologies

4 Table of Contents

4.1 List of Figures

4.2 List of Tables

5 Antibody Drug Target Analysis in Oncology: What and Where Are We Targeting? __ 19

6 Antibody Drug Targets by Molecular Function

6.1 Carboxypeptidase Activity Targets

6.2 Catalytic Activity Targets

6.3 Cell Adhesion Molecule Activity Targets

6.4 Chaperone Activity Targets

6.5 Chemokine Activity Targets

6.6 Cofactor Binding Targets

6.7 Complement Activity Targets

6.8 Cytokine Activity Targets

6.9 DNA Topoisomerase Activity Targets

6.10 Extracellular Matrix Structural Constituent Targets

6.11 G-protein Coupled Receptor Activity Targets

6.12 Growth Factor Activity Targets

6.13 Hormone Activity Targets

6.14 Hydrolase Activity Targets

6.15 Intracellular Ligand-gated Ion Channel Activity Targets

6.16 Metallopeptidase Activity Targets

6.17 MHC Class I Receptor Activity Targets

6.18 Molecular Function Unknown Targets

6.19 Oxidoreductase Activity Targets

6.20 Peptide Hormone Targets

6.21 Protease Inhibitor Activity Targets

6.22 Protein Binding Targets

6.23 Receptor Activity Targets

6.24 Receptor Binding Targets

6.25 Receptor Signaling Complex Scaffold Activity Targets

6.26 Receptor Signaling Protein Tyrosine Phosphatase Activity Targets

6.27 RNA-directed DNA polymerase Activity Targets

6.28 Serine-type Peptidase Activity Targets

6.29 T Cell Receptor Activity Targets

6.30 Translation Regulator Activity Targets

6.31 Transmembrane Receptor Activity Targets

6.32 Transmembrane Receptor Protein Tyrosine Kinase Activity Targets

6.33 Transporter Activity Targets

6.34 Unclassified Targets

7 Antibody Drugs Targeting Signaling Pathways

7.1 Alpha6 Beta4 Integrin Signaling Pathway

7.1.1 Description of Pathway

7.1.2 Antibody Drugs by Target, Developmental Stage, and Cancer Type

7.2 Androgen Receptor Signaling Pathway

7.2.1 Description of Pathway

7.2.2 Antibody Drugs by Target, Developmental Stage, and Cancer Type

7.3 B Cell Receptor Signaling Pathway

7.3.1 Description of Pathway

7.3.2 Antibody Drugs by Target, Developmental Stage and Cancer Type

7.4 EGFR1 Signaling Pathway

7.4.1 Description of Pathway

7.4.2 Antibody Drugs by Target, Developmental Stage, and Cancer Type

7.5 IL-2 Signaling Pathway

7.5.1 Description of Pathway

7.5.2 Antibody Drugs by Target, Developmental Stage and Cancer Type

7.6 IL-4 Signaling Pathway

7.6.1 Description of Pathway

7.6.2 Antibody Drugs by Target, Developmental Stage and Cancer Type

7.7 IL-6 Signaling Pathway

7.7.1 Description of Pathway

7.7.2 Antibody Drugs by Target, Developmental Stage, and Cancer Type

7.8 Kit Receptor Signaling Pathway

7.8.1 Description of Pathway

7.8.2 Antibody Drugs by Target, Developmental Stage, and Cancer Type

7.9 Notch Signaling Pathway

7.9.1 Description of Pathway

7.9.2 Antibody Drugs by Target, Developmental Stage, and Cancer Type

7.10 T Cell Receptor Signaling Pathway

7.10.1 Description of Pathway

7.10.2 Antibody Drugs by Target, Developmental Stage, and Cancer Type

7.11 TGF-beta Receptor Signaling Pathway

7.11.1 Description of Pathway

7.11.2 Antibody Drugs byTarget, Developmental Stage, and Cancer Type

7.12 TNF-alpha Signaling Pathway

7.12.1 Description of Pathway

7.12.2 Antibody Drugs by Target, Developmental Stage, and Cancer Type

7.13 Wnt Signaling Pathway

7.13.1 Description of Pathway

7.13.2 Antibody Drugs by Target, Developmental Stage, and Cancer Type

8 Antibodies Targeting Cancer Stem Cells

9 Targets of Antibody Conjugates

10 Antibody Drug Targets by Three Major Non Immunological Therapeutic Effects

10.1 Anti-Angiogenesis

10.2 Apoptosis

10.3 Protein Kinase Inhibitors

11 Antibody Targets and Drugs by Cancer Indications

11.1 Basal Cell Cancer

11.2 Biliary Cancer

11.3 Bladder Cancer

11.4 Bone Cancer

