Aliskiren is a first-in-class antihypertensive drug that acts by direct
inhibition of renin. It is indicated for oral administration either as monotherapy
or in combination with other antihypertensive agents. Renin catalyzes the
cleavage of angiotensin to form angiotensin I, the first and the rate-limiting step
of the RAAS. The inhibition of renin by aliskiren results in reduced levels of
angiotensin I, angiotensin II, and aldosterone, all of which contribute to the
antihypertensive effect. RAAS modulators are among some of the most
commonly prescribed antihypertensive agents to date.The most common side effect of aliskiren is diarrhea, particularly
with doses higher than 300mg daily. Unlike ACE inhibition, direct inhibition of
renin does not increase bradykinin levels. Elevated bradykinin levels are
thought to be responsible for the angioderma and cough that occur commonly
during treatment with ACE inhibitors.
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An orally active, synthetic nonpeptide renin inhibitor. Antihypertensive
liquid crystal intermediate
ChEBI: A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position.
Aliskiren, (2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methyl-propyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-8-methyl-2-propan-2-yl-nonanamide (Tekturna), is the first renin inhibitorintroduced into the U. S. market. It was approved by theFDA in 2007 for the management of hypertension.The trade name for aliskiren in the United Kingdom isRasilez.
