Aliskiren

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Aliskiren
Systematic (IUPAC) name
(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
Identifiers
CAS number	173334-57-1
ATC code	C09XA02 C09XA52
PubChem	5493444
Chemical data
Formula	C30H53N3O6
Mol. mass	551.758 g/mol
Pharmacokinetic data
Bioavailability	Low (approximately 2.5%)
Metabolism	Hepatic, CYP3A4-mediated
Half life	24 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C in first trimester D in second and third trimesters
Legal status	℞-only(US)
Routes	Oral

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Overview

Aliskiren (INN) is a first in class renin inhibitor co-developed by the Swiss pharmaceutical companies Novartis and Speedel.^[1][2] It was approved by the U.S. Food and Drug Administration in 2007 for the treatment of hypertension.^[3] The trade name for aliskiren is Tekturna in the USA, and Rasilez in the UK.

Adverse effects

• Angioedema
• Hyperkalemia (particularly when used with ACE inhibitors in diabetic patients)
• Hypotension (particularly in volume-depleted patients)
• Diarrhea and other GI symptoms
• Rash, elevated uric acid, gout, and renal stones.

A rare adverse event was allergic swelling of the face, lips or tongue and difficulty breathing, side effects that are common with other drugs for hypertension that act directly on the renin-angiotensin system. ^[4]

Contraindications

As with ACE inhibitors, renin inhibitors should not be used in pregnancy, specifically the second and third trimesters, during which they will interfere with fetal kidney development and lead to oligohydramnios.

Aliskiren has not yet been evaluated in patients with significantly impaired renal function.

Drug Interactions

Minor substrate of CYP3A4:

• Reduces furosemide blood concentration.
• Atorvastatin or ketoconazole may increase blood concentration.

References

1. ↑ Gradman A, Schmieder R, Lins R, Nussberger J, Chiang Y, Bedigian M (2005). "Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients". Circulation 111 (8): 1012-8. PMID 15723979.
2. ↑ Straessen JA, Li Y, and Richart T (2006). "Oral Renin Inhibitors". Lancet 368 (9545): 1449-56. PMID 17055947.
3. ↑ "First Hypertension Drug to Inhibit Kidney Enzyme Approved", CBC, March 6, 2007. 
4. ↑ FDA approves renin inhibitor aliskiren for hypertension. RxDrug News (2007).

External links

• Tekturna U.S. prescribing informationPDF (143 KiB) at the U.S. Food and Drug Administration website
• Aliskiren at KEGG Ligand Database
• MeSH aliskiren
• Speedel [3]

v • d • e Agents acting on the renin-angiotensin system (C09)
ACE inhibitors	Benazepril • Captopril • Delapril • Enalapril • Fosinopril • Imidapril • Lisinopril • Moexipril • Perindopril • Quinapril • Ramipril • Spirapril • Temocapril • Trandolapril • Zofenopril
Angiotensin II receptor antagonists (AIIRA)	Candesartan • Eprosartan • Irbesartan • Losartan • Olmesartan • Tasosartan • Telmisartan • Valsartan
Renin inhibitors	Aliskiren • Remikiren

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