11.5 Brain Cancer

11.6 Breast Cancer

11.7 Cervical Cancer

11.8 Cervical Dysplasia

11.9 Colorectal Cancer

11.10 Endometrial Cancer

11.11 Esophageal Cancer

11.12 Fallopian Tube Cancer

11.13 Gastrointestinal Cancers

11.14 Head and Neck Cancer

11.15 Leukemias

11.16 Liver Cancer

11.17 Lung Cancers

11.18 Lymphomas

11.19 Melanoma

11.20 Mesothelioma

11.21 Myelodysplastic syndrome

11.22 Myelomas

11.23 Nasopharyngeal Cancer

11.24 Oesophageal Cancer

11.25 Ovarian Cancer

11.26 Pancreatic Cancer

11.27 Peritoneal Cancer

11.28 Prostate Cancer

11.29 Renal Cancers

11.30 Sarcomas

11.31 Thyroid Cancer

12 Expression Profiles of Antibody Drug Targets

12.1 Human Tissues and Cancer Tissues

12.2 Cancer Lines and Cells

13 Disclaimer

14 Drug Index

15 Company Index

16 Appendix I: Antibody Targets by Companies


4.1 List of Figures

Figure 1: Antibody Pipeline Maturity by Molecular Function Classes of Targets 1(3)

Figure 2: Antibody Pipeline Maturity by Molecular Function Classes of Targets 2(3)

Figure 3: Antibdody Pipeline Maturity by Molecular Function Classes of Targets 3(3)

Figure 4: Pipeline Maturation of Carboxypeptidase Activity Targets

Figure 5: Number of Antibody Drugs per Cancer Indication and Carboxypeptidase Activity Target

Figure 6: Pipeline Maturation of Catalytic Activity Targets

Figure 7: Number of Antibody Drugs per Cancer Indication and Catalytic Activity Target

Figure 8: Pipeline Maturation of Cell Adhesion Molecule Activity Targets

Figure 9: Number of Antibody Drugs per Cancer Indication and Cell Adhesion Molecule Activity Target

Figure 10: Pipeline Maturation of Chaperone Activity Targets

Figure 11: Number of Antibody Drugs per Cancer Indication and Chaperone Activity Target

Figure 12: Pipeline Maturation of Chemokine Activity Targets

Figure 13: Number of Antibody Drugs per Cancer Indication and Chemokine Activity Target

Figure 14: Pipeline Maturation of Cofactor Binding Targets

Figure 15: Number of Antibody Drugs per Cancer Indication and Cofactor Binding Target

Figure 16: Pipeline Maturation of Complement Activity Targets

Figure 17: Number of Antibody Drugs per Cancer Indication and Complement Activity Target

Figure 18: Pipeline Maturation of Cytokine Activity Targets

Figure 19: Number of Antibody Drugs per Cancer Indication and Cytokine Activity Target

Figure 20: Pipeline Maturation of DNA Topoisomerase Activity Targets

Figure 21: Number of Antibody Drugs per Cancer Indication and DNA Topoisomerase Activity Target

Figure 22: Pipeline Maturation of Extracellular Matrix Structural Constituent Targets

Figure 23: Number of Antibody Drugs per Cancer Indication and Extracellular Matrix Structural Constituent

Target
Figure 24: Pipeline Maturation of G-protein Coupled Receptor Activity Targets

Figure 25: Number of Antibody Drugs per Cancer Indication and Extracellular G-protein Coupled Receptor Activity Target

Figure 26: Pipeline Maturation of Growth Factor Activity Targets

Figure 27: Number of Antibody Drugs per Cancer Indication and Extracellular Growth Factor Activity Target

Figure 28: Pipeline Maturation of Hormone Activity Targets

Figure 29: Number of Antibody Drugs per Cancer Indication and Hormone Activity Target

Figure 30: Pipeline Maturation of Hydrolase Activity Targets

Figure 31: Number of Antibody Drugs per Cancer Indication and Hydrolase Activity Target

Figure 32: Pipeline Maturation of Ligand-gated Ion Channel Activity Targets

Figure 33: Number of Antibody Drugs per Cancer Indication and Intracellular Ligand-gated Ion Channel Activity Target

Figure 34: Pipeline Maturation of Metallopeptidase Activity Targets

Figure 35: Number of Antibody Drugs per Cancer Indication and Intracellular Metallopeptidase Activity Target51

