Liraglutide

Liraglutide

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-N6- [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 = Arg34Lys26-("N"-ε-(γ-Glu("N"-α-hexadecanoyl)))-GLP-1 [7-37]



CAS_number = 204656-20-2
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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 =
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routes_of_administration = Subcutanous

Liraglutide (NN2211), which if approved, will be marketed under the brand=name "Victoza", is a long-acting glucagon-like peptide-1 (GLP-1) analog that is being developed by Novo Nordisk for the treatment of type 2 diabetes. As of|September 2008, it is pending FDA and EMEA approvals. The company anticipates it could be brought to market in 2009, though third-party financial analysts are less certain. Liraglutide is required to go to a Food and Drug Administration Advisory Committee, creating further doubt about the safety and efficacy of Liraglutide, "Victoza". [novodordisk website]

Pharmacodynamics

Studies to date suggest liraglutide improves control of blood glucose. 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 cells (seen in animal studies).
*It decreases appetite and maintains body weight, as shown in a head-to-head study versus glimepiride.
*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.

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.

Notes

[1] http://www.novonordisk.com/press/sea/sea.asp?sShowNewsItemGUID=2015c61f-7d6e-4740-8538-d22780320022&sShowLanguageCode=en-GB


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