Renin inhibitor

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 cells 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^[1]. 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.

Examples

• Aliskiren^[2]
• Remikiren

See also

• Discovery and development of renin inhibitors

References

External links

• Renin inhibitor aliskiren leads to dose-dependent blood pressure reductions - medicalnewstoday.com.