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A tyrosine kinase inhibitor used in cancer treatment


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Apatinib, also known as YN968D1, is a small-molecule tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor 2 (VEGFR-2). It is primarily used in the treatment of various types of cancer, including gastric cancer and non-small cell lung cancer.

Mechanism of Action

Apatinib functions by targeting and inhibiting the activity of VEGFR-2, a receptor that plays a crucial role in angiogenesis, the process by which new blood vessels form from pre-existing vessels. By blocking this receptor, apatinib effectively reduces the blood supply to tumors, thereby inhibiting their growth and proliferation.

Clinical Applications

Apatinib has been studied extensively in clinical trials for its efficacy in treating advanced gastric cancer, particularly in patients who have not responded to other treatments. It has shown promise in improving progression-free survival and overall survival rates in these patients. Additionally, apatinib is being investigated for its potential use in other cancers, such as breast cancer and colorectal cancer.

Pharmacokinetics

Apatinib is administered orally and is absorbed into the bloodstream, where it reaches peak plasma concentrations within a few hours. It is metabolized primarily in the liver and excreted through the feces. The drug has a half-life of approximately 9 hours, allowing for once-daily dosing.

Side Effects

Common side effects of apatinib include hypertension, proteinuria, and hand-foot syndrome. Patients may also experience fatigue, diarrhea, and anorexia. It is important for healthcare providers to monitor patients for these adverse effects and manage them appropriately.

Research and Development

Ongoing research is exploring the use of apatinib in combination with other chemotherapeutic agents and immunotherapies to enhance its efficacy and broaden its application in cancer treatment. Studies are also investigating biomarkers that may predict patient response to apatinib, allowing for more personalized treatment approaches.

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Contributors: Prab R. Tumpati, MD