Liraglutide

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Liraglutide
File:Liraglutide structure.svg
Clinical data
SynonymsArg34Lys26-(N-ε-(γ-Glu(N-α-hexadecanoyl)))-GLP-1[7-37]
Routes of
administration
Subcutanous
ATC code
Pharmacokinetic data
BioavailabilityN/A
Elimination half-life11-15 hours
Identifiers
CAS Number
E number{{#property:P628}}
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Chemical and physical data
FormulaC172H265N43O51
Molar mass3751.20 g/mol

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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. [1] [2] [3] [4] [5]

Pharmacodynamics

Studies to date suggest liraglutide improves control of blood glucose.[6]

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.[7][8]
  • 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.

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