Abasaglar ® (insulin glargin)

För fullständig produktresumé för Abasaglar® se FASS.

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Abasaglar® (insulin glargin): verkningsmekanism

Metabolismen av Abasaglar ger 2 aktiva metaboliter, M1 och M2, som har en in vitro-aktivitet som liknar insulin.

Detailed Information

Abasaglar is a human insulin analogue designed to have a low solubility at neutral pH. It is completely soluble at the acidic pH of the Abasaglar injection solution (pH 4).1

After injection of Abasaglar into the subcutaneous tissue, the acidic solution is neutralised, leading to formation of micro-precipitates from which small amounts of Abasaglar are continuously released.1

Abasaglar has a slow and prolonged absorption and a relatively constant concentration/time profile over 24 hours with no pronounced peak.1

Insulin glargine is metabolized at the carboxyl terminus of the beta chain with formation of 2 active metabolites: M1 and M2. The in vitro activity of M1 and M2 are similar to that of insulin.1

Insulin Receptor Binding

Abasaglar is very similar to human insulin with respect to insulin receptor binding kinetics; therefore, Abasaglar can be considered to mediate the same type of effect via the insulin receptor as insulin.2

Insulin-like Growth Factor 1 Receptor Binding

The potency of IGlar in stimulating human IGF-1R autophosphorylation is approximately 5-fold greater than human insulin. However, the potency of IGlar for autophosphorylation of the same receptor is approximately 30-fold lower than the potency of IGF-1. The glargine metabolites, M1 and M2, have comparable mitogenic potencies to human insulin.3

The therapeutic IGlar concentration found in healthy patients and those with T1DM was similar to the levels of free circulating IGF-1 due to 99% of IGF-1 being bound by IGF-binding proteins 1 to 6. However, due to reduced affinity for the IGF-1R, IGlar is not likely to compete with IGF-1 at this receptor.3

References

1. Abasaglar [summary of product characteristics]. Eli Lilly Nederland B.V., The Netherlands.

2. Data on file, Eli Lilly and Company and/or one of its subsidiaries.

3. Sommerfeld MR, Müller G, Tschank G, et al. In vitro metabolic and mitogenic signaling of insulin glargine and its metabolites. PLoS One. 2010;5(3):e9540. http://dx.doi.org/10.1371/journal.pone.0009540

Glossary

Abasaglar = Abasaglar® (insulin glargine injection) 100 units/mL

IGF = insulin-like growth factor

IGF-1 = insulin-like growth factor 1

IGF-1R = insulin-like growth factor 1 receptor

IGlar = insulin glargine

M1 = 21A-Gly-human insulin

M2 = 21A-Gly-des-30B-Thr-human insulin

SC = subcutaneous

T1DM = type 1 diabetes mellitus

Datum fӧr senaste ӧversyn 2019 M01 10


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