Insulin 0123-338 (oral) (LYS) is an investigational oral insulin analogue under development for type 2 diabetes treatment. The “(oral)” designation means it is formulated for oral administration, aiming to overcome the challenges of insulin degradation and poor absorption in the gastrointestinal tract. The “(LYS)” indicates a modification at a lysine residue, typically involving a protective or lipophilic group such as PEGylation or acylation, which enhances stability and absorption.
Appearance:
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Likely formulated as a tablet or capsule; appearance depends on specific formulation.
Source:
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Produced by recombinant DNA technology (e.g., E. coli or yeast).
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Post-expression chemical modification and formulation for oral use.
Molecular Weight:
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Higher than unmodified human insulin (~5.8 kDa) due to modification and excipients.
Structure:
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Human insulin sequence modified at lysine with an attached chemical group to protect against degradation and promote oral bioavailability; exact chemical nature proprietary.
Biological Activity:
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Stimulates glucose uptake and inhibits hepatic glucose production via binding to insulin receptor.
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Modified for absorption through the gut and sustained activity.
Purity and Contamination:
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Purity typically ≥95% (HPLC).
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Regulatory-compliant microbial and endotoxin controls.
Identity and Quality Control:
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Mass spectrometry confirms modification and molecular weight.
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Amino acid analysis and sequencing verify correct peptide composition.
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HPLC for purity and stability.
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Dissolution testing for oral dosage release.
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Bioactivity assays confirm functional receptor activation.
Shelf Life and Storage:
| Feature | Description |
|---|---|
| Shelf Life | Data not publicly available; consult suppliers |
| Storage | Likely room temperature controlled, protected from moisture and light |
Applications:
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Investigational oral therapy for type 2 diabetes mellitus.
Key Characteristics:
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Human insulin analogue with chemical modification at lysine to enhance oral bioavailability.
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Formulated for oral delivery with protective groups or carriers.
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Activates insulin receptor signaling comparable to injectable insulin.
Citation
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Structural and dynamic features of cagrilintide binding to receptors:
https://www.nature.com/articles/s41467-025-58680-y -
Cagrilintide lowers body weight through brain amylin receptor interaction:
https://pmc.ncbi.nlm.nih.gov/articles/PMC12270663/ -
Structural and mechanistic insights into dual activation of receptors by cagrilintide:
https://www.nature.com/articles/s41401-025-01635-2 -
Development of cagrilintide as a long-acting amylin analogue:
https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c00565 -
Efficacy of the dual amylin and calcitonin receptor agonist cagrilintide:
https://www.sciencedirect.com/science/article/pii/S0753332222012318 -
Weekly somapacitan effective and well tolerated in GH-deficient children:
https://pmc.ncbi.nlm.nih.gov/articles/PMC9693810/ -
Glucagon-like peptide-1 receptor mechanisms and regulation:
https://www.nature.com/articles/s41392-024-01931-z -
Liraglutide lowers palmitoleate levels in type 2 diabetes:
https://www.frontiersin.org/journals/clinical-diabetes-and-healthcare/articles/10.3389/fcdhc.2022.856485/full -
A new basal insulin analog designed for once-weekly dosing (Insulin Icodec):
https://pmc.ncbi.nlm.nih.gov/articles/PMC8378355/ -
Insulin icodec information on DrugBank:
https://go.drugbank.com/drugs/DB16693
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