Liraglutide

Liraglutide

Clinical data
Synonyms	Arg34Lys26-(N-ε-(γ-Glu(N-α-hexadecanoyl)))-GLP-1[7-37]
Routes of administration	Subcutanous
ATC code	A10BX07 (WHO)
Pharmacokinetic data
Bioavailability	N/A
Elimination half-life	11-15 hours
Identifiers
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
CAS Number	204656-20-2
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C172H265N43O51
Molar mass	3751.20 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.

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 (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