ArticleActa pharmaceutica Sinica. B2024
Di-PEGylated insulin: A long-acting insulin conjugate with superior safety in reducing hypoglycemic events.
Article in Acta pharmaceutica Sinica. B, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- Re-engineering insulin for oral delivery: structural modifications, advanced formulation strategies, and future directions.Drug delivery · 2026Review
- Dichotomous role of CD47-SIRPActa pharmaceutica Sinica. B · 2026Article
- Site-specific PEGylation of proteins: Insights into structural and functional changes.Acta pharmaceutica Sinica. B · 2025Review
- Nanofibrous supramolecular peptide hydrogels for controlled release of small-molecule drugs and biologics.Nature nanotechnology · 2025Article
- Design of a novel long-acting insulin analogs by acetylation modification and compared with insulin Icodec.Scientific reports · 2025Article
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Authors and funding
8 authors.
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Abstract
Although the discovery of insulin 100 years ago revolutionized the treatment of diabetes, its therapeutic potential is compromised by its short half-life and narrow therapeutic index. Current long-acting insulin analogs, such as insulin-polymer conjugates, are mainly used to improve pharmacokinetics by reducing renal clearance. However, these conjugates are synthesized without sacrificing the bioactivity of insulin, thus retaining the narrow therapeutic index of native insulin, and exceeding the efficacious dose still leads to hypoglycemia. Here, we report a kind of di-PEGylated insulin that can simultaneously reduce renal clearance and receptor-mediated clearance. By impairing the binding affinity to the receptor and the activation of the receptor, di-PEGylated insulin not only further prolongs the half-life of insulin compared to classical mono-PEGylated insulin but most importantly, increases its maximum tolerated dose 10-fold. The target of long-term glycemic management
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