Pharmacy World & Science

, Volume 30, Issue 6, pp 741–749 | Cite as

First renin inhibitor, aliskiren, for the treatment of hypertension

  • Darren M. Triller
  • Samuel D. Evang
  • Mina Tadrous
  • Bong Kyu YooEmail author
Review Article


Aim of the review To systematically analyze the efficacy and safety of aliskiren for the treatment of hypertension in comparison to placebo, other monotherapy, and various combination therapies. Method A PubMed database (1966-June 2008) search was conducted with aliskiren as a search term with limits of humans, written in English, and in title only. Phase III pivotal clinical studies retrieved by PubMed database and resources such as printed labeling, approval letter, pharmacology reviews, and medical reviews posted in Drug@FDA website were evaluated with regard to study design and outcomes of efficacy and safety. Results Six Phase III pivotal clinical studies compared various doses of aliskiren to placebo and some studies compared aliskiren to treatment with other monotherapies or combinations. Aliskiren in doses of 300 mg showed a statistically significant reduction in both systolic and diastolic blood pressure versus placebo. Comparison to other antihypertensive treatments suggest that aliskiren doses of 150 and 300 mg may induce blood pressure changes similar to those seen with moderate doses of hydrochlorothiazide or angiotensin receptor blockers. Aliskiren in combination with angiotensin receptor blockers or hydrochlorothiazide showed additional blood pressure reduction only when higher doses of aliskiren were used. Aliskiren appears to be well tolerated, with diarrhea being the only statistically significant adverse event. Conclusion Aliskiren is a novel antihypertensive that exerts its effects through the direct inhibition of renin. Although the drug is well tolerated, its modest effects on blood pressure and the present lack of evidence of impact on objective cardiovascular outcomes appear to limit its utility in the general treatment of hypertension at this time.

Key words

Adverse events Aliskiren Blood pressure Efficacy Hypertension Renin inhibitor 



The authors wish to acknowledge the support of the Yeungnam University, South Korea.


This research was supported by the Yeungnam University research grant in 2007.

Conflicts of Interest

The authors have no conflicts of interest to declare.


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Copyright information

© Springer Science+Business Media B.V. 2008

Authors and Affiliations

  • Darren M. Triller
    • 1
  • Samuel D. Evang
    • 2
  • Mina Tadrous
    • 2
  • Bong Kyu Yoo
    • 3
    Email author
  1. 1.Pharmacy ServicesHealth Care Quality Improvement Program, IPROAlbanyUSA
  2. 2.Albany College of PharmacyAlbanyUSA
  3. 3.Department of Pharmacy Practice, College of PharmacyYeungnam UniversityKyungsanKorea

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