Quantitation of TAK-981 in human plasma via LC-MS/MS and its application in clinical trials

TAK-981 is a highly effective and selective inhibitor of the small ubiquitin-like modifier (SUMO) activating enzyme, and it promotes the expression of type I interferons (IFN-Is). Developing a sensitive bioanalytical assay for quantitating TAK-981 is essential in the clinical investigations for oncology drug development. TAK-981 and its stable isotope labeled compound (TAK-981¹³C₄, ¹⁵N₂) as the internal standard were employed in this LC-MS/MS assay. This assay was successfully validated from 0.1 ng/mL to 100 ng/mL with good accuracy and precision and has been applied to support clinical studies. A sensitive and robust LC-MS/MS assay was validated for TAK-981 in human plasma for the first time. TAK-981 is a drug being studied to help treat cancer. It blocks a certain enzyme and helps the immune system work better. A special lab test was made to measure how much TAK-981 is in the blood after someone takes it. The test worked well at many different levels and gave correct and steady results. This is the first time such a reliable test has been made to measure TAK-981 in human blood for clinical research.