Azilsartan (EDARBI): A New Angiotensin Receptor Blocker (ARB) for Hypertension

Approved by the FDA for Marketing in the USA

Randa Hilal-Dandan


AccessMedicine from McGraw-Hill 

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Azilsartan (EDARBI, Takeda Pharmaceutical) is an Angiotensin Receptor Blocker (ARB) approved by the FDA in February 2011 for the treatment of hypertension.[1,2,3] Azilsartan medoxomil (Figure 1) is a prodrug that is hydrolyzed in the GI tract during absorption into the active drug azilsartan (Figure 2). The drug is available in 40 mg and 80 mg doses. At the recommended dose of 80 mg once a day, azilsartan medoxomil is superior to the maximal doses of other ARBs such as valsartan and olmesartan in lowering blood pressure.[2,4,5] Two features of azilsartan likely contribute to its enhanced efficacy clinically: a high affinity for the AT1 receptor; and some inverse agonist activity.[9] The commercial tablets contain the potassium salt of azilsartan medoxomil, also known as azilsartan kamedoxomil.

Figure 1. Chemical Structure of Azilsartan Medoxomil (PubChem CID: 11238823)

Figure 2. Chemical Structure of Azilsartan (PubChem CID: 9825285)