ArticleNaunyn-Schmiedeberg's archives of pharmacology2025
GZR101, a Novel Premixed Insulin for the Treatment of Diabetes Mellitus.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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16 authors.
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Abstract
Inadequate glycemic control in patients with current premixed insulin regimens is often due to the short half-life and pronounced peak-to-trough ratio of basal insulin. This study evaluated insulin GZR33 (GZR33), an ultra-long basal insulin, and insulin GZR101 (GZR101), which is a premix of GZR33 and postprandial insulin aspart. The binding affinity of GZR33 to the human insulin receptor (hIR) was analyzed using surface plasmon resonance. Potency was tested in vivo in streptozotocin-induced T1DM rats and db/db T2DM mice, using insulin degludec (degludec, IDeg) and insulin degludec/insulin aspart (IDegAsp) as controls. GZR33 was constructed by linking a C22 fatty diacid side chain to desB30 human insulin via a 6 × oligoethylene glycol (OEG) linker. GZR33 exhibited strong hIR-A and hIR-B binding (dissociation constants: 2.86E-6 M and 1.28E-6 M). It activated IRA and IRB with EC
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