Abstract: Tropomyosin receptor kinase (TRK) belongs to the tyrosine kinases family. It is encoded by the gene of neurotrophic tyrosine receptor kinase (NTRK) and participates in the differentiation of neurons. The fusion of NTRK with other genes is closely related to the pathogenesis of cancer. In recent years, small molecule inhibitors targeting TRK have become a new strategy for cancer treatment. Several TRK inhibitors are currently in different clinical research stages. Larotrectinib and entrectinib have been approved by FDA in 2018 and 2019, respectively. In this article, the structure of TRK and research progress of some representative TRK inhibitors have been introduced, and the future of TRK inhibitors R&D and treatment strategies to overcome drug resistance have been prospected.