Insulin icodec (LYS)

Insulin Icodec (LYS) is an ultra-long-acting basal insulin analogue engineered for once-weekly administration in people with type 2 diabetes. It is a modified human insulin molecule with site-specific acylation at a lysine residue. This acylation involves attaching a fatty acid or other lipophilic group that promotes strong binding to albumin in the bloodstream, thereby greatly extending the half-life and enabling sustained glucose-lowering activity.

Appearance:

• Clear, colorless solution for subcutaneous injection.

Source:

• Produced recombinantly in Saccharomyces cerevisiae or similar expression systems.

• Insulin is subsequently chemically modified with a lipophilic fatty acid.

Molecular Weight:

• Greater than unmodified human insulin (~5.8 kDa) due to the fatty acid conjugation; exact weight depends on the moiety attached.

Structure:

• Human insulin sequence modified at a specific lysine residue by covalent attachment of a fatty acid through its epsilon-amino group.

• This modification enhances albumin binding and alters pharmacokinetics.

Biological Activity:

• Stimulates cellular glucose uptake and reduces hepatic glucose production.

• Binds insulin receptors to activate signaling pathways regulating glucose homeostasis.

• The LYS modification extends duration of action for once-weekly dosing.

Purity and Microbial Contamination:

• Purity typically ≥95%, ensuring pharmaceutical quality.

• Sterility and endotoxin levels meet strict regulatory thresholds.

Identity and Quality Control:

• Confirmed by mass spectrometry for molecular weight and modification.

• Amino acid and peptide mapping verify correct sequence and modification site.

• HPLC and SDS-PAGE confirm purity and aggregation status.

• Bioassays confirm activity at the insulin receptor.

Shelf Life and Storage

Applications:

• Treatment of type 2 diabetes requiring basal insulin support with reduced injection frequency.

Key Characteristics:

• Recombinant human insulin analogue.

• Modified at lysine for ultra-long-acting properties via albumin binding.

• Supports glucose regulation with once-weekly administration.

• Formulated as sterile injectable solution.

Research and Information Sources:

• FDA and EMA approval documents (status may vary; check latest updates).

• Clinical trial databases like clinicaltrials.gov and PubMed.

• Publications on insulin acylation and albumin-binding modifications.

• Patent databases for structure and manufacturing details.

• Search terms: “Insulin Icodec pharmacokinetics,” “acylated insulin,” “albumin binding insulin analogue,” “insulin receptor binding affinity.”