How LANTUS® Works: Long-Acting Insulin MOA

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LANTUS® is a recombinant human insulin analog that is a long-acting, parenteral blood-glucose-lowering agent. The activity of LANTUS® results in a relatively constant concentration/time profile over 24 hours with no pronounced peak. This profile is what allows LANTUS® to be dosed once a day as a patient's basal insulin. Long-acting LANTUS® provides a continuous level of insulin, mimicking the slow, steady (basal) secretion of insulin provided by the normal pancreas. LANTUS® may need to be prescribed in combination with mealtime insulins or oral hypoglycemic agents.

LANTUS® long-acting (basal) insulin differs from human insulin in that the physio/chemical properties have been modified.

The amino acid asparagine at position A21 is replaced by glycine, and two arginines are added to the C-terminus of the B-chain. The effect of these changes is to shift the isoelectric point, producing a solution that is completely soluble at pH 4.¹

When injected into the subcutaneous tissue, which has a physiological pH of 7.4, the acidic solution is neutralized. This leads to the formation of microprecipitates, or stabilized aggregates, from which small amounts of LANTUS® are slowly released. The slow dissolution of free hexamers results in the lack of a pronounced peak, which allows LANTUS® to be dosed once daily.¹

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