Captopril (SQ-14534; SA333)

Description: Captopril (SQ 14225; SA333) is a potent angiotensin-converting enzyme (ACE) inhibitor with IC50 of 6 nM. It is the prototypical drug in the ACE class with antihypertensive efficacy commonly used in the control of blood pressure. Captopril has been shown to be an inhibitor of ACE1, but not ACE2. Captopril is also a reversible and competitive inhibitor of leukotriene A4 hydrolase. Administration of captopril inhibits the pressor response to intravenously administered angiotensin I but not that induced by angiotensin II both in normal human beings and in conscious normotensive rabbits. Captopril is proven to be a useful alternative to combination antihypertensive therapy.

References: Nat Rev Drug Discov. 2002 Aug; 1(8):621-36.