Drug intelligence / Profile preview

telmisartan

Development stage
Approved
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Telmisartan is an orally active small molecule angiotensin II receptor blocker (ARB) used primarily to treat high blood pressure (hypertension), heart failure, and to reduce the risk of cardiovascular events such as heart attack and stroke in patients at increased risk. It works by selectively blocking the binding of angiotensin II to the type 1 angiotensin II receptor (AT1) in vascular smooth muscle and adrenal gland tissue. This blockade leads to vasodilation and reduced aldosterone secretion, thereby lowering blood pressure. Telmisartan has a much higher affinity for AT1 than AT2 receptors (>3,000-fold). In addition to its ARB activity, telmisartan acts as a partial agonist of peroxisome proliferator-activated receptor gamma (PPARγ), which may confer additional metabolic benefits such as improved insulin sensitivity and lipid metabolism[2][4][5][6]. The drug is available by prescription only.

Brand names
MicardisActelsar HctMicardis-hctPritorTwynsta
Other names
THP-00103THP00103THP 00103
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)AGTR1 (Angiotensin II Type-1 receptor)

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