Angiotensin-converting enzyme (ACE) converts angiotensin I to angiotensin II, a peptide hormone that impacts vascular smooth muscle tone and renal salt exchange, driving hypertension. Temocapril is a prodrug of the ACE inhibitor, temocaprilat (IC50 = 3.6 and 7.6 nM in isolated rat lung and aorta, respectively). Upon oral administration it is rapidly deesterified to the active form, which remains long acting until excreted in bile and urine. In clinical trials, it has been used to reduce blood pressure, improve endothelial dysfunction, and prevent vascular remodeling, as well as improve insulin sensitivity and renal function in certain hypertensive or diabetic conditions.
