Lanreotide
Encyclopedia
Lanreotide is a medication used in the management of acromegaly
and symptoms caused by neuroendocrine tumors
, most notably carcinoid syndrome
. It is a long-acting analogue
of somatostatin
, like octreotide
.
Lanreotide (as lanreotide acetate
) is manufactured by Ipsen
, and marketed under the trade name Somatuline. It is available in several countries, including the United Kingdom
, Australia
and Canada
, and was approved for sale in the United States
by the Food and Drug Administration
(FDA) on August 30, 2007.
, 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 receptor
s 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.
, due to both pituitary
and non-pituitary growth hormone-secreting tumors, and the management of symptoms caused by neuroendocrine tumors
, particularly carcinoid tumors and VIPoma
s. 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.
Interestingly, lanreotide also shows activity against non-endocrine tumors, and, along with other somatostatin analogues, is being studied as a possible general antitumor agent.
s 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.
every ten or fourteen days, and an extended release formulation (UK trade name Somatuline Autogel, or Somatuline Depot in the U.S.), which is administered subcutaneously once a month.
Acromegaly
Acromegaly is a syndrome that results when the anterior pituitary gland produces excess growth hormone after epiphyseal plate closure at puberty...
and symptoms caused by neuroendocrine tumors
Neuroendocrine tumors
Neuroendocrine tumors are neoplasms that arise from cells of the endocrine and nervous systems. Many are benign, while some are cancers...
, most notably carcinoid syndrome
Carcinoid syndrome
Carcinoid syndrome refers to the array of symptoms that occur secondary to carcinoid tumors. The syndrome includes flushing and diarrhea, and, less frequently, heart failure and bronchoconstriction...
. It is a long-acting analogue
Analog (chemistry)
In chemistry, a structural analog , also known as chemical analog or simply analog, is a compound having a structure similar to that of another one, but differing from it in respect of a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced...
of somatostatin
Somatostatin
Somatostatin is a peptide hormone that regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G-protein-coupled somatostatin receptors and inhibition of the release of numerous secondary hormones.Somatostatin...
, like octreotide
Octreotide
Octreotide is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone...
.
Lanreotide (as lanreotide acetate
Acetate
An acetate is a derivative of acetic acid. This term includes salts and esters, as well as the anion found in solution. Most of the approximately 5 billion kilograms of acetic acid produced annually in industry are used in the production of acetates, which usually take the form of polymers. In...
) is manufactured by Ipsen
Ipsen
Ipsen is a French pharmaceutical company headquartered in Paris, France. It primarily develops and markets medications used in oncology, endocrinology and the treatment of neuromuscular disorders. In 2005, Ipsen spent € 169 million—20.9% of consolidated sales—on research and development, according...
, and marketed under the trade name Somatuline. It is available in several countries, including the United Kingdom
United Kingdom
The United Kingdom of Great Britain and Northern IrelandIn the United Kingdom and Dependencies, other languages have been officially recognised as legitimate autochthonous languages under the European Charter for Regional or Minority Languages...
, Australia
Australia
Australia , officially the Commonwealth of Australia, is a country in the Southern Hemisphere comprising the mainland of the Australian continent, the island of Tasmania, and numerous smaller islands in the Indian and Pacific Oceans. It is the world's sixth-largest country by total area...
and Canada
Canada
Canada is a North American country consisting of ten provinces and three territories. Located in the northern part of the continent, it extends from the Atlantic Ocean in the east to the Pacific Ocean in the west, and northward into the Arctic Ocean...
, and was approved for sale in the United States
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
by the Food and Drug Administration
Food and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...
(FDA) on August 30, 2007.
Pharmacology
Lanreotide is a synthetic analogue of somatostatinSomatostatin
Somatostatin is a peptide hormone that regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G-protein-coupled somatostatin receptors and inhibition of the release of numerous secondary hormones.Somatostatin...
, a naturally occurring inhibitory hormone
Hormone
A hormone is a chemical released by a cell or a gland in one part of the body that sends out messages that affect cells in other parts of the organism. Only a small amount of hormone is required to alter cell metabolism. In essence, it is a chemical messenger that transports a signal from one...
which blocks the release of several other hormones, including growth hormone
Growth hormone
Growth hormone is a peptide hormone that stimulates growth, cell reproduction and regeneration in humans and other animals. Growth hormone is a 191-amino acid, single-chain polypeptide that is synthesized, stored, and secreted by the somatotroph cells within the lateral wings of the anterior...
