Pharmacological Properties of Tyrosine Kinase Inhibitors: Current Perspectives

Tyrosine kinase inhibitors (TKIs) are an important class of targeted therapeutic agents that have significantly transformed modern cancer treatment. These drugs selectively inhibit abnormal tyrosine kinase signaling pathways involved in cellular proliferation, differentiation, angiogenesis, and survival. The introduction of TKIs has improved therapeutic outcomes in several malignancies, including chronic myeloid leukemia, non-small cell lung cancer, renal cell carcinoma, and breast cancer. Pharmacological properties such as high selectivity, oral bioavailability, and favorable therapeutic efficacy make TKIs highly valuable in targeted therapy. Most TKIs act through inhibition of ATP-binding sites within kinase domains, thereby suppressing downstream signaling pathways associated with tumor progression. However, long-term administration may lead to adverse effects including hepatotoxicity, cardiotoxicity, skin toxicity, and metabolic disturbances. In addition, acquired resistance caused by secondary mutations and activation of alternative signaling pathways remains a major limitation of TKI therapy. Recent advances in next-generation kinase inhibitors and combination therapeutic strategies demonstrate promising potential for overcoming resistance and improving treatment efficacy. This review summarizes the pharmacological characteristics, therapeutic applications, adverse effects, and future perspectives of tyrosine kinase inhibitors in contemporary targeted therapy.