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

Approved by the FDA for Marketing in the USA

Randa Hilal-Dandan

Disclosures

AccessMedicine from McGraw-Hill 

In This Article

Pharmacodynamics

Azilsartan reduces angiotensin II-induced contraction of rabbit aortic strips in a dose-dependent manner.[9] Functional binding studies indicate that azilsartan is highly selective for AT1 receptors with an IC50 of 2.6 nM. The antagonistic effects of azilsartan on the AT1 receptor are insurmountable. Azilsartan dissociates slowly from the receptor; azilsartan binding persists after washout (IC50~2.6 nM before washout and ~7.4 nM after washout) compared to binding with olmesartan (IC50 ~6.7 nM before washout and ~242 nM after washout) or valsartan (IC50 ~45 nM before washout and >10,000 nM after washout).[9] Azilsartan also inhibits angiotensin II-induced inositol phosphate accumulation with an IC50 ~9.2 nM, an effect that also persists after washout (IC50 ~81 nM). Azilsartan can decrease inositol phosphate accumulation of constitutively active AT1 receptors, suggesting that the drug may act as an inverse agonist.[9]

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