Abstract

Coformulations are a novel pharmaceutical development in diabetology. They are composed of two medicinal products, both of which maintain their distinct pharmacokinetic and pharmacodynamic properties. Currently available coformulations include combinations of basal and rapid-acting insulin, and basal and glucagon-like peptide 1 receptor agonists (GLP1RA). This review describes three coformulations which are in advanced stages of development, or are approved in certain markets. We discuss the basic and clinical pharmacology of these drugs, while describing clinical usage of the commercially available insulin degludec aspart (IDegAsp).Electronic supplementary materialThe online version of this article (doi:10.1007/s13300-015-0106-2) contains supplementary material, which is available to authorized users.

Highlights

  • Coformulations are a novel pharmaceutical development in diabetology

  • Injectable coformulations have been developed, which combine two distinct molecules in one formulation. These may be Diabetes Ther (2015) 6:101–111 from the same therapeutic class or from different therapeutic classes

  • These clinical studies were conducted in patients with both type 1 diabetes mellitus (T1DM) and type 2 diabetes mellitus (T2DM), both as once-daily (OD) and twice-daily (BID) dosing

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Summary

COFORMULATIONS IN DIABETOLOGY

Fixed dose combination (FDCs) and fixed ratio combinations (FRCs) or fixed proportion combination (FPCs) are an integral and wellaccepted part of diabetes care. Injectable coformulations have been developed, which combine two distinct molecules in one formulation These may be Diabetes Ther (2015) 6:101–111 from the same therapeutic class (e.g., a rapid acting insulin combined with a basal insulin) or from different therapeutic classes (e.g., a basal insulin combined with a glucagon-like peptide 1 receptor agonist [GLP1RA]). The word ‘‘injection’’ when used in terms of drug dosage refers to solution, suspension and emulsion, including those produced from powders or concentrated solutions Various oral coformulations such as multivitamins, vitamin B complex and certain antibiotics (e.g., co-amoxiclav) are available for intravenous use. We define injectable pharmaceutical coformulations as preparations, and which maintain their distinct pharmacological properties These are distinct from the pre-mixed insulins that have been available over the last 50 years (Table 1).

INSULIN DEGLUDEC AND INSULIN ASPART
Pharmacokinetics and Pharmacodynamics
Clinical Trial Program
No significant difference
Special Populations
INSULIN DEGLUDEC AND LIRAGLUTIDE
Other important points regarding confirmed hypoglycemia and weight change
CONCLUSION
Lixisenatide significantly improved There was a trend in weight
Findings
Not yet approved
Full Text
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