Description
Aliskiren is a direct renin inhibitor that exhibits antihypertensive, antithrombotic, and anti-angiogenic activities. Aliskiren binds to the S3bp binding site of renin, inhibiting its ability to cleave angiotensinin into angiotensin I, therefore preventing the formation of angiotensin II and resulting contraction of arterial smooth muscle. This compound is a vasodilator, decreasing plasma volume and blood pressure in vivo. In animal models of lupus nephritis, aliskiren attenuated proteinuria by decreasing inflammatory cytokine levels and glomerular inflammation. Additionally, in separate animal studies, aliskiren decreases VEGF levels, improves insulin resistance, and prevents development of venous thrombosis.