Lanreotide

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Lanreotide
Clinical data
Trade namesSomatuline
Other namesLanreotide acetate (JAN JP), Lanreotide acetate (USAN US)
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: C
subcutaneous
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityApproximately 80%
Protein binding78%
MetabolismIn GI tract
Elimination half-life2 hours (immediate release)
5 days (sustained release)
ExcretionMostly bile duct
Identifiers
  • 3-(2-naphthyl)-D-alanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-valyl-L-cysteinyl-L-threoninamide (2->7)-disulfide
JSmol)
  • C[C@H]([C@@H](C(=O)N)NC(=O)[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)C(C)C)CCCCN)Cc2c[nH]c3c2cccc3)Cc4ccc(cc4)O)NC(=O)[C@@H](Cc5ccc6ccccc6c5)N)O
  • InChI=1S/C54H69N11O10S2/c1-29(2)45-54(75)63-44(53(74)65-46(30(3)66)47(57)68)28-77-76-27-43(62-48(69)38(56)23-32-15-18-33-10-4-5-11-34(33)22-32)52(73)60-41(24-31-16-19-36(67)20-17-31)50(71)61-42(25-35-26-58-39-13-7-6-12-37(35)39)51(72)59-40(49(70)64-45)14-8-9-21-55/h4-7,10-13,15-20,22,26,29-30,38,40-46,58,66-67H,8-9,14,21,23-25,27-28,55-56H2,1-3H3,(H2,57,68)(H,59,72)(H,60,73)(H,61,71)(H,62,69)(H,63,75)(H,64,70)(H,65,74)/t30-,38-,40+,41+,42-,43+,44+,45+,46+/m1/s1 ☒N
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Lanreotide, sold under the brand name Somatuline among others, is a

analogue of somatostatin, like octreotide
.

Lanreotide (as lanreotide acetate) is manufactured by Ipsen. 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.[2]

Medical uses

Lanreotide is used in the treatment of

thyrotrophic adenoma,[3]
a rare tumor of the pituitary gland which secretes TSH.

Lanreotide also shows activity against non-endocrine tumors, and, along with other

somatostatin 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 gastroenteropancreatic

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]

Side effects

The main

gallstone formation have been associated with use of lanreotide, particularly over long periods of time.[3]

Pharmacology

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),[7] lanreotide has a much longer half-life, and produces far more prolonged effects.[medical citation needed]

Formulations

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,[3] and an extended release formulation (UK trade name 'Somatuline Autogel', or 'Somatuline Depot' in the US), which is administered subcutaneously once a month.[8]

Self-assembling properties

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]

References

  1. ^ "Mytolac (Amdipharm Mercury Australia Pty Ltd)". Therapeutic Goods Administration (TGA). 28 September 2022. Archived from the original on 13 November 2022. Retrieved 29 April 2023.
  2. ^ "FDA Approves New Drug to Treat Rare Disease, Acromegaly" (Press release). U.S. Food and Drug Administration. 30 August 2007. Archived from the original on 10 April 2021. Retrieved 6 September 2007.
  3. ^ a b c "Somatuline LA". electronic Medicines Compendium. 17 September 2003. Archived from the original on 24 September 2006. Retrieved 2 March 2007.
  4. PMID 16917205
    .
  5. PMID 16801334
    .
  6. ^ "FDA Approves Lanreotide Injection for GEP-NETs". 2014. Archived from the original on 26 June 2019. Retrieved 29 April 2023.
  7. S2CID 36873846
    .
  8. ^ "Somatuline Autogel". electronic Medicines Compendium. 12 April 2007. Archived from the original on 28 September 2007. Retrieved 19 April 2007.
  9. PMID 12930900
    .
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