Tyrosine kinase inhibitors generally having a narrow therapeutic window and large inter-patient variability. In order to support its therapeutic drug monitoring, fast and accurate methods are needed to supporting the pharmacokinetic-guided dosing in patients treating with various tyrosine kinase inhibitors (TKIs) either alone or in combination in bulk, formulations or human plasma using HPLC and detection with tandem mass spectrometry (HPLC-MS/MS), gas chromatography with mass spectrometry, spectrofluorimetry and UV-Visible spectrometry. Literature suggested that the methods developed and validated are good for accuracy, precision, and assay for all TKIs studied. These methods are also applied for routine therapeutic drug monitoring and investigator-initiated research. In this review, we described different analytical methods used for the qualitative and quantitative estimation of all TKIs investigated till 2020 in assessing the quality of drugs by using HPLC, LC-MS, HPTLC, UPLC, UV-Visible spectrophotometry, spectrofluorimetry with a huge survey from the research articles published in various pharmaceutical and analytical chemistry journals. From this assessment, these methods were found to be superior based on the quantitative analysis of drugs in API, formulations, biological fluids such as serum and plasma. Detailed validation parameters are also given for the methods that help the researchers select suitable analytical techniques based on the information sought.