Next-Generation Kinase Inhibitors: Overcoming Resistance and Enhancing Clinical Outcomes

Protein kinase inhibitors have revolutionized cancer treatment by targeting specific kinases involved in tumor growth and survival. As of 2024, over 80 small-molecule protein kinase inhibitors have received FDA approval, most of which function by inhibiting ATP binding to the target kinase 1,2 . However, the effectiveness of these inhibitors is often limited by the development of resistance, mainly due to mutations in the kinase domain. In response to this challenge, next-generation kinase inhibitors are being developed to tackle drug resistance and improve patient outcomes.