Figure 36: Pipeline Maturation of MHC Class I Receptor Activity Targets

Figure 37: Number of Antibody Drugs per Cancer Indication and MHC Class I Receptor Activity Target

Figure 38: Pipeline Maturation of Molecular Function Unknown Targets

Figure 39: Number of Antibody Drugs per Cancer Indication and Molecular Function Unknown Target

Figure 40: Pipeline Maturation of Oxidoreductase Activity Targets

Figure 41: Number of Antibody Drugs per Cancer Indication and Oxidoreductase Activity Target

Figure 42: Pipeline Maturation of Peptide Hormone Targets

Figure 43: Number of Antibody Drugs per Cancer Indication and Peptide Hormone Target

Figure 44: Pipeline Maturation of Protease inhibitor Activity Targets

Figure 45: Number of Antibody Drugs per Cancer Indication and Protease Inhibitor Activity Target

Figure 46: Pipeline Maturationof Protein Binding Targets

Figure 47: Number of Antibody Drugs per Cancer Indication and Protein Binding Target

Figure 48: Pipeline Maturation of Receptor Activity Targets 1 (2)

Figure 49: Number of Antibody Drugs per Cancer Indication and Receptor Activity Target 1(2)

Figure 50: Pipeline Maturation of Receptor Activity Targets 2 (2)

Figure 51: Number of Antibody Drugs per Cancer Indication and Receptor Activity Target 2(2)

Figure 52: Pipeline Maturationof Receptor Binding Targets

Figure 53: Number of Antibody Drugs per Cancer Indication and Receptor Binding Target

Figure 54: Pipeline Maturation of Receptor Signaling Complex Scaffold Activity Targets

Figure 55: Number of Antibody Drugs per Cancer Indication and Receptor Signaling Complex Scaffold Activity Target

Figure 56: Pipeline Maturation of by Receptor Signaling Protein Tyrosine Phosphatase Activity Targets

Figure 57: Number of Antibody Drugs per Cancer Indication and Receptor Signaling Protein Tyrosine Phosphatase Activity Target

Figure 58: Pipeline Maturation of RNA-directed DNA polymerase Activity Targets

Figure 59: Number of Antibody Drugs per Cancer Indication and RNA-directed DNA polymerase Activity Target

Figure 60: Pipeline Maturation of Serine-type Peptidase Activity Targets

Figure 61: Number of Antibody Drugs per Cancer Indication and RNA Serine-type Peptidase Activity Target

Figure 62: Pipeline Maturation of T cell Receptor Activity Targets

Figure 63: Number of Antibody Drugs per Cancer Indication and T cell Receptor Activity Target

Figure 64: Pipeline Maturation of Translation Regulator Activity Targets

Figure 65: Number of Antibody Drugs per Cancer Indication and Translation Regulator Activity Target

Figure 66: Pipeline Maturation of Transmembrane Receptor Activity Targets

Figure 67: Number of Antibody Drugs per Cancer Indication and Transmembrane Receptor Activity Target

Figure 68: Pipeline Maturation of Transmembrane Receptor Protein Tyrosine Kinase Activity Targets

Figure 69: Number of Antibody Drugs per Cancer Indication and Transmembrane Receptor Protein Tyrosine Kinase Activity Target

Figure 70: Pipeline Maturation of Transporter Activity Targets

Figure 71: Number of Antibody Drugs per Cancer Indication and Transporter Activity Target

Figure 72: Pipeline Maturation of Unclassified Targets

Figure 73: Number of Antibody Drugs per Cancer Indication and Unclassified Target

Figure 74: Antibody Pipeline Comparison of Targeted Signaling Pathways in Oncology

Figure 75: Pipeline Maturation of Immunoconjugated Antibody Targets

Figure 76: Number of Immunoconjugated Antibody Drugs per Cancer Indication and Target




4.2 List of Tables

Table 1: Molecular Functions versus Oncology Antibody Drug Targets

Table 2: Cancer Antibody Pipeline Listed by Carboxypeptidase Activity Targets

Table 3: Cancer Antibody Pipeline Listed by Catalytic Activity Targets

Table 4: Cancer Antibody Pipeline Listed by Cell Adhesion Molecule Activity Targets

Table 5: Cancer Antibody Pipeline Listed by Chaperone Activity Targets

Table 6: Cancer Antibody Pipeline Listed by Chemokine Activity Targets

Table 7: Cancer Antibody Pipeline Listed by Cofactor Binding Targets

Table 8: Cancer Antibody Pipeline Listed by Complement Activity Targets

Table 9: Cancer Antibody Pipeline Listed by Cytokine Activity Targets

Table 10: Cancer Antibody Pipeline Listed by DNA Topoisomerase Activity Targets

Table 11: Cancer Antibody Pipeline Listed by Extracellular Matrix Structural Constituent Targets

