Identification

Name
Aliskiren
Accession Number
DB09026  (DB01258)
Type
Small Molecule
Groups
Approved, Investigational
Description

Aliskiren is the first in a class of drugs called direct renin inhibitors. Its current licensed indication is essential (primary) hypertension. While used for high blood pressure, other better studied medications are typically recommended due to concerns of higher side effects and less evidence of benefit. In December 2011, Novartis halted a clinical trial of the drug after discovering increased incidence of nonfatal stroke, kidney complications, high blood potassium, and low blood pressure in people with diabetes and kidney impairment.

Structure
Thumb
Synonyms
  • Aliskireno
Product Ingredients
IngredientUNIICASInChI Key
Aliskiren hemifumarateC8A0P8G029173334-58-2KLRSDBSKUSSCGU-KRQUFFFQSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RasilezTablet, film coated150 mgOralNoden Pharma Dac2007-08-22Not applicableEu
RasilezTablet150 mgOralNoden Pharma Dac2007-11-26Not applicableCanada
RasilezTablet, film coated150 mgOralNoden Pharma Dac2007-08-22Not applicableEu
RasilezTablet, film coated300 mgOralNoden Pharma Dac2007-08-22Not applicableEu
RasilezTablet, film coated150 mgOralNoden Pharma Dac2007-08-22Not applicableEu
RasilezTablet, film coated300 mgOralNoden Pharma Dac2007-08-22Not applicableEu
RasilezTablet, film coated150 mgOralNoden Pharma Dac2007-08-22Not applicableEu
RasilezTablet, film coated300 mgOralNoden Pharma Dac2007-08-22Not applicableEu
RasilezTablet, film coated300 mgOralNoden Pharma Dac2007-08-22Not applicableEu
RasilezTablet, film coated150 mgOralNoden Pharma Dac2007-08-22Not applicableEu
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AmturnideAliskiren hemifumarate (300 mg/1) + Amlodipine besylate (5 mg/1) + Hydrochlorothiazide (25 mg/1)Tablet, film coatedOralNovartis2010-12-212016-03-31Us
AmturnideAliskiren hemifumarate (150 mg/1) + Amlodipine besylate (5 mg/1) + Hydrochlorothiazide (12.5 mg/1)Tablet, film coatedOralNovartis2010-12-212015-09-30Us
AmturnideAliskiren hemifumarate (300 mg/1) + Amlodipine besylate (10 mg/1) + Hydrochlorothiazide (25 mg/1)Tablet, film coatedOralNovartis2010-12-212016-01-31Us
AmturnideAliskiren hemifumarate (300 mg/1) + Amlodipine besylate (10 mg/1) + Hydrochlorothiazide (12.5 mg/1)Tablet, film coatedOralNovartis2010-12-212015-10-31Us
AmturnideAliskiren hemifumarate (300 mg/1) + Amlodipine besylate (5 mg/1) + Hydrochlorothiazide (12.5 mg/1)Tablet, film coatedOralNovartis2010-12-212016-01-31Us
Rasilez HctAliskiren (150 mg) + Hydrochlorothiazide (25 mg)Tablet, film coatedOralNoden Pharma Dac2009-01-16Not applicableEu
Rasilez HctAliskiren (300 mg) + Hydrochlorothiazide (12.5 mg)Tablet, film coatedOralNoden Pharma Dac2009-01-16Not applicableEu
Rasilez HCTAliskiren (150 mg) + Hydrochlorothiazide (25 mg)TabletOralNoden Pharma Dac2009-11-24Not applicableCanada
Rasilez HctAliskiren (300 mg) + Hydrochlorothiazide (12.5 mg)Tablet, film coatedOralNoden Pharma Dac2009-01-16Not applicableEu
Rasilez HctAliskiren (300 mg) + Hydrochlorothiazide (25 mg)Tablet, film coatedOralNoden Pharma Dac2009-01-16Not applicableEu
Categories
UNII
502FWN4Q32
CAS number
173334-57-1
Weight
Average: 551.7583
Monoisotopic: 551.393436443
Chemical Formula
C30H53N3O6
InChI Key
UXOWGYHJODZGMF-QORCZRPOSA-N
InChI
InChI=1S/C30H53N3O6/c1-19(2)22(14-21-10-11-26(38-8)27(15-21)39-13-9-12-37-7)16-24(31)25(34)17-23(20(3)4)28(35)33-18-30(5,6)29(32)36/h10-11,15,19-20,22-25,34H,9,12-14,16-18,31H2,1-8H3,(H2,32,36)(H,33,35)/t22-,23-,24-,25-/m0/s1
IUPAC Name
(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2,2-dimethylethyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-8-methyl-2-(propan-2-yl)nonanamide
SMILES
COCCCOC1=C(OC)C=CC(C[C@@H](C[C@H](N)[C@@H](O)C[C@@H](C(C)C)C(=O)NCC(C)(C)C(N)=O)C(C)C)=C1

Pharmacology

Indication

For the treatment of hypertension, to lower blood pressure.

