Albiglutide

Albiglutide is a long acting GLP-1 receptor agonist (GLP-1 RA) administered by weekly injection and approved for use in type 2 diabetes. It has less gastrointestinal side effects than other GLP-1 RAs in current use but does not improve HbA1c or promote weight loss to the same extent as some competitor agents. Area covered: The current use of albiglutide is discussed. The review encompassed a search of PubMed and a thorough analysis of the European Union and US Food and Drug Administration approval documents. Expert opinion: Unlike competitor agents, the gastrointestinal side effects of albiglutide are not much greater than placebo. It has been studied and appears safe at all stages of renal failure. There exists concern about an imbalance of pancreatitis cases in the approval program as well as injection site reactions which led to discontinuance of therapy in up to 2% of participants. A large long-term study is now underway to determine if albiglutide, with its relatively favorable GI tolerance, has a place in the treatment of patients with increased risk of cardiovascular events. At present, albiglutide is a safe agent to introduce GLP-1 RA treatment into the regimen for type 2 diabetes patients and may be the GLP-1 agent of choice in patients with renal insufficiency.

Albiglutide is a long-acting, glucagon-like peptide-1 receptor agonist for subcutaneous administration with a recommended dose of 30-50 mg once weekly. The aim of this article is to outline the pharmacokinetic and pharmacodynamic properties of albiglutide including the clinical efficacy and safety data underlying the approval of albiglutide for the treatment of type 2 diabetes mellitus in both Europe and USA. Albiglutide is cleared from the circulation (by a mechanism partially dependent on renal function) with an elimination half-life of 5 days, allowing once-weekly administration. In the clinical trial program called HARMONY, albiglutide demonstrated placebo-corrected reductions in glycosylated hemoglobin of 0.8-1.0%. In addition, reductions in fasting plasma glucose in the range of 1.3-2.4 mmol/L compared with placebo were reported. Albiglutide caused weight reductions at a level comparable to placebo in the HARMONY trials, possibly related to limited central nervous system penetration of the large albiglutide molecule. Albiglutide demonstrated a generally favorable safety profile, although with a signal of an increased risk of pancreatitis. The well-known adverse events related to glucagon-like peptide-1 receptor activation such as nausea, diarrhea, and vomiting were less frequent with albiglutide compared with another glucagon-like peptide-1 receptor agonist, liraglutide, but slightly more frequent following treatment with albiglutide than with placebo or active comparators from other classes of anti-hyperglycemic drugs. The full risk-benefit profile for albiglutide used in treating type 2 diabetes will not be clear until reporting of the long-term cardiovascular outcome trial (HARMONY Outcome) with planned completion in 2019.

The glucagon-like peptide 1 (GLP-1) receptor agonists are a new class of antidiabetic drugs that provide the benefits of decreasing HbA1c and plasma glucose concentrations, stimulating insulin secretion with a very low risk of hypoglycemia, and promoting weight loss. With the exception of once-weekly exenatide, currently available GLP-1 receptor agonists are administered once or twice daily by injection. Albiglutide is a new GLP-1 receptor agonist recently approved in the U.S. (Tanzeum™) and European Union (Eperzan®) for the treatment of patients with type 2 diabetes with a dosage of 30 mg once weekly, which may be increased to 50 mg if the glycemic response is inadequate. Clinical trials showed that albiglutide once weekly delayed gastric emptying, mildly decreased body weight and had similar efficacy in the reduction of HbA1c as comparators, but it failed to demonstrate noninferiority to liraglutide. Albiglutide exhibits an acceptable safety profile, although it is associated with more frequent gastrointestinal complaints (e.g., nausea, diarrhea, vomiting) and injection-site reactions. Immunogenicity (i.e., testing positive for anti-drug antibody) was observed in 5.5% of subjects but it was not associated with increased adverse events. Long-term studies are needed to fully assess potential adverse events.