Table 12: Cancer Antibody Pipeline Listed by G-protein Coupled Receptor Activity Targets

Table 13: Cancer Antibody Pipeline Listed by Growth Factor Activity Targets

Table 14: Cancer Antibody Pipeline Listed by Hormone Activity Targets

Table 15: Cancer Antibody Pipeline Listed by Hydrolase Activity Targets

Table 16: Cancer Antibody Pipeline Listed by Intracellular Ligand-gated Ion Channel Activity Targets

Table 17: Cancer Antibody Pipeline Listed by Metallopeptidase Activity Targets

Table 18: Cancer Antibody Pipeline Listed by MHC Class I Receptor Activity Targets

Table 19: Cancer Antibody Pipeline Listed by Molecular Function Unknown Targets

Table 20: Cancer Antibody Pipeline Listed by Oxidoreductase Activity Targets

Table 21: Cancer Antibody Pipeline Listed by Peptide Hormone Targets

Table 22: Cancer Antibody Pipeline Listed by Protease inhibitor Activity Targets

Table 23: Cancer Antibody Pipeline Listed by Protein Binding Targets

Table 24: Cancer Antibody Pipeline Listed by Receptor Activity Targets

Table 25: Cancer Antibody Pipeline Listed by Receptor Binding Targets

Table 26: Cancer Antibody Pipeline Listed by Receptor Signaling Complex Scaffold Activity Targets

Table 27: Cancer Antibody Pipeline Listed by Receptor Signaling Protein Tyrosine Phosphatase Activity Targets74

Table 28: Cancer Antibody Pipeline Listed by RNA-directed DNA polymerase Activity Targets

Table 29: Cancer Antibody Pipeline Listed by Serine-type Peptidase Activity Targets

Table 30: Cancer Antibody Pipeline Listed by T cell Receptor Activity Targets

Table 31: Cancer Antibody Pipeline Listed by Translation Regulator Activity Targets

Table 32: Cancer Antibody Pipeline Listed by Transmembrane Receptor Activity Targets

Table 33: Cancer Antibody Pipeline Listed by Transmembrane Receptor Protein Tyrosine Kinase Activity Targets

Table 34: Cancer Antibody Pipeline Listed by Transporter Activity Targets

Table 35: Cancer Antibody Pipeline Listed by Unclassified Targets

Table 36: Antibody Drugs Targeting Signaling Pathways

Table 37: Signaling Pathway Analysis of Oncology Antibody Drug Targets

Table 38: Targets Linking Antibody Drugs to the Alpha6 Beta4 Integrin Signaling Pathway

Table 39: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the Alpha6 Beta4 Integrin Signaling Pathway

Table 40: Targets Linking Antibody Drugs to the Androgen Receptor Signaling Pathway

Table 41: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the Androgen Receptor Signaling Pathway

Table 42: Targets Linking Antibody Drugs to the B Cell Receptor Signaling Pathway

Table 43: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the B Cell Receptor Signaling Pathway

Table 44: Targets Linking Antibody Drugs to the EGFR1 Signaling Pathway

Table 45: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the EGFR1 Signaling Pathway

Table 46: Targets Linking Antibody Drugs to the IL-2 Signaling Pathway

Table 47: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the IL-2 Signaling Pathway

Table 48: Targets Linking Antibody Drugs to the IL-4 Signaling Pathway

Table 49: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the IL-4 Signaling Pathway

Table 50: Targets Linking Antibody Drugs to the IL-6 Signaling Pathway

Table 51: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the IL-6 Signaling Pathway

Table 52: Targets Linking Antibody Drugs to the Kit Receptor Signaling Pathway

Table 53: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the Kit Receptor Signaling Pathway

Table 54: Targets Linking Antibody Drugs to the Notch Signaling Pathway

Table 55: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the Notch Signaling Pathway

Table 56: Targets Linking Antibody Drugs to the T Cell Receptor Signaling Pathway

Table 57: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the T Cell Receptor Signaling Pathway

Table 58: Targets Linking Antibody Drugs to the TGF-beta Receptor Signaling Pathway

Table 59: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the TGF-beta Receptor Signaling Pathway

Table 60: Targets Linking Antibody Drugs to the TNF-alpha Signaling Pathway

Table 61: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the TNF-alpha Signaling Pathway