Associated Conditions
Pharmacodynamics

In placebo controlled clinical trials, plasma renin activity (PRA) was decreased in a range of 50% to 80%. This reduction in PRA was not dose‐related and did not correlate with blood pressure reductions. The clinical implications of the differences in effect on PRA are not known.

Mechanism of action

Renin is secreted by the kidney in response to decreases in blood volume and renal perfusion. Renin cleaves angiotensinogen to form the inactive decapeptide angiotensin I (Ang I). Ang I is converted to the active octapeptide angiotensin II (Ang II) by ACE and non‐ACE pathways. Ang II is a powerful vasoconstrictor and leads to the release of catecholamines from the adrenal medulla and prejunctional nerve endings. It also promotes aldosterone secretion and sodium reabsorption. Together, these effects increase blood pressure. Ang II also inhibits renin release, thus providing a negative feedback to the system. This cycle, from renin through angiotensin to aldosterone and its associated negative feedback loop, is known as the renin‐angiotensin‐aldosterone system (RAAS). Aliskiren is a direct renin inhibitor, decreasing plasma renin activity (PRA) and inhibiting the conversion of angiotensinogen to Ang I. Whether aliskiren affects other RAAS components, e.g., ACE or non‐ACE pathways, is not known. All agents that inhibit the RAAS, including renin inhibitors, suppress the negative feedback loop, leading to a compensatory rise in plasma renin concentration. When this rise occurs during treatment with ACEIs and ARBs, the result is increased levels of PRA. During treatment with aliskiren, however, the effect of increased renin levels is blocked so that PRA, Ang I and Ang II are all reduced, whether aliskiren is used as monotherapy or in combination with other antihypertensive agents.

TargetActionsOrganism
ARenin
inhibitor
Human
Absorption

Poor, with a bioavailability of about 2.5%.

Volume of distribution
Not Available
Protein binding

47-51%

Metabolism

Approximately 80% of the drug in plasma following oral administration is unchanged. Cytochrome P450 (CYP) 3A4 oxidation produces two major metabolites that account for approximately 5% of the drug in plasma. Aliskiren is eliminated primarily through the biliary/fecal route as unchanged drug and, to a lesser extent, via oxidative metabolism via CYP3A4. Only 0.6% of the oral dose is recovered in urine.

Route of elimination

About one fourth of the absorbed dose appears in the urine as parent drug.

Half life

Approximate accumulation half‐life of 24 hours.

Clearance
Not Available
Toxicity

The most likely manifestation of overdosage would be hypotension.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Aliskiren.
AceclofenacThe risk or severity of renal failure and hypertension can be increased when Aceclofenac is combined with Aliskiren.
AcemetacinThe risk or severity of renal failure and hypertension can be increased when Acemetacin is combined with Aliskiren.
Acetylsalicylic acidThe risk or severity of renal failure and hypertension can be increased when Acetylsalicylic acid is combined with Aliskiren.
AgmatineThe risk or severity of hyperkalemia can be increased when Agmatine is combined with Aliskiren.
AlclofenacThe risk or severity of renal failure and hypertension can be increased when Alclofenac is combined with Aliskiren.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Aliskiren.
AlfuzosinAlfuzosin may increase the hypotensive activities of Aliskiren.
AlminoprofenThe risk or severity of renal failure and hypertension can be increased when Alminoprofen is combined with Aliskiren.
AlprenololThe risk or severity of hyperkalemia can be increased when Alprenolol is combined with Aliskiren.
Food Interactions
Not Available

