Key result
Candesartan cilexetil demonstrates the highest receptor affinity among available AT1-receptor blockers in vitro, providing tight and long-lasting binding to block the effects of angiotensin II.
Candesartan cilexetil exhibits tight, long-lasting binding and the highest receptor affinity among available AT1-receptor blockers in vitro.
Supports candesartan prodrug use in hypertension; leaves open comparative outcome trials vs other ARBs.
Several angiotensin II type 1 (AT 1 ) receptor blockers are now available for the treatment of hypertension. Although the agents in this class all act by blocking the AT 1 -receptor, they differ in their pharmacokinetics and binding characteristics. One of the newest AT 1 -receptor blockers, candesartan cilexetil, is administered in an inactive form and is rapidly and completely converted to the active drug, candesartan, during gastrointestinal absorption. In vitro studies have shown that candesartan has the highest receptor affinity of all the available AT 1 -receptor blockers and is not displaced from the receptor by high concentrations of angiotensin II. The tight and long-lasting binding of candesartan to the AT 1 -receptor provides effective blockade of the negative cardiovascular effects of angiotensin II.
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Thomas A. Unger (2000) conducted a review in hypertension. Candesartan cilexetil vs. Other AT1-receptor blockers was evaluated. Candesartan cilexetil demonstrates the highest receptor affinity among available AT1-receptor blockers in vitro, providing tight and long-lasting binding to block the effects of angiotensin II.
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