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
Not Available
Product Ingredients
IngredientUNIICASInChI Key
Aliskiren hemifumarateC8A0P8G029173334-58-2KLRSDBSKUSSCGU-KRQUFFFQSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RasilezTablet, film coated150 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
RasilezTablet, film coated150 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
RasilezTablet, film coated150 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
RasilezTablet, film coated300 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
RasilezTablet, film coated300 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
RasilezTablet, film coated300 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
RasilezTablet, film coated300 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
RasilezTablet, film coated150 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
RasilezTablet, film coated150 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
RasilezTablet, film coated300 mgOralNovartis Europharm Limited2007-08-22Not applicableEu
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AmturnideAliskiren hemifumarate (300 mg/1) + Amlodipine besylate (5 mg/1) + Hydrochlorothiazide (12.5 mg/1)Tablet, film coatedOralNovartis2010-12-212016-01-31Us
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 (25 mg/1)Tablet, film coatedOralNovartis2010-12-212016-03-31Us
Rasilez HctAliskiren (300 mg) + Hydrochlorothiazide (25 mg)Tablet, film coatedOralNovartis Europharm Limited2009-01-16Not applicableEu
Rasilez HctAliskiren (300 mg) + Hydrochlorothiazide (12.5 mg)Tablet, film coatedOralNovartis Europharm Limited2009-01-16Not applicableEu
Rasilez HctAliskiren (300 mg) + Hydrochlorothiazide (25 mg)Tablet, film coatedOralNovartis Europharm Limited2009-01-16Not applicableEu
Rasilez HctAliskiren (300 mg) + Hydrochlorothiazide (25 mg)TabletOralNovartis2009-11-24Not applicableCanada
Rasilez HctAliskiren (150 mg) + Hydrochlorothiazide (12.5 mg)Tablet, film coatedOralNovartis Europharm Limited2009-01-16Not applicableEu
Rasilez HctAliskiren (150 mg) + Hydrochlorothiazide (25 mg)Tablet, film coatedOralNovartis Europharm Limited2009-01-16Not 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[[email protected]@H](C[[email protected]](N)[[email protected]@H](O)C[[email protected]@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.

Structured Indications
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
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Aliskiren.Experimental
AcebutololAcebutolol may increase the hypotensive activities of Aliskiren.Approved
AceclofenacAceclofenac may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
AcemetacinThe therapeutic efficacy of Aliskiren can be decreased when used in combination with Acemetacin.Approved, Experimental, Investigational
Acetylsalicylic acidAcetylsalicylic acid may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
AdapaleneAdapalene may decrease the antihypertensive activities of Aliskiren.Approved
AlclofenacAlclofenac may decrease the antihypertensive activities of Aliskiren.Approved, Withdrawn
AlfuzosinAlfuzosin may increase the hypotensive activities of Aliskiren.Approved, Investigational
AlminoprofenAlminoprofen may decrease the antihypertensive activities of Aliskiren.Experimental
AlprenololAlprenolol may increase the hypotensive activities of Aliskiren.Approved, Withdrawn
AmbrisentanAliskiren may increase the hypotensive activities of Ambrisentan.Approved, Investigational
AmifostineAliskiren may increase the hypotensive activities of Amifostine.Approved, Investigational
AmiodaroneThe metabolism of Aliskiren can be decreased when combined with Amiodarone.Approved, Investigational
AmlodipineAmlodipine may increase the hypotensive activities of Aliskiren.Approved
AmphetamineAmphetamine may increase the hypotensive activities of Aliskiren.Approved, Illicit
AndrographolideAndrographolide may decrease the antihypertensive activities of Aliskiren.Investigational
AnisodamineAnisodamine may decrease the antihypertensive activities of Aliskiren.Investigational
AntipyrineAntipyrine may decrease the antihypertensive activities of Aliskiren.Approved
ApocyninApocynin may decrease the antihypertensive activities of Aliskiren.Investigational
ApremilastApremilast may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
AprepitantThe serum concentration of Aliskiren can be increased when it is combined with Aprepitant.Approved, Investigational
AtazanavirThe metabolism of Aliskiren can be decreased when combined with Atazanavir.Approved, Investigational
AtenololAtenolol may increase the hypotensive activities of Aliskiren.Approved
AtomoxetineThe metabolism of Aliskiren can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Aliskiren can be increased when it is combined with Atorvastatin.Approved
AvanafilAvanafil may increase the antihypertensive activities of Aliskiren.Approved
AzapropazoneAzapropazone may decrease the antihypertensive activities of Aliskiren.Withdrawn
AzelastineAzelastine may decrease the antihypertensive activities of Aliskiren.Approved
Azilsartan medoxomilAliskiren may increase the hyperkalemic activities of Azilsartan medoxomil.Approved
BalsalazideBalsalazide may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
BarnidipineAliskiren may increase the antihypertensive activities of Barnidipine.Approved
BenazeprilAliskiren may increase the hyperkalemic activities of Benazepril.Approved, Investigational
