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Updated: Jul 31, 2026

Monitoring Functionality and Morphology of Vasculature Recruited by Factors Secreted by Fast-growing Tumor-generating Cells
Published on: November 23, 2014
Targeting angiogenesis with vascular endothelial growth factor receptor small-molecule inhibitors: novel agents with
Heather A Wakelee1, Joan H Schiller
1Oncology Division, Stanford University School of Medicine, CA, USA.
Abstract:
The treatment of lung cancer remains a significant challenge. Although chemotherapy remains the standard approach, a plateau has been reached in its efficacy. The development of novel targeted agents, particularly those targeting the epidermal growth factor receptor, has given us another approach. Developments with antiangiogenesis agents hold promise as new approaches in lung cancer therapy. Much of the work to date has focused on the anti-vascular endothelial growth factor (VEGF) antibody bevacizumab. In this article we will focus on the tyrosine kinase inhibitors of the VEGF receptors. These compounds, including sunitinib (SU11248; Sutent), vatalanib (PTK787), ZD6474, AZD2171, GW786034, sorafenib (BAY 43-9006), CP-547,632, and AG013736, are still at an early stage of development. We present phase I data (and phase II/III data when available) of these compounds and discuss their potential development in the treatment of lung cancer.
Insights
New targeted therapies, specifically tyrosine kinase inhibitors blocking vascular endothelial growth factor (VEGF) receptors, show promise for lung cancer treatment. These agents offer a novel approach beyond traditional chemotherapy.
Area of Science:
- Oncology
- Pharmacology
Background:
- Lung cancer treatment faces challenges with chemotherapy efficacy reaching a plateau.
- Targeted therapies, including those against the epidermal growth factor receptor and antiangiogenesis agents, represent promising new avenues.
Purpose of the Study:
- To review the development of tyrosine kinase inhibitors targeting vascular endothelial growth factor (VEGF) receptors for lung cancer.
- To present available Phase I, II, and III data for these novel agents.
Main Methods:
- Focus on tyrosine kinase inhibitors (TKIs) of VEGF receptors.
- Review of clinical trial data (Phase I, II, and III) for specific TKIs.
Main Results:
- Several TKIs targeting VEGF receptors are in early development.
- Data from Phase I trials are presented, with Phase II/III data included where available.
Conclusions:
- Tyrosine kinase inhibitors of VEGF receptors are emerging as a potential new class of drugs for lung cancer.
- Further clinical development is necessary to establish their role in lung cancer therapy.
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