Drug Targets for Breast Cancer

Table of Contents

• Breast Cancer Therapeutics
• Breast Cancer Technologies
• Breast Cancer Markets
• The Future and Breast Cancer

• Epidemiology
• Breast Cancer Types and Stages
• Causes and Risk Factors
• Biomarkers and Diagnostics
• Awareness and Education
• Treatment Strategies
• Objectives and Scope

• Estrogen and the Estrogen Receptor
  • Normal Estrogen Function
  • The Estrogen Receptor
• Estrogen, The Estrogen Receptor, and Breast Cancer
  • Estrogen and Breast Cancer
  • The Estrogen Receptor and Breast Cancer
• Categories of Endocrine Therapy
  • Selective Estrogen Receptor Modulators (SERMs)
    • Mode of Action of SERMs
    • Approved SERMs
    • Emerging SERMs
      • Raloxifene
      • Arzoxifene
      • Lasofoxifene
• Selective Estrogen Receptor Downregulators (SERDs)
  • Mode of Action of SERDs
  • Approved SERDs
• Aromatase Inhibitors
  • Mode of Action of Aromatase Inhibitors
  • Approved Aromatase Inhibitors
  • Emerging Aromatase Inhibitors
• LHRH Agonists
  • Mode of Action of LHRH Agonists
  • Approved LHRH Agonists

• Targeting Growth Factors
  • The erbB Receptor Family
    • erbB1/EGFR
    • erbB2/EGFR2/HER2
  • Targeting Growth Factors (IGF)
• Targeting Angiogenesis
  • Vascular Endothelial Growth Factor (VEGF)
• Targeting Farnesylation
• Targeting the MEK Pathway
• Targeting the mTOR Pathway
• Targeting Apoptosis
• Targeting DNA Synthesis and Repair
• Targeting the Proteasome

• Cancer Vaccines and Breast Cancer
  • Current Approaches in Cancer Vaccine Development
• Approved and Emerging Cancer Vaccines
  • Approved Cancer Vaccines
  • Emerging Breast Cancer Vaccines
• Adjuvants
• Approved and Emerging Monoclonal Antibodies
  • Categories of Monoclonal Antibodies
    • Naked Monoclonal Antibodies
    • Conjugated Monoclonal Antibodies
  • Approved and Emerging Monoclonal Antibodies
    • Approved Monoclonal Antibodies
    • Emerging Monoclonal Antibodies

• Historical Timeline
• Chemotherapy Categorization
  • Antimetabolites
  • Mitotic Inhibitors
  • Alkylating Agents
  • Anthracyclines
  • Topoisomerase II Inhibitors
• Approved Chemotherapy Drugs for Breast Cancer
• Emerging Chemotherapy Drugs for Breast Cancer
• Combination Chemotherapy

• Gene Cloning and Characterization
• Gene Expression Profiling
• Proteomics
• RNAi
• Bioinformatics
• Population Genetics
• Biomarkers
• Diagnostics and Prognosis

• Endocrine Therapies
  • Selective Estrogen Receptor Modulators (SERMs)
  • Selective Estrogen Receptor Downregulators (SERDs)
  • Aromatase Inhibitors
    • Arimidex®
    • Femara®
    • Aromasin®
  • Luteinizing Hormone-Releasing Hormone Analogs (LHRH Analogs)
• Innovative Therapies
• Immunotherapies
• The Chemotherapy Market

• Therapeutic Potential
• Market Potential
• Breast Cancer Treatment and The Future
• Breast Cancer and The Patient
• Summary

• James D. Winkler, Ph.D., Senior Director, Discovery Biology, Array BioPharma
• Dr. George Blackledge, Senior Oncology Physician, AstraZeneca
• Dr. Rene Bernards, Chief Scientific Officer, Agendia
• Dr. Thomas J. Schuetz, Chief Medical Officer and Senior VP of Medical Affairs,
• Therion Biologics

• Aeterna Zentaris Inc
• Agendia BV
• American Pharmaceutical Partners, Inc
• Array BioPharma Inc.
• AstraZeneca plc
• Bristol Myers Squibb
• Dendreon Corporation
• Eli Lilly and Company
• Genentech, Inc
• Genta, Inc.
• Igeneon
• Novartis AG
• Sanofi-aventis
• Therion Biologics Corporation
• ViRexx Medical Corp.

