Apatinib

Overview

Apatinib is a small molecule tyrosine kinase inhibitor that selectively targets the vascular endothelial growth factor receptor-2 (VEGFR-2). It is primarily used in the treatment of various types of cancer, particularly gastric cancer and colorectal cancer. Apatinib works by inhibiting angiogenesis, the process by which new blood vessels form from pre-existing vessels, which is crucial for tumor growth and metastasis.

Mechanism of Action

Apatinib exerts its effects by binding to the intracellular domain of VEGFR-2, thereby blocking the downstream signaling pathways that promote endothelial cell proliferation and migration. This inhibition leads to reduced tumor vascularization and, consequently, tumor growth suppression.

Clinical Applications

Apatinib has been studied extensively in clinical trials for its efficacy in treating advanced gastric cancer and other malignancies. It is often considered for patients who have not responded to standard chemotherapy regimens. The drug has shown promise in improving progression-free survival and overall survival in certain patient populations.

Side Effects

Common side effects of apatinib include hypertension, proteinuria, hand-foot syndrome, and fatigue. These adverse effects are generally manageable with supportive care and dose adjustments.

Research and Development

Ongoing research is exploring the potential of apatinib in combination with other therapeutic agents, such as immunotherapy and chemotherapy, to enhance its anticancer effects. Studies are also investigating its role in treating other types of cancer, including non-small cell lung cancer and breast cancer.

Related Pages

• VEGFR-2
• Angiogenesis
• Gastric cancer
• Colorectal cancer
• Tyrosine kinase inhibitor

Gallery

Chemical structure of Apatinib