|Pronunciation||lan ree' oh tide|
|Other names||Lanreotide acetate|
|Drug class||Somatostatin analogue|
|Main uses||Acromegaly, neuroendocrine tumors such as carcinoid, thyroid tumors|
|Side effects||Diarrhea, abdominal pain, nausea, gallstones, joint pain, pain at the site of injection|
|Metabolism||In GI tract|
|Elimination half-life||2 hours (immediate release)|
5 days (sustained release)
|Chemical and physical data|
|Molar mass||1096.33 g/mol|
1156.380 g/mol (acetate) g·mol−1
|3D model (JSmol)|
Lanreotide, sold under the brand name Somatuline, is a medication used to treat acromegaly, neuroendocrine tumors such as carcinoid, and thyroid tumors. In acromegaly it is used when other treatments are not effective. It is given by injection under the skin or into a muscle.
Common side effects include diarrhea, abdominal pain, nausea, gallstones, joint pain, and pain at the site of injection. Other side effects may include pancreatitis, high blood sugar, low blood sugar, and liver problems. It is a somatostatin analogue and works by decreasing levels of growth hormone, insulin, and glucagon.
Lanreotide was approved for medical use in the United States in 2007. In the United Kingdom it costs the NHS about £550 at a dose of 60 mg per month as of 2021. This amount in the United States costs about 6,100 USD.
Lanreotide is used in the treatment of acromegaly, due to both pituitary and non-pituitary growth hormone-secreting tumors, and the management of symptoms caused by neuroendocrine tumors, particularly carcinoid tumors and VIPomas. In the United States and Canada, lanreotide is only indicated for the treatment of acromegaly. In the United Kingdom, it is also indicated in the treatment of thyrotrophic adenoma, a rare tumor of the pituitary gland which secretes TSH.
In Dec 2014 the US FDA approved lanreotide for the treatment of patients with unresectable, well or moderately differentiated, locally advanced or metastatic gastroenteropancreatic neuroendocrine tumors (GEP-NETs).
Lanreotide is available in two formulations: a sustained release formulation (sold under the trade name "Somatuline LA"), which is injected intramuscularly every ten or fourteen days, and an extended release formulation (UK trade name "Somatuline Autogel", or "Somatuline Depot" in the US), which is administered subcutaneously once a month.
The main side effects of lanreotide treatment are mild to moderate pain at the injection site and gastrointestinal disturbances, such as diarrhea, nausea and vomiting. Isolated cases of gallstone formation have been associated with use of lanreotide, particularly over long periods of time.
Lanreotide is a synthetic analogue of somatostatin, a naturally occurring inhibitory hormone which blocks the release of several other hormones, including growth hormone, thyroid-stimulating hormone (TSH), insulin and glucagon. Lanreotide binds to the same receptors as somatostatin, although with higher affinity to peripheral receptors, and has similar activity. However, while somatostatin is quickly broken down in the body (within minutes), lanreotide has a much longer half-life, and produces far more prolonged effects.
The efficacy of lanreotide has not been extensively studied, and results differ greatly between trials and formulations.
Lanreotide has been shown to spontaneously self-assemble into monodisperse nanotubes of 24.4 nm diameter and has been thereafter used as a fruitful and versatile model system in several biophysical studies.
Its sequence is H-D-2Nal-Cys(1)-Tyr-D-Trp-Lys-Val-Cys(1)-Thr-NH2.
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