Tanzisertib is primarily investigated for its use in oncology, specifically as a targeted therapy in cancer treatment. It functions as a selective inhibitor of certain kinases involved in tumor growth and progression. Its main application lies in the treatment of cancers driven by specific genetic mutations, particularly those involving the TRK (tropomyosin receptor kinase) family and ROS1 rearrangements. These mutations are found in a range of solid tumors, including lung, thyroid, and pediatric cancers. Due to its ability to cross the blood-brain barrier, tanzisertib shows promise in managing central nervous system (CNS) metastases, which are often challenging to treat with conventional therapies. This makes it valuable in advanced-stage cancers where brain involvement is present. It is also being studied in patients who have developed resistance to earlier-generation kinase inhibitors, offering a potential therapeutic option in refractory cases. Clinical trials are evaluating its efficacy, safety, and optimal dosing in both adult and pediatric populations, highlighting its role in precision medicine approaches to cancer care.