Apatinib Mesylate in the Treatment of Advanced Triple-Negative Breast Cancer

BACKGROUND: The effectiveness of conventional chemotherapy in treating metastatic triple-negative breast cancer (TNBC) is unsatisfactory. Apatinib, a small-molecule tyrosine kinase vascular inhibitor, is a multi-targeted antitumor angiogenesis agent that promotes apoptosis to inhibit tumors. SUMMARY: Apatinib, when combined with chemotherapy, has demonstrated efficacy in treating advanced TNBC. Additionally, immune checkpoint inhibitors (ICIs) have emerged as a promising therapeutic option for metastatic TNBC; however, their efficacy still requires further improvement. One potential strategy to enhance the efficacy of ICIs in metastatic TNBC is through their combination with chemotherapy and anti-angiogenic agents. The combination of apatinib, chemotherapy, and ICIs has demonstrated favorable efficacy, with improved progression-free survival compared with the conventional chemotherapy for advanced TNBC. This warrants further exploration of its clinical value. This triple therapy exhibits synergistic effects rather than representing a simple combination of agents. Apatinib can reverse chemoresistance and enhance the efficacy of programmed death receptor-1 (PD-1) inhibitor therapy. Combining chemotherapeutic agents with ICIs is complementary, and apatinib, combined with chemotherapy, can modify the tumor microenvironment to improve the effectiveness of ICIs. KEY MESSAGES: This review examines the role of apatinib in treating TNBC and explores its potential mechanisms when combined with chemotherapeutic agents and ICIs for advanced TNBC in the era of immunotherapy.