References

General References
  1. Vaidyanathan S, Jarugula V, Dieterich HA, Howard D, Dole WP: Clinical pharmacokinetics and pharmacodynamics of aliskiren. Clin Pharmacokinet. 2008;47(8):515-31. [PubMed:18611061]
  2. Gradman AH, Schmieder RE, Lins RL, Nussberger J, Chiang Y, Bedigian MP: Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation. 2005 Mar 1;111(8):1012-8. Epub 2005 Feb 21. [PubMed:15723979]
  3. Staessen JA, Li Y, Richart T: Oral renin inhibitors. Lancet. 2006 Oct 21;368(9545):1449-56. [PubMed:17055947]
External Links
Human Metabolome Database
HMDB0015387
KEGG Drug
D03208
PubChem Compound
5493444
PubChem Substance
310264980
ChemSpider
4591452
BindingDB
17950
ChEBI
601027
ChEMBL
CHEMBL1639
PharmGKB
PA143487910
HET
C41
Drugs.com
Drugs.com Drug Page
Wikipedia
Aliskiren
ATC Codes
C09DX02 — Valsartan and aliskirenC09XA52 — Aliskiren and hydrochlorothiazideC09XA02 — AliskirenC09XA54 — Aliskiren, amlodipine and hydrochlorothiazideC09XA53 — Aliskiren and amlodipine
AHFS Codes
  • 24:32.40 — Renin Inhibitors
PDB Entries
2v0z
FDA label
Download (612 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableEnd Stage Renal Disease (ESRD)1
1CompletedBasic ScienceHigh Blood Pressure (Hypertension)1
1CompletedBasic ScienceRenal Function1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentHigh Blood Pressure (Hypertension)3
1WithdrawnTreatmentHigh Blood Pressure (Hypertension) / Metabolic Syndromes1
1, 2CompletedTreatmentType 2 Diabetes Mellitus3
2CompletedBasic ScienceHigh Blood Pressure (Hypertension)1
2CompletedOtherDiabetic Nephropathies1
2CompletedTreatmentEndothelial Dysfunction / High Blood Pressure (Hypertension) / Insulin Resistance / Metabolic Syndromes1
2CompletedTreatmentHeart Failure, Unspecified2
2CompletedTreatmentHigh Blood Pressure (Hypertension)2
2CompletedTreatmentMyocardial Ischemia / Post Acute Coronary Syndrome1
2TerminatedTreatmentAnkle Edema / High Blood Pressure (Hypertension)1
2TerminatedTreatmentDiabetic Macular Edema (DME)1
2TerminatedTreatmentHeart Failure, Unspecified / Renal Failure1
2TerminatedTreatmentHigh Blood Pressure (Hypertension) / Obesity, Abdominal1
2TerminatedTreatmentNon-diabetic Nephropathy1
2, 3TerminatedTreatmentAtherosclerosis1
3CompletedBasic ScienceHigh Blood Pressure (Hypertension)1
3CompletedDiagnosticHigh Blood Pressure (Hypertension)1
3CompletedOtherHeart Failure, Unspecified1
3CompletedTreatmentAcute Decompensated Heart Failure (ADHF) / Congestive Heart Failure (CHF)1
3CompletedTreatmentArterial Hypertension1
3CompletedTreatmentBMI >27 kg/m2 / High Blood Pressure (Hypertension) / Left Ventricular Hypertrophy1
3CompletedTreatmentChronic Heart Failure (CHF)1
3CompletedTreatmentCoronary Artery Atherosclerosis / Coronary Artery Disease1
3CompletedTreatmentDiabetes Mellitus (DM) / High Blood Pressure (Hypertension)1
3CompletedTreatmentHigh Blood Pressure (Hypertension)31
3CompletedTreatmentHypertension, Diabetes Mellitus1
3CompletedTreatmentHypertension,Essential4
3CompletedTreatmentIgA Nephropathy1
3CompletedTreatmentMarfan Syndrome1
3CompletedTreatmentModerate to Severe Hypertension1
3CompletedTreatmentMyocardial Infarction1
3RecruitingTreatmentNonvalvular Atrial Fibrillation1
3TerminatedTreatmentCardiovascular Disease (CVD) / Type 2 Diabetes Mellitus1
3TerminatedTreatmentCardiovascular Events1
3TerminatedTreatmentEndothelial Dysfunction1
4CompletedNot AvailableType 2 Diabetes Mellitus1
4CompletedDiagnosticHigh Blood Pressure (Hypertension)1
4CompletedOtherCoronary Artery Disease / Type 2 Diabetes Mellitus1
4CompletedScreeningChronic Kidney Disease (CKD) / High Blood Pressure (Hypertension) / Proteinuria1
4CompletedTreatmentBlood Pressures / Chronic Kidney Disease (CKD) / Proteinuria1
4CompletedTreatmentChronic Kidney Disease (CKD) / High Blood Pressure (Hypertension)1
4CompletedTreatmentChronic Kidney Disease (CKD) / Proteinuria1
4CompletedTreatmentDiabetes Mellitus (DM) / High Blood Pressure (Hypertension)1
4CompletedTreatmentEssential Hypertension ( Mild to Moderate)1
4CompletedTreatmentHeart Failure, Unspecified1
4CompletedTreatmentHigh Blood Pressure (Hypertension)10
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Left Ventricle Hypertrophy1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Metabolic Syndromes / Obesity, Abdominal1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedTreatmentHypertension,Essential2
4CompletedTreatmentIgA Nephropathy1
4CompletedTreatmentKidney Diseases1
4CompletedTreatmentStage 2 Hypertension1
4TerminatedHealth Services ResearchDiabetes Mellitus (DM) / High Blood Pressure (Hypertension) / Pre-Hypertension1
4TerminatedTreatmentAlbuminuria / Diabetes Mellitus (DM) / Macroalbuminuric Diabetic Nephropathy / Microalbuminuria / Proteinuria1
