Skip to Main Content

++

INTRODUCTION

++

This chapter will be most useful after having a basic understanding of the material in Chapter 62 Targeted Therapies: Tyrosine Kinase Inhibitors, Monoclonal Antibodies, and Cytokines, and Chapter 63 Natural Products in Cancer Chemotherapy: Hormones, in Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition. In addition to the material presented here, the 12th Edition contains:

++

  • A discussion of the use of targeted anticancer therapies in combination with cytotoxic agents in Chapter 60 General Principles of Cancer Chemotherapy

  • The molecular structures of small molecule drugs used in targeted anticancer therapies

++

LEARNING OBJECTIVES

++

  • Understand the mechanisms of action and clinical uses of small molecule inhibitors of protein tyrosine kinases.

  • Understand the mechanisms of action and clinical uses of monoclonal antibodies that target growth factor receptors and other tumor cell antigens.

  • Understand the mechanisms of action and clinical uses of monoclonal antibodies that target the VEGF pathway.

  • Understand the mechanism of action and clinical uses of anticancer drugs that target the mTOR pathway, and proteosome-mediated protein degradation.

  • Understand the mechanism of action and clinical uses of anticancer drugs that target the IL-2 receptor.

  • Understand the clinical uses of the immunomodulatory analogs (IMiDs) in treating multiple myeloma and myelodysplastic syndrome.

  • Understand the mechanism of action and use of hormone therapy to treat hormone-dependent tumors.

  • Know the common and important toxicities of targeted anticancer pharmacotherapies.

  • Know mechanisms of acquired resistance to specific targeted anticancer therapies.

++

DRUGS INCLUDED IN THIS CHAPTER

  • 131I-Tositumomab (BEXXAR)

  • 90Y-Ibritumomab tiuxetan (ZEVALIN)

  • Abarelix (PLENAXIS; withdrawn from market)

  • Abiraterone (ZYTIGA)

  • Aldesleukin (IL-2; PROLEUKIN)

  • Alemtuzumab (CAMPATH)

  • Anastrozole (ARIMIDEX)

  • Bevacizumab (AVASTIN)

  • Bicalutamide (CASODEX, others)

  • Bortezomib (VELCADE)

  • Buserelin (SUPREFACT)—not available in the United States

  • Cetrorelix (CETROTIDE)

  • Cetuximab (ERBITUX)

  • Cyproterone—not available in the United States

  • Dasatinib (BMS-354825; SPRYCEL)

  • Degarelix (FIRMAGON)

  • Denileukin diftitox (ONTAK)

  • Deslorelin—not available in the United States

  • Dexamethasone

  • Erlotinib (TARCEVA)

  • Everolimus (AFINITOR)

  • Exemestane (AROMASIN)

  • Flutamide (EULEXIN)

  • Fulvestrant (FASLODEX)

  • Ganirelix—not available in the United States

  • Gefitinib (IRESSA)

  • Gemtuzumab ozogamicin (MYLOTARG)—withdrawn from the US market in 2010

  • GnRH (GONADORELIN)

  • Goserelin (ZOLADEX)

  • Histrelin (VANTAS)

  • Imatinib mesylate (STI 571; GLEEVEC, GLIVEC)

  • Ketoconazole (NIZORAL)

  • Lapatinib (TYKERB)

  • Lenalidomide (REVLIMID)

  • Letrozole (FEMARA)

  • Leuprolide (LUPRON, ELIGARD)

  • Medroxyprogesterone (DEPO-PROVERA, others)

  • Megestrol (MEGACE)

  • Megestrol acetate (MEGACE, others)

  • Nafarelin (SYNAREL)

  • Nilotinib (AMN107; TASIGNA)

  • Nilutamide (NILANDRON)

  • Ofatumumab (ARZERRA)

  • Panitumumab (VECTIBIX)

  • Pazopanib (VOTRIENT)

  • Prednisone

  • Raloxifene (EVISTA)

  • Ranibizumab (LUCENTIS)

  • Rapamycin (sirolimus; RAPAMUNE)

  • Rituximab (RITUXAN)

  • Sorafenib (NEXAVAR)

  • Sunitinib (SUTENT)

  • Tamoxifen (NOLVADEX, others)

  • Temsirolimus (TORISEL)

  • Thalidomide (THALOMID)

  • Toremifene (FARESTON)

  • Trastuzumab (HERCEPTIN)

  • Triptorelin (TRELSTAR, TRELSTARDEPOT)

++
Table Graphic Jump Location
MECHANISMS OF ACTION AND RESISTANCE OF TARGETED ANTICANCER DRUGS

Pop-up div Successfully Displayed

This div only appears when the trigger link is hovered over. Otherwise it is hidden from view.