, thyroid-stimulating hormone
Thyroid-stimulating hormone
Thyrotrophin-stimulating hormone is a peptide hormone synthesized and secreted by thyrotrope cells in the anterior pituitary gland, which regulates the endocrine function of the thyroid gland.- Physiology :...
(TSH), insulin
Insulin
Insulin is a hormone central to regulating carbohydrate and fat metabolism in the body. Insulin causes cells in the liver, muscle, and fat tissue to take up glucose from the blood, storing it as glycogen in the liver and muscle....
and glucagon
Glucagon
Glucagon, a hormone secreted by the pancreas, raises blood glucose levels. Its effect is opposite that of insulin, which lowers blood glucose levels. The pancreas releases glucagon when blood sugar levels fall too low. Glucagon causes the liver to convert stored glycogen into glucose, which is...
. Lanreotide binds to the same receptor
Somatostatin receptor
There are five known somatostatin receptors:* SST1 * SST2 * SST3 * SST4 * SST5 All are G protein-coupled seven transmembrane receptors.-External links:...
s 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.
Indications
Lanreotide is used in the treatment of acromegalyAcromegaly
Acromegaly is a syndrome that results when the anterior pituitary gland produces excess growth hormone after epiphyseal plate closure at puberty...
, due to both pituitary
Pituitary gland
In vertebrate anatomy the pituitary gland, or hypophysis, is an endocrine gland about the size of a pea and weighing 0.5 g , in humans. It is a protrusion off the bottom of the hypothalamus at the base of the brain, and rests in a small, bony cavity covered by a dural fold...
and non-pituitary growth hormone-secreting tumors, and the management of symptoms caused by neuroendocrine tumors
Neuroendocrine tumors
Neuroendocrine tumors are neoplasms that arise from cells of the endocrine and nervous systems. Many are benign, while some are cancers...
, particularly carcinoid tumors and VIPoma
VIPoma
A VIPoma is a rare endocrine tumor, usually originating in the pancreas, that produces vasoactive intestinal peptide ....
s. 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
Thyrotrope
Thyrotropes are endocrine cells in the anterior pituitary which produce thyroid stimulating hormone in response to thyrotropin releasing hormone .Thyrotropes appear basophilic in histological preparations....
adenoma
Pituitary adenoma
Pituitary adenomas are tumors that occur in the pituitary gland, and account for about 15% of intracranial neoplasms. Tumors which exceed 10 mm in size are defined as macroadenomas, and those smaller than 10 mm are referred to as microadenomas...
, a rare tumor of the pituitary gland which secretes TSH.
Interestingly, lanreotide also shows activity against non-endocrine tumors, and, along with other somatostatin analogues, is being studied as a possible general antitumor agent.
Side effects
The main side effectAdverse drug reaction
An adverse drug reaction is an expression that describes harm associated with the use of given medications at a normal dosage. ADRs may occur following a single dose or prolonged administration of a drug or result from the combination of two or more drugs...
s of lanreotide treatment are mild to moderate pain at the injection site and gastrointestinal
Gastrointestinal tract
The human gastrointestinal tract refers to the stomach and intestine, and sometimes to all the structures from the mouth to the anus. ....
disturbances, such as diarrhea
Diarrhea
Diarrhea , also spelled diarrhoea, is the condition of having three or more loose or liquid bowel movements per day. It is a common cause of death in developing countries and the second most common cause of infant deaths worldwide. The loss of fluids through diarrhea can cause dehydration and...
, nausea
Nausea
Nausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...
and vomiting
Vomiting
Vomiting is the forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose...
. Isolated cases of gallstone formation have been associated with use of lanreotide, particularly over long periods of time.
Formulations
Lanreotide is available in two formulations: a sustained release formulation (sold under the trade name Somatuline LA), which is injected intramuscularlyIntramuscular injection
Intramuscular injection is the injection of a substance directly into a muscle. In medicine, it is one of several alternative methods for the administration of medications . It is used for particular forms of medication that are administered in small amounts...
every ten or fourteen days, and an extended release formulation (UK trade name Somatuline Autogel, or Somatuline Depot in the U.S.), which is administered subcutaneously once a month.