OBJECTIVES The use of off-label medication is restricted by government in some countries, because using off-label anticancer drugs has some concerns about its efficacy and toxicity. HIRA (Health Insurance Review & Assessment Service) has the process for the assessment and control for the off-label use of anticancer drugs in South Korea. We would introduce the controlling for the off-label use of anticancer drugs and evaluate the trend of off-label use in anticancer drugs. METHODS Since Dec. 2006, HIRA has permitted off-label uses for which there is adequate evidence for the efficacy, toxicity, and cost effectiveness. We collected the patient’s medical record data (briefly recorded response rate, major adverse effects. etc) which updated every year from hospital. We defined 37 cancers (36 cancers, other cancer) and preparative regimens of Hematopoietic stem cell transplantation. We calculated the number of approved off-label regimens by year and cancer type, and the regimen of the most widely used. RESULTS From Dec. 2006 to 2013, total 203 off-label regimens were approved their use in 63 hospitals (number of cumulative cases: 16,596). From 2006 to 2012, the number of approved off-label regimen was increased (1, 3, 3, 14, 39. 37, 67, respectively). In 2013, only 38 regimens were approved. Compared with the other cancer, non-Hodgkin lymphoma (30 regimens, 15%), ovarian cancer (10 regimens, 5%), and CLL (10 regimens, 5%) have many off-label regimens. The regimens: “<3 weekly> S-1 + cisplatin for gastric cancer” was the most widely used regimens (59 hospitals, number of cumulative cases: 2,283). CONCLUSIONS The use of off-label anticancer drugs has been increased in South Korea since 2006. These results suggest that the development of new drugs and the more clinical trials should be needed in cancer disease.