Aliskiren

Description

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. .

Originator

Novartis (Switzerland)

Uses

An orally active, synthetic nonpeptide renin inhibitor. Antihypertensive

Uses

liquid crystal intermediate

Definition

ChEBI: A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position.

brand name

Tekturna

General Description

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.