Azilsartan is an antagonist of the angiotensin II type 1 receptor (AT1; IC50 = 0.42 μM) and the active metabolite of azilsartan medoxomil . Azilsartan is formed from azilsartan medoxomil by hydrolysis in the gastrointestinal tract and liver. Azilsartan also acts as an inverse agonist, inhibiting angiotensin II-induced accumulation of inositol-1-phosphate in COS-7 cells expressing recombinant human AT1 (IC50 = 2.6 nM). It reduces the maximal contractile response induced by angiotensin II in isolated rabbit aortic strips (pD2 = 9.9). Azilsartan (100 ng/kg, i.v.) inhibits the angiotensin II-induced pressor response in conscious normotensive rats.
화학적 성질
White to Off-White Solid
용도
Azilsartan is an analgesic and antiinflammatory drugs containing angiotensin II antagonists.
정의
ChEBI: A benzimidazolecarboxylic acid that is benzimidazole-7-carboxylic acid substituted at position 2 by a methoxy group and at position 1 by a 2'-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl group. Used (as the prodrug, azilsartan medoxomil) f
r treatment of hypertension.
Clinical Use
Azilsartan is an orally active angiotensin II blocker which was approved and launched in Japan for
the treatment of arterial hypertension in May 2012. Azilsartan, which is marketed under the trade
name Azilva®, was discovered and developed by Takeda—the same firm which had developed and
launched a prodrug of azilsartan (azilsartan kamedoxomil, Edarbi®) in 2010. Azilsartan exhibits higher
potency and slower off-rate kinetics for type 1 angiotensin II receptors, which contributes to azilsartan’s
comparatively improved blood pressure lowering effect.
