Candesartan cilexetil 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 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 is administered as a pro-drug that undergoes activation during gastrointestinal absorption. In clinical trials, candesartan cilexetil 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 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 to hydrochlorothiazide 12.5-25 mg/day and amlodipine 5 mg/day led to enhanced blood-pressure reductions and was well tolerated.
| Molecular Weight | 610.66 |
| Formula | C33H34N6O6 |
| CAS Number | 145040-37-5 |
| Solubility (25°C) | DMSO 52 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Febry Ardiana, et al. Candesartan cilexetil
[3] Alexander Joost, et al. Candesartan cilexetil: an update
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