Antiangiogenic Tyrosine Kinase Inhibitors in Metastatic Colorectal Cancer: Focusing on Regorafenib

Marios Papadimitriou1, Christos A Papadimitriou2

  • 1Oncology Unit, Second Department of Surgery, "Aretaieion" University Hospital, National and Kapodistrian University of Athens, Medical School, Athens, Greece.

Anticancer Research
|January 31, 2021
PubMed

Insights

Metastatic colorectal cancer (mCRC) progression involves VEGF and EGFR pathways. Antiangiogenic therapies targeting VEGF/VEGFR signaling, like regorafenib, show efficacy in treating mCRC.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cancer Research

Background:

  • Metastatic colorectal cancer (mCRC) progression is driven by key signaling pathways, including vascular endothelial growth factor (VEGF) and epidermal growth factor receptor (EGFR).
  • An imbalance favoring pro-angiogenesis (angiogenic switch) occurs early in colorectal cancer (CRC) development, promoting neovascularization and tumor progression.
  • VEGF-A is a critical cytokine in CRC angiogenesis, tumor growth, and metastasis.

Purpose of the Study:

  • To review the role of antiangiogenic tyrosine kinase inhibitors (TKIs) in mCRC treatment.
  • To highlight the efficacy of regorafenib as a targeted therapy for mCRC.

Main Methods:

  • Review of scientific literature on angiogenesis in CRC.
  • Analysis of clinical data for antiangiogenic agents targeting VEGF/VEGFR signaling.
  • Focus on tyrosine kinase inhibitors (TKIs) including regorafenib.

Main Results:

  • VEGF/VEGFR signaling is a crucial target in mCRC therapy.
  • Approved antiangiogenic agents demonstrate significant efficacy in mCRC treatment.
  • Regorafenib is an effective antiangiogenic TKI for mCRC.

Conclusions:

  • Targeting VEGF/VEGFR signaling is a validated strategy for mCRC.
  • Antiangiogenic TKIs, particularly regorafenib, represent important therapeutic options for patients with mCRC.

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