Renin inhibitor
Encyclopedia
Renin inhibitor, or inhibitors of renin
, are a new group of pharmaceuticals that are used primarily in treatment of hypertension
.
They act on the juxtaglomerular cell
s of kidney
, which produce renin in response to decreased blood flow
.
Aliskiren
is a first-in-class oral renin inhibitor developed by Novartis
in conjunction with the biotech company Speedel. It was approved by the US Food and Drug Administration
in 2007. It is an octanamide, is the first known representative of a new class of non-peptide, low-molecular weight, orally active transition-state renin inhibitors. Designed through the use of molecular modeling techniques, it is a potent and specific in vitro inhibitor of human renin (IC50 in the low nanomolar range), with a plasma half-life of ≈24 hours. Aliskiren has good water solubility and low lipophilicity and is resistant to biodegradation by peptidases in the intestine, blood circulation, and the liver. It was approved by the United States FDA on 6 March 2007, and for use in Europe on 27 August 2007. Its trade name is Tekturna in the USA, and Rasilez in the UK.
Renin
Renin , also known as an angiotensinogenase, is an enzyme that participates in the body's renin-angiotensin system -- also known as the Renin-Angiotensin-Aldosterone Axis -- that mediates extracellular volume , and arterial vasoconstriction...
, are a new group of pharmaceuticals that are used primarily in treatment of hypertension
Hypertension
Hypertension or high blood pressure is a cardiac chronic medical condition in which the systemic arterial blood pressure is elevated. What that means is that the heart is having to work harder than it should to pump the blood around the body. Blood pressure involves two measurements, systolic and...
.
They act on the juxtaglomerular cell
Juxtaglomerular cell
The juxtaglomerular cells are cells in the kidney that synthesize, store, and secrete the enzyme renin. They are specialized smooth muscle cells in the wall of the afferent arteriole that delivers blood to the glomerulus...
s of kidney
Kidney
The kidneys, organs with several functions, serve essential regulatory roles in most animals, including vertebrates and some invertebrates. They are essential in the urinary system and also serve homeostatic functions such as the regulation of electrolytes, maintenance of acid–base balance, and...
, which produce renin in response to decreased blood flow
Blood flow
Blood flow is the continuous running of blood in the cardiovascular system.The human body is made up of several processes all carrying out various functions. We have the gastrointestinal system which aids the digestion and the absorption of food...
.
Aliskiren
Aliskiren
Aliskiren is the first in a class of drugs called direct renin inhibitor. Its current licensed indication is essential hypertension....
is a first-in-class oral renin inhibitor developed by Novartis
Novartis
Novartis International AG is a multinational pharmaceutical company based in Basel, Switzerland, ranking number three in sales among the world-wide industry...
in conjunction with the biotech company Speedel. It was approved by the US Food and Drug Administration
Food and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...
in 2007. It is an octanamide, is the first known representative of a new class of non-peptide, low-molecular weight, orally active transition-state renin inhibitors. Designed through the use of molecular modeling techniques, it is a potent and specific in vitro inhibitor of human renin (IC50 in the low nanomolar range), with a plasma half-life of ≈24 hours. Aliskiren has good water solubility and low lipophilicity and is resistant to biodegradation by peptidases in the intestine, blood circulation, and the liver. It was approved by the United States FDA on 6 March 2007, and for use in Europe on 27 August 2007. Its trade name is Tekturna in the USA, and Rasilez in the UK.
External links
- Renin inhibitor aliskiren leads to dose-dependent blood pressure reductions - medicalnewstoday.com.