Tyrosine kinase inhibitors (TKIs) have transformed cancer treatment by selectively targeting crucial signalling pathways that drive tumour development and progression. This review examines the evolution, classification, and mechanisms of action of TKIs in oncology. It highlights their use across various cancers, such as chronic myeloid leukaemia, non-small cell lung cancer, and renal cell carcinoma. Key challenges, including drug resistance, side effects, and differences in patient outcomes, are discussed. Additionally, the review explores recent advancements, such as next-generation TKIs and their use in combination with immunotherapy. It aims to provide a thorough overview of the current role of TKIs in cancer care while outlining potential strategies to enhance patient outcomes in the future. This study offers a thorough analysis of TKIs, covering their pharmacological classifications, therapeutic uses, resistance mechanisms, and new developments. The emergence of first-, second-, and third-generation TKIs highlights their increasing specificity and effectiveness, especially in the treatment of cancers such gastrointestinal stromal tumors (GISTs), non-small cell lung cancer (NSCLC), and chronic myeloid leukaemia (CML). Problems like acquired resistance, side effects, and financial concerns continue to be important research topics. Combination treatments and next-generation TKIs are two recent developments that hold promise for enhancing precision medicine and improving patient outcomes.