Which medications in the drug class Antineoplastics, Tyrosine Kinase Inhibitors are used in the treatment of Colon Cancer?

Updated: Apr 15, 2020
  • Author: Tomislav Dragovich, MD, PhD; Chief Editor: N Joseph Espat, MD, MS, FACS  more...
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Antineoplastics, Tyrosine Kinase Inhibitors

VEGF induces endothelial cell proliferation and blood vessel permeability. Inhibiting VEGF prevents tyrosine kinase stimulation. The FDA approved the VEGF inhibitor ziv-aflibercept for metastatic colorectal cancer in August 2012. Approval was based on the Aflibercept Versus Placebo in Metastatic Colorectal Cancer (mCRC) After Failure of an Oxaliplatin-Based Regimen (VELOUR) trial that included 1226 patients. Results showed that when ziv-aflibercept was used in combination with FOLFIRI, overall survival and progression-free survival improved in patients with mCRC previously treated with an oxaliplatin containing regimen.

Ziv-aflibercept (Zaltrap)

Vascular endothelial growth factor (VEGF) inhibitor; prevents VEGF from stimulating cellular responses by binding to tyrosine kinase receptors (ie, the VEGF receptors). Indicated in combination with 5-fluorouracil, leucovorin, irinotecan (FOLFIRI) for metastatic colorectal cancer that is resistant to or has progressed after an oxaliplatin regimen.

Regorafenib (Stivarga)

Regorafenib is a tyrosine kinase inhibitor. It is indicated for metastatic colorectal cancer in patients who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy; an anti-VEGF therapy (eg, bevacizumab, ziv-aflibercept); and, if KRAS wild type, an anti-EGFR therapy (eg, cetuximab, panitumumab).

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