Tyrosine Kinase Inhibitors For Cancer | Amanda Ngo, PharmD Intern | RxEconsult

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Tyrosine Kinase Inhibitors For The Treatment Of Cancer Category: Cancer by - October 24, 2016 | Views: 25148 | Likes: 0 | Comment: 0  

Tyrosine kinase inhibitors for cancer

Tyrosine Kinase Inhibitors For Cancer

Cancer is a disease characterized by abnormal and improperly controlled cell growth, resulting in invasive growths that have the potential to spread throughout the body. Cancer can be caused by a number of different processes, one being the overexpression of protein kinases, leading to over-phosphorylation of proteins that can change a cell’s function and activity.

There are at least 518 kinases and 156 phosphatases that act on different factors and receptors, such as endothelial growth factors and colony-stimulating factors. Kinase and phosphatase activity are involved in many aspects of cellular function. Mutations that cause abnormal activation of these proteins, leading to the unregulated growth of the cell, are involved in the development cancer.

Development of kinase inhibitors that target specific protein kinases has demonstrated a great, positive clinical impact in the treatment of different cancers as they halt the proliferation and survival of cancer cells.

Tyrosine Kinase Function And Tyrosine Kinase Inhibitor (TKI) Mechanism of Action

Protein kinase inhibitors are targeted therapy. They work by inhibiting kinases, which are enzymes that are involved in many cellular processes. Kinases add phosphate groups to amino acids and they are categorized according to the type of amino acid that they phosphorylate. For example, the addition of phosphate groups to the serine and threonine amino acids of proteins are added by serine and threonine-specific protein kinases. Histidine-specific protein kinases add a phosphate group to the histidine portion of amino acids. Protein kinase inhibitors block the action of specific kinases. 

Tyrosine protein kinases add a phosphate group to the tyrosine amino acid of proteins. This reaction affects cellular communication signals that are responsible for cell division and growth. These kinases affect growth factors that regulate the cell cycle; the main growth factors that these kinases phosphorylate are epidermal growth factors (EGF), platelet-derived growth factors (PDGF), and vascular endothelial growth factors (VEGFR). EGF regulate cell growth and differentiation, PDGF is involved in cell development, and VEGFR plays a role in the creation of blood vessels. 

Tyrosine kinase inhibitors used for treating cancer turn off tyrosine kinase activity, halting the signals required for cells, including cancer cells, to divide and grow.

List of tyrosine kinase inhibitors for cancer 

  • Imatinib (Gleevec)
  • Dasatinib (Sprycel)
  • Osimertinib (Tagrisso)
  • Erlotinib (Tarceva)
  • Gefitinib (Iressa)
  • Lapatinib (Tykerb)
  • Inbrutinib (Imbruvica)
  • Cabozantinib (Cometriq)
  • Lenvatinib (Lenvima)
  • Sunitinib (Sutent)

Types of cancers and examples of tyrosine kinase inhibitors


  • imatinib (Gleevec)
  • dasatinib (Sprycel)

Non-small cell lung cancer

  • osimertinib (Tagrisso)
  • erlotinib (Tarceva)
  • gefitinib (Iressa)

Colorectal cancer

  • regorafenib (Stivarga)

Breast cancer

  • lapatinib (Tykerb)


  • inbrutinib (Imbruvica)
  • thyroid cancer
  • cabozantinib (Cometriq)
  • lenvatinib (Lenvima)

Gastrointestinal stromal tumors, 

  • imatinib (Gleevec)
  • sunitinib (Sutent)

Renal cancer

  • sunitinib (Sutent)


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