Putting the efficacy of candesartan cilexetil into perspective: a review of new comparative data

Abstract

Candesartan is one of the first angiotensin II receptor antagonists (AIIRAs) to be developed. It binds tightly to and dissociates slowly from the angiotensin subtype 1 (AT₁) receptor in vitro. These binding characteristics differ from those of losartan, which demonstrates lower affinity and faster dissociation from the AT₁ receptor. Candesartan causes long-lasting antagonism of the vascular contractile response to angiotensin II compared with irbesartan, losartan or the active metabolite of losartan – EXP-3174. While there are relatively few distinctions that can be made between the AIIRAs in terms of their pharmacokinetic profiles, the antagonistic potency of candesartan cilexetil at the AT₁ receptor over 24 h clearly differentiates it from other members of its class. These differences are reflected in the antihypertensive efficacy and duration of action of candesartan in clinical trials.