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Rosiglitazone


Mechanism of action:

Rosiglitazone is a thiazolidinedione derivative and acts as a peroxisome proliferator-activated receptor gamma, or PPAR-gamma, agonist. After entering the cell, rosiglitazone binds to the nuclear PPAR-gamma receptor. PPAR-gamma then forms a complex with the retinoid X receptor, which binds to PPAR response elements, or PPREs, on DNA and regulates the transcription of multiple metabolism-related genes. This increases insulin sensitivity in adipocytes, promotes GLUT4-related expression, and reduces the release of free fatty acids.

Reference(s):

1. Mohanty P et al. (2004). Evidence for a potent antiinflammatory effect of rosiglitazone. J Clin Endocrinol Metab. 


2. Kahn SE et al. (2006). Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N Engl J Med.

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