Table 3.

Comparison of pharmacological and other relevant properties of thiazolidinedione (TZD) full PPARγ agonists and dual angiotensin II type 1 receptor blocker/selective PPARγ modulator (ARB/SPPARγM).

Parameter	TZDs†			ARBs*
	Troglitazone	Pioglitazone	Rosiglitazone	Telmisartan	Irbesartan
Primary pharmacological target	PPARγ	PPARγ	PPARγ	AT1-R	AT1-R
Type of PPARγ agonists	Full PPARγ agonists			Selective PPARγ modulator (SPPARγM)
Drug class (common names)	Thiazolidinedione (TZDs)			Angiotensin receptor blockers (ARBs)
PPARγ activation (EC50 in μM)	0.55	0.58	0.043	4.5	27
Therapeutic indication	Treatment of type 2 diabetes mellitus			Treatment of hypertension
Primary therapeutic mechanism	Increase insulin sensitivity			Lower blood pressure
Serious adverse effect (Black box warning)	Fluid retention/weight gain/heart failure			None	None
Supplier/Pharmaceutical Co.	Sigma-Aldrich, St. Louis, Mo, USA	Takeda Pharmaceuticals North America, Deerfield, Ill, USA	GlaxoSmithKline, NC, USA	Boehringer- Ingelheim Pharmaceuticals, Inc., Ridgefield, Conn, USA	Sanofi-Aventis, Bridgewater, NJ, USA

^†Thiazolidinedione full PPARγ agonists; troglitazone was withdrawn from the market (1998) because of association with rare cases of fatal hepatic failure. Rosiglitazone and pioglitazone have no such known association.

*Other FDA-approved ARBs had EC₅₀ values > 100μM (see [37, 38]). EC₅₀ values shown were determined using the standard PPARγ-GAL4 transactivation assays.