• Exhibit 2.1 Risk Factors Associated with Breast Cancer
• Exhibit 2.2 Examples of Sub-groups of Breast Cancer Patients
• Exhibit 2.3 Pink Breast Cancer Ribbon
• Exhibit 3.1 Illustration of Estrogen Action
• Exhibit 3.2 Tissue Distribution of Estrogen Receptor ƒ¿ and ƒÀ
• Exhibit 3.3 Key Classes of Endocrine Therapy for Breast Cancer
• Exhibit 3.4 The Dual Role of SERMs on Breast and Uterine Tissue
• Exhibit 3.5 Approved SERMs for Breast Cancer Treatment
• Exhibit 3.6 Characteristics of the Ideal SERM
• Exhibit 3.7 Emerging SERMs
• Exhibit 3.8 Approved SERDs
• Exhibit 3.9 Approved Aromatase Inhibitors
• Exhibit 3.10 Emerging Aromatase Inhibitors
• Exhibit 3.11 Mode of Action of ZoladexR
• Exhibit 3.12 Approved LHRH Agonists
• Exhibit 4.1 Illustration of the Four erbB (EGFR) Receptor Sub-types
• Exhibit 4.2 Emerging Therapeutics Targeting erb1 (EGFR)
• Exhibit 4.3 Approved Therapeutics Targeting erbB2 (Her2/EGFR2/neu)
• Exhibit 4.4 Emerging Therapeutics Targeting erbB2 (and multiple erbBs)
• Exhibit 4.5 Emerging Therapeutics Targeting Angiogenesis
• Exhibit 4.6 Emerging Therapeutics Targeting Farnesyl Transferases
• Exhibit 4.7 Emerging Therapeutics Targeting the MEK Pathway
• Exhibit 4.8 Emerging Therapeutics Targeting the mTOR Pathway
• Exhibit 4.9 RAD001 Effects on Tumor and Vascular Cells
• Exhibit 4.10 Emerging Therapeutics Targeting Apoptosis
• Exhibit 4.11 Emerging Therapeutics Targeting DNA Synthesis and Repair
• Exhibit 4.12 Emerging Therapeutics Targeting the Proteasome
• Exhibit 5.1 Breast Cancer Vaccines in Clinical Development
• Exhibit 5.2 Mechanism of Action of Therion' s Cancer Vaccines
• Exhibit 5.3 Mechanism of Action of Dendreon' s Therapeutic Vaccines
• Exhibit 5.4 Adjuvants for Cancer Vaccines in Clinical Development
• Exhibit 5.5 Approved Non-conjugated Monoclonal Antibodies
• Exhibit 5.6 FDA-Approved Monoclonal Antibodies for Treating Cancer
• Exhibit 5.7 Mode of Action of HerceptinR
• Exhibit 5.8 Timeline of HerceptinR Development
• Exhibit 5.9 Emerging Monoclonal Antibodies for Breast Cancer
• Exhibit 6.1 Historical Milestones Associated with Chemotherapy Development
• Exhibit 6.2 Approved Chemotherapy Drugs for Breast Cancer
• Exhibit 6.3 Phase III Chemotherapy Agents
• Exhibit 6.4 Structure of Targaceutical®
• Exhibit 6.5 Select Phase II Chemotherapy Agents
• Exhibit 6.6 Gemzar and Paclitaxel as Combination Therapy
• Exhibit 7.1 Drug Targets Associated with Breast Cancer Therapeutics
• Exhibit 7.2 Tumor Marker Testing in Breast Cancer
• Exhibit 8.1 Key/Emerging Players in the Endocrine Therapy Market for Breast Cancer
• Exhibit 8.2 Sales of Endocrine Therapies for Breast Cancer (2003 and 2004)
• Exhibit 8.3 Sales of NolvadexR (tamoxifen) from 2001 to 2004
• Exhibit 8.4 Sales of Approved Aromatase Inhibitors (2003-2004)