Clinical data
Trade names Edarbi
AHFS/ Consumer Drug Information
MedlinePlus a611028
License data
  • C (1st trimester)
    D (2nd/3rd trimester) (US)
Routes of
ATC code C09CA09 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability 60%
Metabolism CYP2C9
Biological half-life 11 hrs
Excretion 55% faeces, 42% urine
Synonyms TAK-536
CAS Number 147403-03-0 N
PubChem (CID) 9825285
ChemSpider 8001032 N
KEGG D08864 N
Chemical and physical data
Formula C25H20N4O5
Molar mass 456.46 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Azilsartan (INN) is an angiotensin II receptor antagonist used in the treatment of hypertension, developed by Takeda. It is marketed in tablet form under the trade name Edarbi as the prodrug azilsartan medoxomil (INN).

Medical uses

Azilsartan is used for the treatment of essential hypertension in adults.[1]


Azilsartan must not be used with aliskiren, a renin inhibitor, in patients with diabetes as this increases the risk of serious adverse effects. Like other antihypertensive drugs acting on the renin–angiotensin system, it is contraindicated during the second and third trimesters of pregnancy.[1][2]

Adverse effects

Common side effects include dizziness, diarrhoea and eleveted levels of the enzyme creatine kinase. More serious reactions such as angioedema are rare.[1][2]


No relevant drug interactions have been found in studies. Based on experiences with other drugs acting on the renin–angiotensin system, it is theorized that azilsartan could increase the toxicity of lithium and of other drugs increasing potassium levels, such as potassium sparing diuretics.[1][2]


Mechanism of action

Azilsartan medoxomil lowers blood pressure by blocking the action of angiotensin II at the AT1 receptor, a hormone that contracts blood vessels and reduces water excretion through the kidneys.[1]


Azilsartan medoxomil is quickly absorbed from the gut, independently of food intake. Maximal blood plasma concentrations are reached after one to three hours. The liver enzyme CYP2C9 is involved in the formation of the two main metabolites, which are pharmacologically inactive; they are the O-deethylation and decarboxylation products of azilsartan. Elimination half life is about 11 hours. 55% are excreted via the faeces, and 42% via the urine, of which 15% are present as azilsartan and the rest in form of the metabolites.[2]


Azilsartan medoxomil, the prodrug

The drug formulation contains the potassium salt of azilsartan medoxomil (codenamed TAK-491), an ester of azilsartan's carboxyl group with the alcohol (5-methyl-2-oxo-1,3-dioxol-4-yl)methanol.[2] This ester is more lipophilic than azilsartan itself.


On 25 February 2011, the U.S. Food and Drug Administration approved azilsartan medoxomil for the treatment of high blood pressure in adults.[3] On March 8, 2012, Health Canada approved the drug for mild to moderate essential hypertension.[4]


  1. 1 2 3 4 5 Haberfeld, H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag.
  2. 1 2 3 4 5 Dinnendahl, V; Fricke, U, eds. (2012). "Arzneistoff-Profile" (in German). 2 (26 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.
  3. "FDA approves Edarbi to treat high blood pressure" (Press release). U.S. Food and Drug Administration. February 25, 2011. Retrieved 2011-03-01.
  4. Notice of Decision for EDARBI
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