Tyrosine KIs have become a targeted drug therapy for different malignancies. Over the past ten years, kinase inhibitors, including monoclonal antibodies and small-molecule TKIs targeted at kinases, have become a significant class of chemotherapeutic agents. A number of studies documenting the design, usage and validation of bioanalytical methods for TCKIs have been published as a result of the rising need for bioanalytical approaches to both qualitatively and quantitatively study such compounds. Many biomatrices, including blood, cerebrospinal fluid, urine, tissue, and even liver microsomes, can be used to quantify TCKIs. The majority of papers explain the technological framework of analytical methods that can do this. In recent times, there has also been an increase in interest in the discovery of intermediates and biotransformation mechanisms for novel TCKIs. We give a summary of TCKI bioanalytical techniques.