InsulInomas are tumors that secrete insulin and cause hypoglycemia [1]. Approximately 80-90% of insulinomas occur as a single mass and can be treated via surgical resection; however, in cases of unclear localization, the presence of metastasis, advanced patient age, or other conditions that make surgery difficult, medical therapy is preferred [2]. Octreotide is a somatostatin analog that affects the somatostatin A 73-year-old woman with malignant insulinoma was treated with 100 µg/day octreotide for unresected insulinoma and liver metastases. The daily administration of the drug induced hyperglycemia after dinner in addition to existing fasting hypoglycemia possibly because this drug suppressed both insulin and glucagon secretion and its blood concentration was unstable. After replacing a daily injection of octreotide with a monthly injection of octreotide longacting repeatable (LAR), blood glucose levels stabilized within the normal range. The findings of the present study showed that octreotide LAR could be useful for the long-term treatment of unresectable insulinomas.Key words: Insulinoma, Octreotide, Octreotide long-acting repeatable, Hypoglycemia, Hyperglycemia receptors (SSTRs), with a strong affinity for SSTR2 and SSTR5 isoforms. This drug has been shown to inhibit the secretion of gastrointestinal hormones from the tumor as well as the growth of tumor cells [3]. Octreotide is sometimes used to prevent hypoglycemia caused by insulinomas; however, this drug can induce hyperglycemia as a side effect because it suppresses both insulin and glucagon secretion. There are 2 ways to administer this drug; daily subcutaneous injection of octreotide or monthly intramuscular injection of octreotide LAR, a slow-release formulation of octreotide. The half-life of octreotide is approximately 1.8 hours, whereas the effect of octreotide long-actingrepeatable (LAR) persists for over a month. We report herein on a case of a woman with malignant insulinoma who showed uncontrolled hypoglycemia and postprandial hyperglycemia when treated with octreotide but achieved good glycemic control after octreotide treatment was replaced with octreotide LAR.