Levemir (LYS)

Levemir (LYS), also known as Insulin Detemir, is a long-acting basal insulin analogue used for the treatment of diabetes mellitus. It’s designed to provide a relatively stable and prolonged glucose-lowering effect, typically lasting up to 24 hours, allowing for once- or twice-daily administration. The “(LYS)” designation indicates a specific lysine residue within the insulin molecule that has been modified. This modification involves the attachment of a myristic acid (a C14 fatty acid) to the lysine residue. This acylation enhances the molecule’s binding to albumin in the bloodstream. The albumin binding prolongs the duration of action of Levemir by slowing its absorption from the injection site and reducing its clearance from the circulation. The primary biological activity of Levemir (LYS) is to lower blood glucose levels by stimulating glucose uptake by cells and inhibiting hepatic glucose production. The specific modification at the LYS residue is crucial for its long-acting properties and relatively predictable absorption profile.

Appearance

• Clear, colorless solution for subcutaneous injection.

Source

• Produced by recombinant DNA technology in Saccharomyces cerevisiae (yeast).

• The insulin analogue is then synthetically modified with myristic acid.

• Purified and formulated for pharmaceutical use.

Molecular Weight and Structure

• Molecular weight is higher than unmodified human insulin (~5.8 kDa) due to myristic acid (C14:0) modification; approximately 5917 g/mol.

• Structure: Human insulin sequence with threonine at position B30 removed (desB30).

• Lysine at B29 is acylated with myristic acid via a glutamyl spacer.

Biological Activity

• Lowers blood glucose by stimulating cellular glucose uptake and inhibiting hepatic glucose production.

• Binds insulin receptor on muscle, liver, and fat cells to activate signaling.

• Lysine modification promotes self-association and albumin binding, leading to prolonged half-life enabling once- or twice-daily dosing.

Application

• Treatment of diabetes mellitus for both type 1 and type 2 diabetes.

Key Characteristics

• Human insulin analogue with desB30 base sequence.

• Long-acting profile enabling once or twice daily injections.

• Acylation at lysine B29 with myristic acid to enhance albumin binding and prolong action.

• Activates insulin receptor-mediated pathways akin to endogenous insulin.

• Formulated as a sterile injectable solution for subcutaneous administration.

Purity and Microbial Contamination

Identity and Quality Control

Shelf Life and Storage

Citation 

• Pharmacology of insulin detemir (PubMed)

• Insulin detemir overview (ScienceDirect)

• FDA Approval History for Levemir

• DrugBank entry for insulin detemir

• PubChem: Insulin detemir

• Levemir clinical trials (clinicaltrials.gov)

• Novo Nordisk Levemir patient leaflet

• FDA label (DailyMed)

• Clinical experience of insulin detemir (PubMed)