Table 62: Targets Linking Antibody Drugs to the Wnt Signaling Pathway

Table 63: Antibodies, Listed by Investigator, Developmental Stage, and Cancer Type, Targeting the Wnt Signaling Pathway

Table 64: Cell Surface Markers of Identified Cancer Stem Cells in Human Tumors

Table 65: Signaling Pathways Involved in Stem Cell Self-Renewal

Table 66: Immunoconjugated Antibody Targets According to Molecular Function of Target

Table 67: Immunoconjugated Antibody Pipeline According to Target

Table 68: Antibodies in Oncology Reported to Affect Angiogenesis

Table 69 Antibodies in Oncology Reported to Affect Apoptosis

Table 70: Antibody Drug Protein Kinase Targets Ranked by Probability of Carrying at Least One Driver Mutation, Conditional on the Gene-Specific Selection Pressures

Table 71: Antibodies in Oncology Reported to Act as Protein Kinase Inhibitors

Table 72: Cancer Indicaions by Number of Known Antibody Targets, Number of Antibody Drugs, and Highest Developmental Stage

Table 73: Antibody Pipeline by Targets in Basal Cell Cancer

Table 74: Antibody Pipeline by Targets in Biliary Cancer

Table 75: Antibody Pipeline by Targets in Bladder Cancer

Table 76: Antibody Pipeline by Targets in Bone Cancer

Table 77: Antibody Pipeline by Targets in Brain Cancer

Table 78: Antibody Pipeline by Targets in Breast Cancer

Table 79: Antibody Pipeline by Targets in Cervical Cancer

Table 80: Antibody Pipeline by Targets in Cervical Dysplasia

Table 81: Antibody Pipeline by Targets in Colorectal Cancer

Table 82: Antibody Pipeline by Targets in Endometrial Cancer

Table 83: Antibody Pipeline by Targets in Esophageal Cancer

Table 84: Antibody Pipeline by Targets in Fallopian Tube Cancer

Table 85: Antibody Pipeline by Targets in Gastrointestinal Cancers

Table 86: Antibody Pipeline by Targets in Head and Neck Cancer

Table 87: Antibody Pipeline by Targets in Leukemias

Table 88: Antibody Pipeline by Targets in Liver Cancer

Table 89: Antibody Pipeline by Targets in Lung Cancers

Table 90: Antibody Pipeline by Targets in Lymphomas

Table 91: Antibody Pipeline by Targets in Melanoma

Table 92: Antibody Pipeline by Targets in Mesothelioma

Table 93: Antibody Pipeline by Targets in Myelodysplastic syndrome

Table 94: Antibody Pipeline by Targets in Myelomas

Table 95: Antibody Pipeline by Targets in Nasopharyngeal Cancer

Table 96: Antibody Pipeline by Targets in Oesophageal Cancer

Table 97: Antibody Pipeline by Targets in Ovarian Cancer

Table 98: Antibody Pipeline by Targets in Pancreatic Cancer

Table 99: Antibody Pipeline by Targets in Peritoneal Cancer

Table 100: Antibody Pipeline by Targets in Prostate Cancer

Table 101: Antibody Pipeline by Targets in Renal Cancers

Table 102: Antibody Pipeline by Targets in Sarcomas

Table 103: Antibody Pipeline by Targets in Thyroid Cancer

Table 104: Expression Profiles of Antibody Drug Targets in Oncology

Abstract

The elaborate advances towards the blueprinting of the altered molecular networks that lie behind cancer development have paved the way for targeted therapy in cancer. There are currently more than 400 antibody based drugs in development for the treatment of cancer. What and where they are targeting has to date only been a fragmented knowledge. First in place, BioSeeker has surveyed these antibodies and identified 132 antibody drug targets, belonging to 220 antibody drugs. In all they range from preclinical development to established therapy leaders in the market place. Drug targets and their associated antibodies have been analyzed by BioSeeker according to:
  • 34 Different molecular functions of target
  • 13 Major signaling pathways
  • Cancer stem cells
  • Conjugated antibodies
  • Therapeutic effects: Anti-angiogenesis, Apoptosis and Protein Kinase Inhibition
  • 31 Targeted cancer indications
  • Availability of expression profiles of targets in human tissues, cancer tissues, established cell lines and primary cell cultures
  • Antibody therapeutic companies
  • Single target analysis of the 132 antibody targets is performed, including targeted cancer indications, antibody drugs involved and their developmental stages. In total more than 420 clinical trials are included in this analysis, covering more than 30 different cancer indications plus diagnosis and supportive care.
This report serves as a serious reference for professionals interested in the development of oncology drug targets and selection/validation of targeting strategies.

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