MICARDIS®: Unique Group of Characteristics
In addition to it’s long half-life, large volume of distribution, high lipophilicity and selective AT1 blockade, MICARDIS® has also been shown to function as a partial agonist of PPARg, in addition to its activity as an ARB.1-4
The peroxisome proliferator-activated receptor-g (PPARg) plays an important role in the regulation of carbohydrate and lipid metabolism. It has been shown that ligands of PPARg can improve insulin sensitivity, reduce triglyceride levels, and decrease the risk for atherosclerosis.1 For this reason, PPARg is a well known target of insulin-sensitizing drugs used to treat type 2 diabetes.
Results from a study examining the ability of different ARBs to activate PPARg in an in vitro assay showed that MICARDIS® is unique in this activity. No other commercially available ARBs demonstrated activity at PPARg when tested at plasma concentrations typical of conventional oral dosing.1
The ability of MICARDIS® to block the angiotensin II receptor and simultaneously activate PPARg confers potential benefits beyond blood pressure lowering, which could include:
- Increased insulin sensitivity
- Improved lipid profile
- Improved anti-inflammatory profile
- Improved anti-atherogenic risk profile
These properties could provide superior clinical efficacy in hypertensive patients with insulin-resistant states, such as the metabolic syndrome and type 2 diabetes. Thus, MICARDIS® may have added benefits in treating cardiovascular patients with metabolic pathology and associated end-organ micro- and macrovascular complications.
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