gene is responsible for encoding , which consists of three family members: , , and . These family members encode different proteins known as , , and , respectively. fusion genes are the clearest driving factor for carcinogenesis. gene fusion detection and inhibitors are effective measures for the treatment of malignant tumors. The development of anti-tumor drugs targeting proteins has been favored by various scientific research institutions and pharmaceutical companies. The first-generation inhibitors, larotrectinib and entrectinib, have been approved for the treatment of pediatric and adult patients with metastatic or locally advanced solid tumors harboring fusion proteins, demonstrating remarkable anticancer efficacy in clinical settings. However, the issue of acquired resistance to inhibitors has emerged. Currently, efforts are underway to develop next-generation inhibitors based on sequence, structural, and kinetic methodologies, as well as to explore the intracellular signaling pathways of and the mechanisms underlying resistance. The main focus of this review was to discuss the fusion of genes and the application of inhibitor treatment.