What are angiogenesis inhibitors and how do they work?
Angiogenesis inhibitors (antiangiogenic agents) are drugs that prevent the formation of new blood vessels (angiogenesis). Because growing tumours require oxygen and nutrients to proliferate and survive, angiogenesis is a crucial mechanism in tumour growth and metastasis. Angiogenesis inhibitors primarily target the vascular endothelial growth factor (VEGF) signalling pathway: either by binding to the ligand itself to inhibit its activity (such as the monoclonal antibody bevacizumab or the fusion protein aflibercept), or by inhibiting receptor tyrosine kinases with small-molecule kinase inhibitors (TKIs, such as sunitinib or sorafenib). In addition, they can induce what is known as vascular normalisation of the abnormal tumour vasculature, which can improve blood perfusion and enhance the efficacy of co-administered chemotherapy or immunotherapy. Their use can be associated with characteristic adverse effects, such as hypertension and proteinuria.\n\nIn addition to ligand and receptor blockers, bispecific antibodies (such as faricimab, which dual-targets VEGF-A and Ang-2) are also being investigated and used to inhibit neovascularisation in ophthalmologic conditions (such as neovascular age-related macular degeneration) and tumours.
References
- [Angiogenesis inhibitors: mechanism of action and nephrotoxicity]. PMID 34838486
- Tumor Anti-Angiogenesis Therapy and Its Influence on Immune Cell Function in the Tumor Microenvironment. PMID 42120944
- Anatomic and functional outcomes of intravitreal faricimab for polypoidal choroidal vasculopathy: a review. PMID 41973161