Abstract
Angiogenesis has always been the topic of major scientific interest in the field of malignant tumors. Nowadays, targeting angiogenesis has achieved success in various carcinomas by several mechanisms, including the use of anti-angiogenic small molecule receptor tyrosine kinase inhibitors (TKIs). The development of TKIs targeting pro-angiogenic receptors, mainly vascular endothelial growth factor receptor (VEGFR) family, have significantly improved the outcome of certain types of cancers, like renal cell carcinoma, hepatocellular carcinoma, and colorectal carcinoma. However, the general response rate is not very satisfactory. The particular toxicity profile and resistance to anti-angiogenic targeted agents are unavoidable, and no specific marker is available to screen responsive patients to TKIs for precision therapy. To date, about 11 anti-angiogenic TKIs with different binding capacities to angiogenic receptor tyrosine kinase have been approved for the treatment of patients with advanced cancers. This review presents all approved anti-angiogenic small molecule receptor TKIs so far with an emphasis on their indications and clinical efficacy. We also discuss the combination between TKIs and immune checkpoint blockade inhibitors based on the most recent exciting outcome in immunotherapy.
Highlights
As described by Hanahan and Weinberg, tumor angiogenesis is regarded as one of the ten hallmarks of cancer [1]
Based on the theory that tumor growth, progression, and metastasis depend on angiogenesis, targeting tumor blood vessels has been introduced as a logical approach to the treatment of various malignancies [3]
This study showed progression-free survival (PFS) was not inferior in the pazopanib group compared to the sunitinib group, and the objective response rate (ORR) was higher in the pazopanib group (p < 0.05) and the overall survival (OS) between these two groups showed no statistical significance
Summary
As described by Hanahan and Weinberg, tumor angiogenesis is regarded as one of the ten hallmarks of cancer [1]. It was initially approved for the treatment of advanced renal cell carcinoma (RCC) based on a phase III, randomized, double-blind clinical trial [27]. In May 2011, the FDA approved sunitinib for treating patients with advanced progressive pancreatic neuroendocrine tumors (pNETs) based on the results of a phase III study [35].
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