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Updated: Jul 7, 2026

Monitoring Functionality and Morphology of Vasculature Recruited by Factors Secreted by Fast-growing Tumor-generating Cells
Published on: November 23, 2014
Antiangiogenesis in the treatment of skin cancer
1The Angiogenesis Foundation, Cambridge, MA 02238, USA.
Abstract:
Angiogenesis is the formation of new capillary blood vessels from existing vasculature. Cancers are dependent upon angiogenesis for their growth. Inhibition of angiogenesis can slow, halt, or regress tumors. Angiogenesis inhibition is now validated for the treatment of cancer using a variety of approved biologic, small molecule, multitargeting, and immunomodulatory agents. In the skin, strategies to inhibit angiogenesis-signaling pathways include blockade of COX-2, m-TOR, sonic hedgehog, growth factor receptor activation, and activation of Toll-like receptors (TLR). The agent with the most clinical experience as a topical antiangiogenic therapy is imiquimod. Imiquimod is a TLR agonist, with immune response modifying properties that also stimulates antiangiogenic cytokines, downregulates the expression of proangiogenic factors, upregulates the expression of endogenous inhibitors, and induces endothelial cell apoptosis. By titrating its dosing for angiogenesis inhibitory activity and not for gross inflammation, imiquimod can be applied in an efficacious and well-tolerated fashion to treat skin cancer.
Insights
Angiogenesis inhibition is crucial for cancer treatment. Topical imiquimod, a Toll-like receptor (TLR) agonist, effectively inhibits skin cancer growth by targeting angiogenesis pathways.
Area of Science:
- Oncology
- Dermatology
- Vascular Biology
Background:
- Cancer growth is critically dependent on angiogenesis, the formation of new blood vessels.
- Inhibiting angiogenesis is a validated strategy for cancer treatment, employing diverse therapeutic agents.
- Several signaling pathways in the skin, including Toll-like receptors (TLR), are targets for antiangiogenic therapy.
Purpose of the Study:
- To evaluate imiquimod as a topical agent for inhibiting angiogenesis in skin cancer treatment.
- To explore the mechanisms by which imiquimod exerts antiangiogenic effects.
Main Methods:
- Review of clinical experience with imiquimod as a topical antiangiogenic therapy.
- Analysis of imiquimod's molecular actions, including TLR agonism, cytokine modulation, and effects on angiogenic factors and endothelial cells.
Main Results:
- Imiquimod, a TLR agonist, demonstrates significant clinical experience as a topical antiangiogenic therapy.
- Imiquimod modulates the immune response, stimulates antiangiogenic cytokines, downregulates proangiogenic factors, upregulates inhibitors, and induces endothelial cell apoptosis.
- Titrated dosing of imiquimod for angiogenesis inhibition, rather than inflammation, allows for efficacious and well-tolerated topical treatment of skin cancer.
Conclusions:
- Imiquimod is an effective and well-tolerated topical antiangiogenic agent for skin cancer.
- Targeting angiogenesis pathways with agents like imiquimod offers a promising therapeutic strategy for skin malignancies.
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