Rivoglitazone: A New Thiazolidinedione for the Treatment of Type 2 Diabetes Mellitus

OBJECTIVE: To review the pharmacology, pharmacokinetics, efficacy, and safety of the thiazolidinedione rivoglitazone, a peroxisome proliferator-activated receptor-gamma (PPAR-gamma) agonist, to determine its potential role in the treatment of type 2 diabetes mellitus. DATA SOURCES: A MEDLINE search (1966-February 2013) was conducted for English-language studies in humans, using the terms rivoglitazone and CS011. Abstracts presented at the American Diabetes Association and European Association for the Study of Diabetes annual meetings from 2007 to 2012 were also evaluated for relevant data. STUDY SELECTION AND DATA EXTRACTION: Articles pertinent to the pharmacology, pharmacokinetics, efficacy, and safety of rivoglitazone were reviewed. DATA SYNTHESIS: Rivoglitazone has been shown, through small clinical studies, to decrease hemoglobin A(1c) (A1C) by 0.11-1.1% when compared with placebo and may provide greater A1C reduction than pioglitazone. Rivoglitazone reduces hyperglycemia, hyperinsulinemia, and hypertriglyceridemia by acting as an agonist of PPAR-gamma. Rivoglitazone is the most potent PPAR-gamma agonist; the initial recommended dose is 1 mg daily, with adjustment as needed to a maximum dose of 2 mg daily. Additionally, rivoglitazone has a longer half-life than other PPAR-gamma agonists. Similar to those of the other PPAR-gamma agonists, rivoglitazone's adverse effects include peripheral edema and weight gain. CONCLUSIONS: Rivoglitazone is the fourth agent in the thiazolidinedione class of antidiabetes drugs. Although rivoglitazone appears to be more potent in its ability to lower A1C levels compared with other thiazolidinediones, further studies of longer duration are needed to fully assess the risks associated with this drug. Until these can be completed, we cannot recommend rivoglitazone over currently approved drugs in this class.