Gastrointestinal stromal tumors (GIST) are one of the common tumors in the gastrointestinal system. DCC-2618 is a new kinase inhibitor that was designed to block the activity of pan-KIT and PDGFRα kinase. In a phase I study, 32 gastrointestinal stromal tumors (GIST) patients who previously failed all 3 approved therapies (imatinib, sunitinib or regorafenib) were treated with DCC-2618 ≥100 mg/day. The most recent data presented at the 2017 Connective Tissue Oncology Society (CTOS) Annual Meeting revealed that the disease control rate (DCR) was 76% after treated with DCC-2618 for 12 weeks, and at 24 weeks, the DCR was 57%. The KIT mutations (exons 9, 11, 13, 14, 17 and 18) were detected in plasma cell-free DNA of 19 patients. After treating with 2 cycles of DCC-2618, the allele mutation frequency decreased compared to baseline. According to the treatment-emergent adverse events (TEAEs) analysis at the 2017 ESMO Annual Congress, there were 18 events of grade 3/4 anemia in 70 patients, and the investigators noted that the anemia may not be related to treatment. These data revealed that the DCC-2618 is a potential drug for heavily pretreated GIST patients.