Octreotide LAR: Safety and tolerability issues

Background: Somatostatin analogues are the cornerstone in therapy of acromegaly and functioning neuroendocrine tumors. Long-acting retard formulations have improved patient survival and contributed considerably to quality of life. The first such compound was octreotide LAR ('long-acting release'), characterized by high affinity to somatostatin receptor subtypes 2 and 5, which has to be injected intramuscularly every 4 weeks. Objective: The aim was to screen all octreotide LAR-related literature and assess the compound's profile for safety and tolerability. Methods: An extensive literature search has been performed using the MEDLINE database to retrieve data from clinical studies evaluating the efficacy and tolerability of octreotide LAR. Results/conclusion: Octreotide LAR is well tolerated; however, diarrhea and gallstone formation were identified as the main adverse events. Impairment of glucose homeostasis was a regular phenomenon, but its occurrence was unpredictable. General side effects such as headache, abdominal discomfort or fatigue were also reported. According to incidental case reports, administration during pregnancy appears to be safe for both mother and child; however, definitive evidence is missing. In addition, octreotide LAR has been evaluated for further indications including treatment of solid tumor entities, due to its antiproliferative effect. Currently, several compounds (lanreotide, SOM230) with a broader receptor spectrum are under evaluation and may improve treatment efficacy and lower incidence of side effects.