CAS: 334678-67-0

21-hydroxy Eplerenone, a key eplerenone metabolite, is produced via CYP3A4.

21-Hydroxyeplerenone is a metabolite of eplerenone, which is used to treat patients with hypertension and congestive heart failure. 21-Hydroxyeplerenone is formed by the action of cytochrome P450 3A4 (CYP3A4) on eplerenone. The concentration of 21-hydroxyeplerenone in plasma is subject to significant variation between individuals and may be an important factor for determining the appropriate dose for individual patients. In addition, CYP3A5, which has been shown to have a lower affinity for eplerenone than CYP3A4, also contributes to the formation of 21-hydroxyeplerenone. It has been proposed that measurement of the plasma levels of both metabolites can be used as markers for CYP3A activity and could be useful in monitoring drug therapy.