Research Area: Cardiovascular Disease
Biological Activity:
Candesartan cilexetil (Atacand) is a specific nonpeptide Ang II receptor (ATR) antagonist and the prodrug of candesartan which is an ATR antagonist with an IC50 of 15 µg/kg. Candesartan cilexetil (Atacand) efficacy is entirely due to its active metabolite candesartan (CV-11794) and is dose-dependent over the range of 1–8 mg and its clinical antihypertensive dose is stated to be around 4 mg/day.Candesartan cilexetil (Atacand) is administered as a pro-drug that undergoes activation during gastrointestinal absorption. In clinical trials, candesartan cilexetil (Atacand) has produced a dose-dependent effect when given in dosages of 2-32 mg/day. Observed trough-to-peak blood pressure ratios support a once-daily dosage regimen. The antihypertensive effect of candesartan cilexetil (Atacand) 4-16 mg/day was as great as that of enalapril 10-20 mg/day and amlodipine 5 mg/day and larger than that of losartan potassium 50 mg/day. Adding candesartan cilexetil (Atacand)  to hydrochlorothiazide 12.5-25 mg/day and amlodipine 5 mg/day led to enhanced blood-pressure reductions and was well tolerated. [1][2]