Pharmacokinetics and pharmacodynamics of insulin glargine 300 U/mL in the treatment of diabetes and their clinical relevance

ABSTRACT

Introduction: A more concentrated insulin glargine formulation, containing 300 U/mL (Gla-300) was approved in 2015 in the US and Europe for the treatment of diabetes mellitus in adults.

Areas covered: This drug evaluation focuses on the pharmacokinetics (PK) and pharmacodynamics (PD) of Gla-300 from studies published up to May 2016. The clinical relevance of this new formulation will be addressed.

Expert opinion: Gla-300 was developed to produce a flatter and more prolonged PK/PD profile compared with insulin glargine 100 U/mL (Gla-100) in order to maintain effective glycemic control and reduce the risk of hypoglycemia. Compared to Gla-100, Gla-300 achieves lower and delayed peak concentrations with a PK exposure that is more stable and evenly distributed across a 24-h dosing interval. As a consequence, Gla-300 results in a consistent glucose-lowering effect with less variability over a 24-h dosing interval, which translates to a reduction in the rate of hypoglycemia (particularly nocturnal events).

KEYWORDS:

• Euglycemic glucose clamp
• insulin glargine 100 U/ml
• insulin glargine 300 U/ml
• pharmacokinetics
• pharmacodynamics
• type 1 diabetes
• type 2 diabetes

Declaration of interest

DR Owens has received lecture fees/honoraria from Sanofi, Boehringer Ingelheim, Eli Lilly, Novo Nordisk, Mendor and Roche Diagnostics. The author has no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed. The author wishes to acknowledge the support of Oberon Ltd for figure preparation, article formatting and editing, funded by Sanofi.