4TerminatedTreatmentCardiac Transplantation / High Blood Pressure (Hypertension)1
4TerminatedTreatmentChronic Renal Failure (CRF) / Kidney Diseases1
4TerminatedTreatmentDeficiency, Vitamin D / High Blood Pressure (Hypertension)1
4TerminatedTreatmentDiabetic Nephropathies / Glomerulonephritis, Membranous / Glomerulopathy (Obesity-associated) / Glomerulosclerosis, Focal Segmental / Hypertensive Nephrosclerosis / IgA Nephropathy / Proteinuric Kidney Disease1
4TerminatedTreatmentHigh Blood Pressure (Hypertension)1
4TerminatedTreatmentHypertension With Metabolic Syndrome1
4Unknown StatusTreatmentChronic Kidney Disease (CKD) / High Blood Pressure (Hypertension) / Muscle Sympathetic Nerve Activity1
4Unknown StatusTreatmentCongestive Heart Failure (CHF)1
4Unknown StatusTreatmentDiabetes Mellitus (DM)1
4Unknown StatusTreatmentDialysis therapy / High Blood Pressure (Hypertension)1
4Unknown StatusTreatmentEnd Stage Renal Disease (ESRD) / High Blood Pressure (Hypertension)1
4Unknown StatusTreatmentHeart Failure, Unspecified1
4Unknown StatusTreatmentHigh Blood Pressure (Hypertension)3
4Unknown StatusTreatmentHigh Blood Pressure (Hypertension) / IgA Glomerulonephritis1
4Unknown StatusTreatmentHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentHypertensive Left Ventricular Hypertrophy1
4Unknown StatusTreatmentPeritoneal Membrane Failure1
4Unknown StatusTreatmentType 2 Diabetes With Nephropathy1
4WithdrawnTreatmentDiabetes Mellitus (DM) / High Blood Pressure (Hypertension)1
4WithdrawnTreatmentHigh Blood Pressure (Hypertension)1
4WithdrawnTreatmentHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableArterial Hypertension1
Not AvailableCompletedBasic ScienceType 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentAlbuminuria1
Not AvailableCompletedTreatmentDiabetes Mellitus (DM)1
Not AvailableTerminatedTreatmentAbdominal Aortic Aneurysms (AAA) / High Blood Pressure (Hypertension)1
Not AvailableTerminatedTreatmentAortic Compliance / Diastolic Function / Insulin Sensitivity1
Not AvailableTerminatedTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableUnknown StatusNot AvailableAtherosclerosis / Diabetes Mellitus (DM)1
Not AvailableUnknown StatusPreventionDiabetes Mellitus (DM) / Endocrine System Diseases / Glucose Metabolism Disorders / Metabolic Diseases1
Not AvailableUnknown StatusTreatmentHeart Failure, Unspecified1
Not AvailableWithdrawnTreatmentDiastolic Heart Failure1
Not AvailableWithdrawnTreatmentIdiopathic Membranous Nephropathy1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, film coatedOral150 mg
Tablet, film coatedOral300 mg
TabletOral
Tablet, film coatedOral
TabletOral150 mg
TabletOral300 mg
Tablet, film coatedOral150 mg/1
Tablet, film coatedOral300 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2147056No2005-10-252015-04-13Canada
US5559111Yes1996-09-242019-01-21Us
US8617595Yes2013-12-312026-08-19Us
US8618172No2013-12-312028-07-13Us
US8168616No2012-05-012026-07-03Us
US8613949No2013-12-242029-12-21Us
US8618174No2013-12-312021-11-15Us
US8183295No2012-05-222023-05-16Us
US9023893No2015-05-052022-03-03Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityHighly soluble in water (as hemifumarate salt)Not Available
logP3.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0021 mg/mLALOGPS
logP3.87ALOGPS
logP3.12ChemAxon
logS-5.4ALOGPS
pKa (Strongest Acidic)14.56ChemAxon
pKa (Strongest Basic)9.57ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area146.13 Å2ChemAxon
Rotatable Bond Count19ChemAxon
Refractivity154.32 m3·mol-1ChemAxon
Polarizability64.25 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0uxr-0700090000-7a3148e765b056fbdbb2
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-3901100000-cb596bd3c4d4c9e1c01f
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00kr-7911000000-f660df43e70edac0517a
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0079-5910000000-d3e40bdba155982e7e43
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00dr-3900000000-8bce7f74c2390532741c
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00di-3900000000-12d8e1ded46f53c83764
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0019-0000950000-e45c32fa4cac95668993
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0v4i-4920100000-82dc644fa438b541d394
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0fk9-9810000000-c1c9bdda4686e3e603b1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-3900000000-f5052afca313a2f0c68b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0f9f-7900000000-12cc981f01c6cad986b8
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-9300000000-a3026b636a234fc9ae1f

