Albiglutide: new once-weekly GLP-1 receptor agonist for diabetes

Eperzan (albiglutide) is indicated for the treatment of type II diabetes in adults as monotherapy or in combination with other antidiabetic agents.

Eperzan should be injected subcutaneously into the abdomen, thigh or upper arm, on the same day each week. | SCIENCE PHOTO LIBRARY
Eperzan should be injected subcutaneously into the abdomen, thigh or upper arm, on the same day each week. | SCIENCE PHOTO LIBRARY

Eperzan can be prescribed when diet and exercise have failed to adequately control glucose levels in patients in whom metformin is contraindicated or not tolerated. It can also be used with other hypoglycaemic agents when these, combined with diet and exercise, do not provide sufficient control.

Albiglutide is a recombinant protein consisting of two copies of a 30-amino acid sequence of modified human GLP-1 genetically fused to human albumin. It acts by enhancing glucose-dependent insulin secretion and slowing gastric emptying, reducing postprandial glucose excursions and lowering fasting glucose.

Further information
View Eperzan drug record 

Manufacturer: GlaxoSmithKline

Eperzan is available as 30mg and 50mg pens containing powder and solvent for reconstitution. Like Bydureon (exenatide) and Trulicity (dulaglutide), it is given once weekly.

Monotherapy

Significant HbA1c reduction 

, a randomised phase III study (n=309), compared the effects of once-weekly subcutaneous injection of albiglutide 30mg or 50mg or placebo as monotherapy. Over the 52-week treatment period, HbA1c decreased in both albiglutide groups and increased in the placebo group. The treatment difference was significant for both doses of the GLP-1 agonist (albiglutide 30mg: -0.84% [95% CI -1.11% to -0.58%], p<0.0001; albiglutide 50mg: -1.04% [-1.31% to -0.77%], p<0.0001).

There was no significant difference in weight loss between the treatment and placebo groups at week 52.

Hyperglycaemic rescue

The time to hyperglycaemic rescue differed significantly between patients receiving albiglutide (30mg or 50mg) and those given placebo (p<0.0001). At week 52, a greater proportion of patients required rescue therapy in the placebo group (50.5%) than in the albiglutide 30mg (20.0%) or 50mg (15.5%) groups. In the weeks leading up to this, the probability of rescue was up to 55.7% in patients receiving placebo compared with a maximum of 21.7% in patients using albiglutide.

A higher proportion of patients experienced adverse effects with albiglutide than with placebo. For this reason more patients in the albiglutide groups withdrew from the study. The most common reasons for withdrawal in the higher-dose group were gastrointestinal events and injection site reactions.

In combination with metformin

A placebo-controlled study compared weekly albiglutide with daily sitagliptin, glimepiride and placebo when used in combination with metformin.  used change in HbA1c from baseline at week 104 as the primary endpoint; fasting plasma glucose, weight and time to hyperglycaemic rescue were secondary endpoints.

Results showed that albiglutide, when added to metformin, was superior in terms of HbA1c reduction to placebo (-0.9% [95% CI -1.2% to -0.7%], p<0.0001), sitagliptin (-0.4% [95% CI -0.5% to -0.2%], p=0.0001) and glimepiride (-0.3% [95% CI -0.5% to -0.1%], p=0.0033). Patients on glimepiride gained weight whereas those on albiglutide, placebo or sitagliptin lost weight; the treatment difference between albiglutide and glimepiride was significant (p<0.0001). 

A smaller proportion of patients received hyperglycaemic rescue in the albiglutide group (25.8%) than in the placebo or sitagliptin groups. The proportion of patients requiring hyperglycaemic rescue was highest in the placebo group (59.2%), followed by the sitagliptin (36.4%) and glimepiride (32.7%) groups. 

Other regimens

Albiglutide has also been studied as an add-on to pioglitazone with or without metformin (); metformin with or without a sulfonylurea (); metformin and a sulfonylurea (); insulin glargine (); and metformin, pioglitazone or a sulfonylurea ().

In ranging from mild to severe, albiglutide had a significantly greater effect on HbA1c from baseline to week 26 than daily sitagliptin (-0.83% vs -0.52%, p=0.0003), with a comparable safety profile.

Acute pancreatitis

Acute pancreatitis was the most serious adverse effect of albiglutide in clinical trials. As with all GLP-1 receptor agonists, patients should be informed of the symptoms of pancreatitis. If pancreatitis is suspected, albiglutide should be discontinued and only restarted when pancreatitis has been ruled out. Care should be taken when albiglutide is used in patients with a history of pancreatitis.

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