The uses and biological activity of Candesartan cilexetil

Description

Candesartan cilexetil is an off-white powder that is almost insoluble in water. Its molecular formula is C33H34N6O6. Angiotensin II receptor blockers (ARB) are a new class of drugs with increasing use in treating hypertension. Candesartan cilexetil is among the newest drugs in the class including losartan, irbesartan, and valsartan[1].

Uses

Candesartan is approved by the FDA for the management of hypertension in adults. This may be used to treat hypertension, isolated systolic hypertension, left ventricular hypertrophy, and diabetic nephropathy. It may also be used as an alternative agent for the treatment of heart failure, systolic dysfunction, myocardial infarction, and coronary artery disease. In particular, candesartan cilexetil might be a potential antibacterial agent for the treatment of S. aureus-associated infections[2]. This drug had strong antimicrobial activity against S. aureus with minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations (MBCs) of 8–16 μg/ml and 16–32 μg/ml.

Biological activity

Candesartan is a potent and selective angiotensin II type 1 receptor blocker that binds tightly to and dissociates slowly from the AT1 receptor. Candesartan cilexetil is a prodrug of Candesartan and is converted completely into the active metabolite candesartan during gastrointestinal absorption, whereas losartan is converted partially by hepatic metabolism into the more active compound EXP 3174. Candesartan cilexetil has more than 1000 times more affinity for the angiotensin II, type AT1 receptor ARBs, and the binding affinity and competitive angiotensin II receptor antagonism is stronger than that of losartan[3].

Adverse effects

Candesartan appears to be very well tolerated. No substantial changes in heart rate or orthostatic blood pressure have been observed. Adverse effects reported in clinical trials have been described as mild to moderate and include headache, lightheadedness, dizziness, nausea, diarrhea, and transient elevations in serum liver transaminases.

References

[1]Stoukides, and C. "Candesartan cilexetil: an angiotensin II receptor blocker. " Annals of Pharmacotherapy 33. 12(1999):1287-1298.

[2] Xu L., "Repurposing Candesartan Cilexetil as Antibacterial Agent for MRSA Infection." Frontiers in Microbiology (2021).

[3] Unger, Thomas. "Significance of angiotensin type 1 receptor blockade: why are angiotensin II receptor blockers different?." American Journal of Cardiology 84.10A(1999):9S.