TARGETED THERAPIES IN CANCER

TARGETED THERAPIES IN CANCER

Library of Congress Cataloging-in-Publication Data

Contents

Preface

Chapter 1: Innovation in the Biopharmaceutical Pipeline

Abstract

Introduction

Drug Discovery and Development Process

Discovery and Preclinical Testing

Clinical Testing in Human Subjects

Regulatory Review and Approval

Post-Approval Research and Monitoring

References

Chapter 2: The Diversity of Targeted Cancer Drugs Recently Approved by the FDA

Abstract

Introduction

1) Tyrosine Kinase (TK) Inhibitors (TKIs)

2) Serine/Threonine Kinase Inhibitors (STKIs)

3) Monoclonal Antibodies (MAbs)

4) Decoy Vascular Endothelial Growth Factor Receptor

5) Immunomodulatory Agents

7) Antimetabolites

8) Enzymes

9) Histone Deacetylase (HDAC) Inhibitors

10) Proteasome Inhibitors

11) Hedgehog Pathway Inhibitor

12) Protein Translation Inhibitor

13) Hormone (Androgen Deprivation) Therapy

14) Microtubule Targeting Agents

15) Autologous Cellular Immunotherapy

16) Radiopharmaceutical Compound

References

Chapter 3: Chronological List of Targeted Cancer Drugs Approved by the FDA

Abstract

Introduction

Reference

Chaper 4: Targeted Therapies: Detailed Description

Abstract

Introduction

Rituximab

Trastuzumab

Imatinib

Alemtuzumab

Ibritumomab

Gefitinib

Tositumomab

Azacitidine

Pemetrexed

Cetuximab

Bevacizumab

Erlotinib

Nelarabine

Sorafenib

Pegaspargase

Lenalidomide

Sunitinib

Dasatinib

Panitumumab

Vorinostat

Bortezomib

Decitabine

Lapatinib

Temsirolimus

Ixabepilone

Nilotinib

Degarelix

Everolimus

Pralatrexate

Pazopanib

Ofatumumab

Romidepsin

Cabazitaxel

Sipuleucel-T

Eribulin

Denosumab

Ipilimumab

Vandetanib

Abiraterone

Vemurafenib

Brentuximab

Crizotinib

Asparaginase Erwinia chrysanthemi

Axitinib

Vismodegib

Pertuzumab

Carfilzomib

Ziv-aflibercept

Enzalutamide

Bosutinib

Regorafenib

Omacetaxine

Cabozantinib

Ponatinib

Pomalidomide

Ado-trastuzumab Emtansine

Radium Ra223

Trametinib

Dabrafenib

Afatinib

Obinutuzumab

Ibrutinib

Ramucirumab

Ceritinib

Chapter 5: Targeted Therapy for Chronic Lymphocytic Leukemia (CLL)

Abstract

Introduction

Rituximab

Rituximab As a Single Agent

Chemoimmunotherapy with Rituximab

Alemtuzumab

Ofatumumab

Ofatumumab and Chlorambucil

Obinutuzumab

Ibrutinib

Conclusion

References

Chapter 6: Targeted Therapy for HER-2-Positive Breast Cancer

Abstract

Introduction

Trastuzumab

Lapatinib

Approved for HER-2-Overexpressing Breast Cancer

Approved for Hormone-Positive and HER-2-Positive Advanced Breast Cancer

Pertuzumab

Ado-Trastuzumab Emtansine

Conclusion

References

Chapter 7: Targeted Therapy for Metastatic Breast Cancer: Varia

Abstract

Introduction

Ixabepilone

Eribulin

Everolimus

Conclusion

References

Chapter 8: Targeted Therapy for Chronic Myelogenous Leukemia (CML)

Abstract

Introduction

Imatinib

Imatinib and Resistance

Nilotinib

Dasatinib

Bosutinib

Ponatinib

Market Removal and Return to the Market of Ponatinib

Omacetaxine

References

Chapter 9: Targeted Therapy for Gastrointestinal Stromal Tumors (GIST)

Abstract

Introduction

Mutated KIT and/or PDGFRA in GIST

Imatinib: From CML to GIST

Sunitinib

Regorafenib

Conclusion

References

Chapter 10: Targeted Therapy for Metastatic Colorectal Cancer (mCRC)

Abstract

Introduction

Bevacizumab

Second-Line Treatment of mCRC

Ziv-Aflibercept

Regorafenib

Cetuximab

K-Ras Wild-Type (WT), EGFR-Expressing mCRC

Panitumumab: Panitumumab Is a MAb

Directed against EGFR

Reminder on the Importance of KRAS on

Anti-EGFR Therapy

Conclusion

References

Chapter 11: Targeted Therapy for Metastatic Melanoma (McM)

Abstract

Introduction

Immunotherapy Options in Metastatic Melanoma

Interleukin-2 (IL-2)

Interferon α-2b

Ipilimumab

Vemurafenib

Dabrafenib

Trametinib

Dabrafenib and trametinib

Conclusion

References

Chapter 12: Targeted Therapy for Multiple Myeloma (MM)

Introduction

Current Strategies: Background

Newly-Diagnosed Disease

Maintenance Treatment

Approvals

1. Immunomodulatory Agents

Thalidomide

Lenalidomide

Pomalidomide

2. Proteasome Inhibitors

Bortezomib

Carfilzomib

Conclusion

References

Chapter 13: Targeted Therapy for Metastatic Castration-Resistant Prostate Cancer (mCRPC)

Abstract

Introduction

Cabazitaxel

Sipuleucel-T

Abiraterone

Denosumab

Enzalutamide

Radium Ra223

Conclusion

References

Chapter 14: Targeted Therapy for Metastatic Renal Cell Carcinoma (mRCC)

Abstract

Introduction

Treatment and Outcomes

Stage IA

Stage IB

Stages II and III

Stage IV

Immunotherapy

Interleukin-2

Bevacizumab Plus Interferon-α

Targeted Therapy

A: VEGF Pathway Inhibitors

First-Line Options: Sunitinib and Pazopanib

Sunitinib

Pazopanib

Bevacizumab Plus Interferon-α

(See Above in “Immunotherapy” Section)

Second-Line Options: Sorafenib and Axitinib

Sorafenib

Axitinib

B: mTOR Inhibitors

Temsirolimus

Everolimus

Conclusion

References

Chapter 15: Targeted Therapy for Gastric Cancer

Abstract

Introduction

Trastuzumab

Ramucirumab

Conclusion

References

Chapter 16: Targeted Therapy for Non-Small Cell Lung Cancer (NSCLC)

Abstract

Introduction

Pemetrexed

Pemetrexed in Maintenance Treatment of

Non-Squamous NSCLC

Bevacizumab

First-Line Treatment of NSCLC

Targeting Genetic Mutations in NSCLC

A. Targeting EGFR

Gefitinib

Erlotinib

Afatinib

B. Targeting KRAS

C. Targeting ALK

Crizotinib

Ceritinib

Conclusion

References

Chapter 17: Targeted Therapy for Myelodysplastic Syndromes (MDS)

Abstract

Introduction

Azacitidine

Decitabine

Lenalidomide

Conclusion

References

Chapter 18: Targeted Therapy for Mantle Cell Lymphoma (MCL)

Abstract

Introduction

Bortezomib

Lenalidomide

Ibrutinib

Conclusion

References

Chapter 19: Abbreviations

Chapter 20: Generic Names – Trade Names: Equivalences

Index