NCIt definition : An orally active nonpeptide renin inhibitor with antihypertensive activity. Aliskiren
selectively binds to the S3 sub-pocket of renin, an enzyme in the renin-angiotensin-aldosterone
system (RAAS) that is responsible for converting angiotensinogen to angiotensin I
(AT I). By inhibiting the activity of renin, the conversion to AT I is prevented,
which in turn prevents the conversion of AT I to AT II. This prevents arterial vasoconstriction
by AT II and inhibits the production of aldosterone by AT II. As aldosterone causes
re-uptake of sodium and water and eventually an increase in extracellular volume,
aliskiren is able to prevent the effects that contribute to an increase in blood pressure.;
Semantic type(s)