Octreotide long-acting release (LAR): a review of its use in the management of acromegaly.

Octreotide long-acting release (LAR) [Sandostatin LAR] is a somatostatin analogue with a well established clinical profile in patients with acromegaly. It binds to somatostatin receptor subtypes 2 and 5 with high potency to reduce the production and secretion of growth hormone (GH) and insulin-like growth factor (IGF)-I. Octreotide LAR is administered intramuscularly once every 28 days, in contrast to the subcutaneous formulation which requires administration two to three times daily. In several noncomparative trials, octreotide LAR was effective as primary therapy in normalizing GH and IGF-I levels and reducing tumour volume in patients with acromegaly. In addition, no significant difference was seen between octreotide LAR and surgery or lanreotide long-acting (LA) or lanreotide Autogel(R) (ATG) in small, randomized or observational, primary therapy trials. In another small, randomized trial, preoperative octreotide LAR followed by surgery was no more effective than surgery alone in terms of normalizing IGF-I levels, except in patients with macroadenoma. Octreotide LAR has also demonstrated good efficacy as postoperative adjuvant therapy, alone or in combination with pegvisomant, in randomized or noncomparative trials. In patients with different treatment histories (mixed populations), the efficacy of octreotide LAR appears to be generally similar to that of lanreotide ATG and greater than that of lanreotide LA, according to data from switching or crossover studies. Also in mixed populations, the efficacy of octreotide LAR was not significantly different to that of pegvisomant in terms of normalizing IGF-I levels in a randomized trial, and octreotide LAR demonstrated good efficacy in combination with cabergoline in a small, sequential-treatment trial. Octreotide LAR was generally well tolerated in clinical trials, with the most commonly occurring adverse events being gastrointestinal or hepatobiliary in nature. Thus, octreotide LAR continues to be a valuable option in the treatment of acromegaly.