Recent FDA-approved kinase inhibitors for cancer therapy in 2025: A comprehensive review and perspectives

Malignant disorders continue to represent one of the major burdens of disease globally, especially in the context of premature deaths. Targeted anticancer treatments, including kinase inhibitors (KIs), have become crucial tools to disrupt the specific signaling pathways that are responsible for cancer growth following malignant transformation. Evidence demonstrates that KIs have substantially advanced precision oncology across multiple malignancies, with clinical success most notable in hematologic cancers and specific solid tumors, such as non-small cell lung cancer. Nonetheless, their long-term efficacy is often constrained by the emergence of acquired resistance, intratumoral heterogeneity, and off-target toxicities, underscoring the need for adaptive therapeutic strategies and combination regimens. While next-generation KIs and ongoing trials of KIs have the promise to expand the therapeutic landscape, the uneven distribution of clinical benefits across different cancer types reveals a considerable gap between molecular advances and real-world outcomes, leading to unequitable improvements in survival and quality of life for patients. Research also indicates disparities in access and affordability, raising concerns about their integration into routine care in low- and middle-income countries. The present review paper aims to provide a summary and a critical synthesis of the development, therapeutic potential, and clinical performance of novel of kinase inhibitors in oncology (i.e. zongeritinib, sunvozertinib, vimseltinib, mirdametinib, avutometinib and defactinib), authorized by the US Food and Drug Administration (FDA) in 2025, aiming to highlight both their transformative role and their inherent limitations. Taken together, KIs represent both a milestone and a challenge in oncology: they highlight the success of rational drug design and targeted therapy, yet show the need for continual innovation, improved global accessibility, and integration into multimodal strategies and standards of care to achieve durable survival benefits. See also the graphical abstract(Fig. 1).