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Selective VEGFR inhibitors for anticancer therapeutics in clinical use and clinical trials

Cunlong Zhang1, Chunyan Tan, Huaiwei Ding

  • 1Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, China.

Current Pharmaceutical Design
|May 11, 2012
PubMed

Insights

Selective Vascular Endothelial Growth Factor Receptor (VEGFR) kinase inhibitors are crucial in cancer treatment, targeting tumor growth and metastasis. This review covers their clinical use, trial results, and strategies to enhance efficacy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Tumor growth and metastasis are critically dependent on angiogenesis and vasculogenesis.
  • Vascular Endothelial Growth Factor (VEGF) and its receptors (VEGFRs) are key regulators of these processes.
  • Targeting VEGFR kinase has emerged as a successful clinical strategy in cancer therapy.

Purpose of the Study:

  • To review selective small-molecule VEGFR inhibitors currently in clinical use and trials.
  • To analyze in vitro, in vivo, and clinical trial data for these inhibitors.
  • To discuss VEGF/VEGFR pathways in tumor angiogenesis and strategies for improving inhibitor efficacy.

Main Methods:

  • Literature review of selective small-molecule VEGFR inhibitors.
  • Analysis of preclinical (in vitro, in vivo) and clinical trial data.
  • Discussion of VEGF/VEGFR signaling and therapeutic strategies.

Main Results:

  • Several VEGFR inhibitors are approved for clinical use, with many more in development.
  • These inhibitors demonstrate varying degrees of efficacy in preclinical and clinical settings.
  • Understanding VEGF/VEGFR pathways is essential for optimizing therapeutic strategies.

Conclusions:

  • Selective VEGFR inhibitors represent a significant advancement in cancer treatment.
  • Continued research is needed to improve their efficacy and overcome resistance.
  • Targeting angiogenesis via VEGFR inhibition remains a promising area in oncology drug development.

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