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Related Experiment Video

Updated: Jul 8, 2026

Improved Renal Denervation Mitigated Hypertension Induced by Angiotensin II Infusion

Improved Renal Denervation Mitigated Hypertension Induced by Angiotensin II Infusion

Published on: May 26, 2022

Antihypertensive therapy with aliskiren.

F C Luft¹, M H Weinberger

¹Experimental and Clinical Research Center, Medical Faculty of the Charité and Max Delbrück Center for Molecular Medicine, HELIOS Klinikum Berlin-Buch, Berlin, Germany. luft@charite.de

Kidney International

|December 28, 2007

Summary

Aliskiren is a novel antihypertensive drug that effectively lowers blood pressure by inhibiting renin. Its favorable pharmacokinetic profile and lack of drug interactions make it a promising therapeutic option.

Related Experiment Videos

Last Updated: Jul 8, 2026

Improved Renal Denervation Mitigated Hypertension Induced by Angiotensin II Infusion

Improved Renal Denervation Mitigated Hypertension Induced by Angiotensin II Infusion

Published on: May 26, 2022

Area of Science:

Pharmacology
Cardiovascular Medicine
Drug Development

Background:

The renin-angiotensin system (RAS) is a key target for hypertension treatment.
Previous attempts to inhibit the RAS at the renin step faced challenges with efficacy and bioavailability.
Aliskiren emerged as a novel, orally active direct renin inhibitor.

Purpose of the Study:

To introduce Aliskiren, the first in a new class of antihypertensive drugs.
To discuss its mechanism of action, pharmacokinetics, and clinical implications.
To highlight its potential role in combination therapy for hypertension.

Main Methods:

Aliskiren's chemical properties and molecular weight (610 Da) were detailed.
Its high affinity for the human renin enzymatic site and long half-life (~40 h) were noted.
Metabolism (not by CYP P450) and excretion routes (primarily fecal) were described.

Main Results:

Aliskiren demonstrates a 3% bioavailability, which is clinically manageable with continuous administration.
It does not require dose adjustments for renal or hepatic impairment, age, ethnicity, or drug interactions.
Blood pressure reduction with aliskiren monotherapy is comparable to existing treatments.
Combination therapy with other antihypertensives (ARB, ACEi, diuretics, CCBs) resulted in further blood pressure reduction.

Conclusions:

Aliskiren effectively inhibits the renin-angiotensin system at its rate-limiting step.
Its unique pharmacokinetic profile offers clinical advantages, including convenience and potential for broader use.
Further studies are ongoing to evaluate its long-term cardiovascular and renal benefits.