VEGF inhibitors (Vascular Endothelial Growth Factor inhibitors) are a class of drugs that block the growth of new blood vessels, a process called angiogenesis.
These receptors play a crucial role in angiogenesis—the formation of new blood vessels that tumors need to grow and spread.
These agents cut off supply of oxygen and nutrients, these drugs are primarily used to treat various cancers and retinal eye diseases.
VEGF Inhibitors They are generally categorized into two main groups based on how they target the pathway:
Monoclonal Antibodies & Chimeric Proteins: Large molecules that bind to the VEGF protein itself or its receptors outside the cell.
Bevacizumab (Avastin): The first approved VEGF inhibitor; used for colorectal, lung, and renal cancers.
Ranibizumab (Lucentis): Specifically designed for intraocular injection to treat wet age-related macular degeneration (AMD).
Aflibercept (Eylea/Zaltrap): A “trap” protein that acts as a decoy receptor for VEGF.
Tyrosine Kinase Inhibitors (TKIs): Small molecules, usually taken orally, that block the intracellular signaling of VEGF receptors.
VEGFRs are tyrosine kinase receptors that, when activated by VEGF ligands, trigger signaling pathways promoting blood vessel formation.
VEGFR inhibitors block this signaling, essentially starving tumors of their blood supply.
Examples: Sunitinib (Sutent), Sorafenib (Nexavar), Pazopanib (Votrient), Axitinib, Cabozantinib, and Lenvatinib (Lenvima).
Used to treat solid tumors such as renal cell carcinoma, colorectal cancer, and glioblastoma.
They are often combined with chemotherapy.
Ophthalmology: Injected directly into the eye (intravitreal) to treat conditions like wet AMD, diabetic retinopathy, and macular edema.
VEGF is also necessary for healthy blood vessels, and systemic use can cause: Hypertension: High blood pressure occurs in 30–80% of patients and is considered a sign that the drug is working.
Proteinuria: Protein in the urine, indicating kidney strain.
Wound Healing Issues: Impaired ability for the body to repair tissues.
Thromboembolic Events: Increased risk of blood clots or stroke.
Side effects: Common side effects include hypertension, fatigue, diarrhea, hand-foot syndrome/skin reactions! and increased bleeding risk.
These occur because VEGF signaling affects normal blood vessels too, not just tumor vasculature.