Introduction: Angiogenesis is a vital process for cellular functions in both physiological and pathophysiological conditions and is one of the hallmarks of cancer progression and metastasis. VEGF/VEGFR-2 signaling pathway has been recognized as the most critical factor in promoting angiogenesis. Hence, several VEGFR-2 inhibitors have been clinically tested and/or approved for the treatment of angiogenesis-related diseases.Areas covered: This review covered reports in the patent literature in the period 2017 to the end of 2020 on the small-molecule inhibitors and antibodies of VEGFR-2 and their potential use as therapeutics for several types of cancers, angiogenesis-related disorders, and Parkinson's and Alzheimer's diseases.Expert opinion: VEGF inhibition has attracted considerable attention as a potential approach for antiangiogenic therapy during the last two decades. However, the effectiveness of this approach may be limited by several issues such as weak response, resistance development, and serious adverse effects. Therefore, the combination of anti-angiogenic therapy with chemotherapy and/or immunotherapy, together with the proper utilization of nanomedicine-based approaches, may have a synergistic effect on improving the efficiency of therapy, reducing side effects and lowering the cost.
Keywords: Patent; VEGFR-2; angiogenesis; anticancer; inhibitors.