Abstract: Antitumor drugs that target the signaling of vascular endothelial growth factor and its receptors have attracted increasing attention with the development of antiangiogenic targeted therapy. Apatinib is a second-generation vascular endothelial growth factor receptor- 2 inhibitor and a potent antiangiogenic agent. Apatinib is one of the recent oral molecular targeted anti tumor drugs. Clinical studies have indicated that apatinib exhibits high bioavailability and a tolerable safety profile. A series of large-scale randomized and controlled clinical trials before and after the release of the drug in the market have demonstrated encouraging objective response rate and survival benefit across a broad range of malignancies, including non-small cell lung cancer, breast cancer, and gastric cancer. Apa -tinib was approved and launched in China in2014as a subsequent-line treatment for patients with advanced gastric cancer. Apatinib is currently undergoing phase II/III clinical trials for the treatment of numerous cancer types, such as gastric carcinoma, lung cancer, he -patocellular carcinoma, esophageal cancer, and colorectal cancer. These clinical trials are conducted to determine the antitumor activi-ty of apatinib when administrated alone or in combination with other therapies. This review summarizes the latest research progress of apatinib, including antitumor mechanisms, clinical effects on different tumor types, safety profile and adverse effects, drug interac-tions, as well as drug resistance and biomarkers. This article presents a deeper understanding of the clinical application of apatinib in anti tumor treatment, and provides reference for future clinical practice in therapeutic options for cancer patients.