Taxonomy

Description
This compound belongs to the class of organic compounds known as delta amino acids and derivatives. These are compounds containing a carboxylic acid group and an amino group at the C5 carbon atom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Delta amino acids and derivatives
Alternative Parents
Beta amino acids and derivatives / Phenylbutylamines / Anisoles / Methoxybenzenes / Phenoxy compounds / Alkyl aryl ethers / Aralkylamines / N-acyl amines / Secondary carboxylic acid amides / 1,2-aminoalcohols
show 8 more
Substituents
Delta amino acid or derivatives / Phenylbutylamine / Beta amino acid or derivatives / Phenol ether / Phenoxy compound / Methoxybenzene / Anisole / Aralkylamine / Alkyl aryl ether / Fatty acyl
show 24 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
monocarboxylic acid amide, monomethoxybenzene (CHEBI:601027)

Targets

Details
1. Renin
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Receptor binding
Specific Function
Renin is a highly specific endopeptidase, whose only known function is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of b...
Gene Name
REN
Uniprot ID
P00797
Uniprot Name
Renin
Molecular Weight
45057.125 Da
References
  1. Nussberger J, Wuerzner G, Jensen C, Brunner HR: Angiotensin II suppression in humans by the orally active renin inhibitor Aliskiren (SPP100): comparison with enalapril. Hypertension. 2002 Jan;39(1):E1-8. [PubMed:11799102]
  2. Wood JM, Maibaum J, Rahuel J, Grutter MG, Cohen NC, Rasetti V, Ruger H, Goschke R, Stutz S, Fuhrer W, Schilling W, Rigollier P, Yamaguchi Y, Cumin F, Baum HP, Schnell CR, Herold P, Mah R, Jensen C, O'Brien E, Stanton A, Bedigian MP: Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705. [PubMed:12927775]
  3. Menard J, Guyene TT, Peyrard S, Azizi M: Conformational changes in prorenin during renin inhibition in vitro and in vivo. J Hypertens. 2006 Mar;24(3):529-34. [PubMed:16467656]
  4. Azizi M, Webb R, Nussberger J, Hollenberg NK: Renin inhibition with aliskiren: where are we now, and where are we going? J Hypertens. 2006 Feb;24(2):243-56. [PubMed:16508564]
  5. Gradman AH, Vivas Y: New drugs for hypertension: what do they offer? Curr Hypertens Rep. 2006 Oct;8(5):425-32. [PubMed:16965731]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Vaidyanathan S, Jarugula V, Dieterich HA, Howard D, Dole WP: Clinical pharmacokinetics and pharmacodynamics of aliskiren. Clin Pharmacokinet. 2008;47(8):515-31. [PubMed:18611061]

Drug created on October 13, 2014 16:29 / Updated on November 17, 2018 04:48