Liraglutide: Difference between revisions

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{{Drugbox
| IUPAC_name        = ''L''-histidyl-''L''-alanyl-''L''-α-glutamylglycyl-''L''-threonyl-''L''-phenylalanyl-''L''-threonyl-''L''-seryl-''L''-α-aspartyl-''L''-valyl-''L''-seryl-''L''-seryl-''L''-tyrosyl-''L''-leucyl-''L''-α-glutamylglycyl-''L''-glutaminyl-''L''-alanyl-''L''-alanyl-N<sup>6</sup>-[N-(1-oxohexadecyl)-''L''-γ-glutamyl]-''L''-lysyl-''L''-α-glutamyl-''L''-phenylalanyl-''L''-isoleucyl-''L''-alanyl-''L''-tryptophyl-''L''-leucyl-''L''-valyl-''L''-arginylglycyl-''L''-arginyl-glycine
| synonyms = Arg<sup>34</sup>Lys<sup>26</sup>-(''N''-ε-(γ-Glu(''N''-α-hexadecanoyl)))-GLP-1[7-37]
| image            = Liraglutide structure.png
| CAS_number        = 204656-20-2
| CAS_supplemental  =
| ATC_prefix        = A10
| ATC_suffix        = BX07
| ATC_supplemental  =
| PubChem          =
| DrugBank          =
| chemical_formula  =
| C=172 | H=265 | N=43 | O=51
| molecular_weight  = 3751.20 g/mol
| smiles            =
| bioavailability  = N/A
| protein_bound    =
| metabolism        =
| elimination_half-life = 11-15 hours
| excretion        =
| pregnancy_AU      =  <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US      =  <!-- A / B            / C / D / X -->
| pregnancy_category= 
| legal_AU =  <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled-->
| legal_CA =  <!-- Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK =  <!-- GSL, P, POM, CD, or Class A, B, C -->
| legal_US =  <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
| legal_status      =
| routes_of_administration = Subcutanous
}}
{{SI}}
{{CMG}}


==Overview==
'''Liraglutide''' or (NN2211) is a glucagon-like peptide-1 ([[GLP-1]]) analog that is being developed by [[Novo Nordisk]] under the brand-name "Victoza" for the treatment of [[type 2 diabetes]]. <ref>http://www.drugs.com/nda/liraglutide_080530.html May 2008</ref> <ref>http://www.medicalnewstoday.com/articles/74913.php June 2007</ref> <ref>http://www.medicalnewstoday.com/articles/110349.php June 2008</ref> <ref>http://www.drugdevelopment-technology.com/projects/liraglutide/ </ref> <ref>http://www.novonordisk.com/science/about_rd/quarterly_rd_update.asp Oct 2008 Inc results of LEAD 6 extension</ref>
==Pharmacodynamics==
Studies to date suggest liraglutide improves control of [[blood glucose]].<ref name="DJN">http://diabetes.webmd.com/news/20080924/new-diabetes-drug-liraglutide-works Sept 2008</ref>
It reduces meal-related [[hyperglycaemia]] (for 12 hours after administration) by increasing [[insulin]] secretion, delaying gastric emptying, and suppressing prandial [[glucagon]] secretion.
Liraglutide may have advantages over current therapies:
*It acts in a glucose-dependent manner, meaning that it will stimulate insulin secretion only when blood glucose levels are higher than normal. Consequently, it shows negligible risk of  [[hypoglycemia]].
*It has the potential for inhibiting [[apoptosis]] and stimulating regeneration of [[beta cell]]s (seen in animal studies).
*It decreases appetite and maintains body weight, as shown in a head-to-head study versus [[glimepiride]].<ref name="Barclay">http://www.medscape.com/viewarticle/581180 "Liraglutide May Be Safe, Effective as First Drug Therapy for Type 2 Diabetes" </ref><ref> http://care.diabetesjournals.org/cgi/content/abstract/32/1/84 Diabetes Care. Oct 2008</ref>
*It lowers blood [[triglyceride]] levels.
*It has only mild and transient side effects, mainly gastrointestinal.
==Pharmacokinetics==
Liraglutide is a once-daily GLP-1 derivative for the treatment of type 2 diabetes. GLP-1, in its natural form, is short-lived in the body (the half-life after subcutaneous injection is approximately one hour), so it is not very useful as a therapeutic agent. However, liraglutide has a half-life after subcutaneous injection of 11–15 hours, making it suitable for once-daily dosing
(in contrast to [[Byetta]]'s twice daily).
The prolonged action of liraglutide is achieved by attaching a fatty acid molecule at one position of the GLP-1 molecule, enabling it to bind to [[albumin]] within the subcutaneous tissue and bloodstream. The active GLP-1 is then released from albumin at a slow, consistent rate. Binding with albumin also results in slower degradation and reduced elimination of liraglutide from the circulation by the kidneys compared to GLP-1.
==See also==
* [[Glucagon-like peptide-1 analog]]
* [[incretin]]
==References==
{{reflist|2}}
{{Oral hypoglycemics and insulin analogs}}
[[Category:Anti-diabetic drugs]]
[[Category:Diabetes]]
[[Category:Hormones]]
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Revision as of 13:13, 5 August 2014