Telmisartan: Unique Group of Characteristics

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Telmisartan has been shown to function as a partial agonist of the peroxisome proliferator-activated receptor-g (PPARg), in addition to its activity as an ARB.^1-4

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 telmisartan is unique in this activity.⁵ No other commercially available ARBs demonstrated activity at PPARg when tested at plasma concentrations typical of conventional oral dosing.¹

The ability of telmisartan to simultaneously block the angiotensin II receptor and activate PPARg can lead to cardiovascular protection, through a complex interaction of physiological mechanisms as illustrated below.^1,6

These properties could provide superior clinical efficacy in hypertensive patients with insulin-resistant states, such as the metabolic syndrome and type 2 diabetes. Thus, telmisartan may have additional benefits in the treatment of cardiovascular patients with metabolic pathology and associated end-organ micro- and macro-vascular complications.

This hypothesis has been explored in several small-scale clinical trials investigating the dual ARB/selective PPARg effects of telmisartan. In these studies, telmisartan has shown differential clinical metabolic effects to other ARBs, resulting in improved measures of glucose and lipid parameters than losartan, eprosartan and irbesartan.^7-9

Results from the ONTARGET^® study will demonstrate whether these improvements translate into reductions in cardiovascular morbidity and mortality.

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