04 January 2024 | Lei Wang, Wang-Qing Liu, Sylvain Broussy, Bingnan Han, Hongming Fang
Recent advances of anti-angiogenic inhibitors targeting the VEGF/VEGFR axis
Angiogenesis is a complex process involving endothelial cell proliferation, migration, vascular tube formation, and new blood vessel formation. It is essential for normal physiological processes such as embryonic development and wound healing. However, excessive angiogenesis can lead to pathological conditions like cancer and retinopathies. Vascular endothelial growth factor (VEGF) and its receptors (VEGFRs) are key regulators of angiogenesis. Anti-angiogenic therapy, which inhibits VEGF/VEGFR signaling, has become a major treatment approach for various cancers and retinal diseases.
Several anti-angiogenic drugs targeting the VEGF/VEGFR axis have been approved, including monoclonal antibodies like bevacizumab, fusion proteins such as ranibizumab and aflibercept, and small molecules like sorafenib and sunitinib. These drugs work by blocking VEGF/VEGFR interactions, inhibiting VEGFR tyrosine kinase activity, or interfering with downstream signaling pathways. They have shown significant clinical benefits in treating cancers and retinal diseases, but also have side effects such as hypertension, fatigue, and gastrointestinal issues.
In addition to these drugs, inhibitors targeting VEGFR downstream signaling pathways, such as the RAS/RAF/MEK/ERK and PI3K/AKT/mTOR pathways, are also being developed. These inhibitors aim to block the signaling cascades that promote angiogenesis and tumor growth. However, they are not yet widely used in clinical practice due to their potential for off-target effects and other side effects.
The development of anti-angiogenic drugs targeting the VEGF/VEGFR axis continues to be an active area of research, with new drugs and therapies being explored to improve efficacy and reduce side effects. The future of anti-angiogenic therapy may involve the development of more targeted and personalized treatments, as well as the combination of different therapeutic approaches to achieve better outcomes for patients.Recent advances of anti-angiogenic inhibitors targeting the VEGF/VEGFR axis
Angiogenesis is a complex process involving endothelial cell proliferation, migration, vascular tube formation, and new blood vessel formation. It is essential for normal physiological processes such as embryonic development and wound healing. However, excessive angiogenesis can lead to pathological conditions like cancer and retinopathies. Vascular endothelial growth factor (VEGF) and its receptors (VEGFRs) are key regulators of angiogenesis. Anti-angiogenic therapy, which inhibits VEGF/VEGFR signaling, has become a major treatment approach for various cancers and retinal diseases.
Several anti-angiogenic drugs targeting the VEGF/VEGFR axis have been approved, including monoclonal antibodies like bevacizumab, fusion proteins such as ranibizumab and aflibercept, and small molecules like sorafenib and sunitinib. These drugs work by blocking VEGF/VEGFR interactions, inhibiting VEGFR tyrosine kinase activity, or interfering with downstream signaling pathways. They have shown significant clinical benefits in treating cancers and retinal diseases, but also have side effects such as hypertension, fatigue, and gastrointestinal issues.
In addition to these drugs, inhibitors targeting VEGFR downstream signaling pathways, such as the RAS/RAF/MEK/ERK and PI3K/AKT/mTOR pathways, are also being developed. These inhibitors aim to block the signaling cascades that promote angiogenesis and tumor growth. However, they are not yet widely used in clinical practice due to their potential for off-target effects and other side effects.
The development of anti-angiogenic drugs targeting the VEGF/VEGFR axis continues to be an active area of research, with new drugs and therapies being explored to improve efficacy and reduce side effects. The future of anti-angiogenic therapy may involve the development of more targeted and personalized treatments, as well as the combination of different therapeutic approaches to achieve better outcomes for patients.