Tyrosine Kinase Inhibitor

Tyrosine kinase inhibitors, or TKIs, are substances that block the action of tyrosine kinase enzymes. Tyrosine kinase enzymes are responsible for the activation of many proteins by signal transduction cascades. They are a part of many cell functions, including cell signaling, growth, and division. These enzymes may be too active or found at high levels in some types of cancer cells. Blocking the enzymes may help keep cancer cells from growing.

Tyrosine kinase inhibitors are an important class of targeted therapy, and play an important role in cancer therapy, specifically in the modulation of growth factor signaling. Several tyrosine kinase inhibitors have been found to have effective antitumor activity, and have been approved or are in clinical trials.

Tyrosine kinase inhibitors interfere with certain cell signaling pathways and allow target-specific therapy for selected malignancies. With the use of these targeted therapies comes the potential for resistance to develop, along with a lack of tumor response in the general patient population. The availability of new inhibitors and enriched patient selection may help overcome such problems for future therapy.

Examples of TKIs are:

  • Imatinib
  • Gefitinib
  • Erlotinib
  • Sorafenib
  • Sunitinib
  • Dasatinib
  • Nilotinib
  • Ponatinib
  • Idelalisib
  • Ibrutinib
  • Acalabrutinib
  • And many others