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| Clinical data | |
|---|---|
| Trade names | Somatuline |
| Other names | Lanreotide acetate (JANJP), Lanreotide acetate (USANUS) |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | Intramuscular,subcutaneous |
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| Pharmacokinetic data | |
| Bioavailability | Approximately 80% |
| Protein binding | 78% |
| Metabolism | InGI tract |
| Eliminationhalf-life | 2 hours (immediate release) 5 days (sustained release) |
| Excretion | Mostly bile duct |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.215.992 |
| Chemical and physical data | |
| Formula | C54H69N11O10S2 |
| Molar mass | 1096.33 g·mol−1 |
| 3D model (JSmol) | |
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Lanreotide, sold under the brand nameSomatuline among others, is amedication used in the management ofacromegaly and symptoms caused byneuroendocrine tumors, most notablycarcinoid syndrome. It is a long-actinganalogue ofsomatostatin, likeoctreotide.
Lanreotide (as lanreotideacetate) is manufactured byIpsen. It is available in several countries, including the United Kingdom, Australia and Canada, and was approved for sale in the United States by theFood and Drug Administration (FDA) on August 30, 2007.[2]
Lanreotide is used in the treatment ofacromegaly, due to bothpituitary and non-pituitary growth hormone-secreting tumors, and the management of symptoms caused byneuroendocrine tumors, particularlycarcinoid tumors andVIPomas. 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 ofthyrotrophicadenoma,[3] a rare tumor of the pituitary gland which secretes TSH.
Lanreotide also shows activity against non-endocrine tumors, and, along with othersomatostatin analogues, is being studied as a possible general antitumor agent.[4][5]
In December 2014, the US FDA approved lanreotide for the treatment of people with unresectable, well or moderately differentiated, locally advanced or metastatic gastroenteropancreaticneuroendocrine tumors (GEP-NETs).[6]
It is used for polycystic liver disease.[medical citation needed] It has also been shown that it reduces the volume by 264mls on average.[medical citation needed]
The mainside effects of lanreotide treatment are mild to moderate pain at the injection site andgastrointestinal disturbances, such asdiarrhea,nausea andvomiting. Isolated cases ofgallstone formation have been associated with use of lanreotide, particularly over long periods of time.[3]
Lanreotide is a synthetic analogue ofsomatostatin, a naturally occurring inhibitoryhormone which blocks the release of several other hormones, includinggrowth hormone,thyroid-stimulating hormone (TSH),insulin andglucagon. Lanreotide binds to the samereceptors 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),[7] lanreotide has a much longer half-life, and produces far more prolonged effects.[medical citation needed]
Lanreotide is available in two formulations: a sustained release formulation (sold under the trade name 'Somatuline LA'), which isinjected intramuscularly every ten or fourteen days,[3] and an extended release formulation (UK trade name 'Somatuline Autogel', or 'SomatulineDepot' in the US), which is administered subcutaneously once a month.[8]
Lanreotide has been shown to spontaneously self-assemble into monodisperse nanotubes of 24.4 nm diameter[9] and has been thereafter used as a fruitful and versatile model system in several biophysical studies.[citation needed]
