Abstract
BACKGROUND AND OBJECTIVE: Advanced or metastatic breast cancer (MBC) is associated with poor prognosis and presents many challenges in medical management and treatment decisions. Anticancer drugs that act on cell cycle mechanisms have shown great potential in preclinical studies. In clinical trials, abemaciclib, a reversible ATP-competitive cyclin-dependent kinase 4/6 (CDK4/6) inhibitor developed by Eli Lilly and Company, combined with endocrine therapy (ET) were associated with superior outcomes compared with ET alone in patients with advanced or metastatic hormone receptor positive (HR(+))/human epidermal growth factor receptor 2 negative (HER2(-)) breast cancer, representing a new standard-of-care in this population. Abemaciclib has been approved by the U.S. Food and Drug Administration (FDA) for use in HR(+)/HER2(-) MBC. In China, abemaciclib was also approved by the National Medical Products Administration (NMPA) based on findings from the MONARCH plus trial. Recently, abemaciclib have been approved as the first and only CDK4/6 inhibitor by FDA and NMPA for use in HR(+)/HER2(-), node-positive, early breast cancer (EBC) at high risk of recurrence and Ki-67 score ≥20%. Further trials of abemaciclib are ongoing. This is an overview of the clinical development of abemaciclib in breast cancer. METHODS: We reviewed English publications in PubMed related to CDK4/6 inhibitors from 2011 to 2021. KEY CONTENT AND FINDINGS: In this review, we summarized the mechanism, results of preclinical and clinical studies of abemaciclib, describing current indications for treatment, ongoing clinical trials, safety and tolerability, and future perspectives. CONCLUSIONS: Abemaciclib is a unique CDK4/6 inhibitor with distinctive characteristics and promising data, which bring benefit to HR(+), HER2(-) breast cancer patients.