Rosiglitazone is an anti-diabetic drug from the thiazolidinedione class. It is being marketed as Avandia by the pharmaceutical company GlaxoSmithKline, both as a standalone preparation and in combination with metformin (Avandamet). Another combination drug approved by the FDA is Avandaryl (with glimepiride).

Like other thiazolidinediones, its mechanism of action is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPARγ. Rosiglitazone is a selective ligand of PPARγ, and has no PPARα-binding action. Apart from its effect on insulin resistance, it appears to have an anti-inflammatory effect: nuclear factor kappa-B (NFκB) levels fall and inhibitor (IκB) levels increase in patients on rosiglitazone.

Recent research has indicated that Rosiglitazone may be of benefit to a subset of sufferers of Alzheimer's disease expressing the ApoE4 allelle. This is the subject of a clinical trial currently underway by GlaxoSmithKline.

Side-effects and contraindications

A February 2007 press release by GlaxoSmithKline notes a greater incidence of fractures of the upper arms, hands and feet in female diabetics given rosiglitazone compared with those given metformin or glyburide. The information was based on data from the ADOPT trial.

An article to be published in the June 14, 2007 print issue of New England Journal of Medicine tied the use of rosiglitazone to a slightly increased risk of heart attack (odds ratio=1.43). The FDA issued an alert on May 21, 2007.[6] The findings of the study by Dr. Steven Nissen and his colleague Kathy Wolski, were considered enough of a public health matter to have caused the New England Journal of Medicine to release the findings several weeks before they appeared in print.

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