BendazacBendazac may decrease the antihypertensive activities of Aliskiren.Experimental
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Aliskiren.Approved
BenorilateBenorilate may decrease the antihypertensive activities of Aliskiren.Experimental
BenoxaprofenBenoxaprofen may decrease the antihypertensive activities of Aliskiren.Withdrawn
BenzydamineBenzydamine may decrease the antihypertensive activities of Aliskiren.Approved
BepridilBepridil may increase the hypotensive activities of Aliskiren.Approved, Withdrawn
BetaxololBetaxolol may increase the hypotensive activities of Aliskiren.Approved
BethanidineBethanidine may increase the hypotensive activities of Aliskiren.Approved
BevoniumBevonium may decrease the antihypertensive activities of Aliskiren.Experimental
BietaserpineBietaserpine may increase the hypotensive activities of Aliskiren.Experimental
BimatoprostBimatoprost may increase the hypotensive activities of Aliskiren.Approved, Investigational
BisoprololBisoprolol may increase the hypotensive activities of Aliskiren.Approved
BoceprevirThe metabolism of Aliskiren can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Aliskiren can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Aliskiren can be decreased when it is combined with Bosentan.Approved, Investigational
BQ-123Aliskiren may increase the hypotensive activities of BQ-123.Investigational
BretyliumBretylium may increase the hypotensive activities of Aliskiren.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Aliskiren.Approved
BrofaromineBrofaromine may increase the hypotensive activities of Aliskiren.Experimental
BromfenacBromfenac may decrease the antihypertensive activities of Aliskiren.Approved
BucillamineBucillamine may decrease the antihypertensive activities of Aliskiren.Investigational
BufexamacBufexamac may decrease the antihypertensive activities of Aliskiren.Experimental
BumadizoneBumadizone may decrease the antihypertensive activities of Aliskiren.Experimental
BupranololBupranolol may increase the hypotensive activities of Aliskiren.Approved
CadralazineCadralazine may increase the hypotensive activities of Aliskiren.Experimental
CafedrineAliskiren may increase the hypotensive activities of Cafedrine.Investigational
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Aliskiren.Approved
CandesartanAliskiren may increase the hyperkalemic activities of Candesartan.Experimental
Candesartan cilexetilThe risk or severity of adverse effects can be increased when Candesartan cilexetil is combined with Aliskiren.Approved
CandoxatrilAliskiren may increase the hyperkalemic activities of Candoxatril.Experimental
CaptoprilAliskiren may increase the hyperkalemic activities of Captopril.Approved
CarbamazepineThe metabolism of Aliskiren can be increased when combined with Carbamazepine.Approved, Investigational
Carbaspirin calciumCarbaspirin calcium may decrease the antihypertensive activities of Aliskiren.Experimental, Investigational
CarprofenCarprofen may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved, Withdrawn
CarteololCarteolol may increase the hypotensive activities of Aliskiren.Approved
CarvedilolCarvedilol may increase the hypotensive activities of Aliskiren.Approved, Investigational
CastanospermineCastanospermine may decrease the antihypertensive activities of Aliskiren.Experimental
CelecoxibCelecoxib may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
CeliprololCeliprolol may increase the hypotensive activities of Aliskiren.Approved, Investigational
CeritinibThe serum concentration of Aliskiren can be increased when it is combined with Ceritinib.Approved
ChloroquineChloroquine may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Aliskiren.Approved, Vet Approved
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Aliskiren.Approved
Choline magnesium trisalicylateCholine magnesium trisalicylate may decrease the antihypertensive activities of Aliskiren.Approved
CicletanineAliskiren may increase the hypotensive activities of Cicletanine.Investigational
CilazaprilAliskiren may increase the hyperkalemic activities of Cilazapril.Approved
ClarithromycinThe metabolism of Aliskiren can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Aliskiren can be decreased when combined with Clemastine.Approved
ClonidineClonidine may increase the hypotensive activities of Aliskiren.Approved
ClonixinClonixin may decrease the antihypertensive activities of Aliskiren.Approved
CloranololAliskiren may increase the hypotensive activities of Cloranolol.Experimental
ClotrimazoleThe metabolism of Aliskiren can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Aliskiren can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Aliskiren.Approved, Investigational
CrizotinibThe metabolism of Aliskiren can be decreased when combined with Crizotinib.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Aliskiren.Approved
CurcuminCurcumin may decrease the antihypertensive activities of Aliskiren.Investigational
CyclopenthiazideAliskiren may increase the hypotensive activities of Cyclopenthiazide.Experimental
CyclosporineThe serum concentration of Aliskiren can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclothiazideCyclothiazide may increase the hypotensive activities of Aliskiren.Approved
DabrafenibThe serum concentration of Aliskiren can be decreased when it is combined with Dabrafenib.Approved
DarunavirThe metabolism of Aliskiren can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Aliskiren can be increased when it is combined with Dasatinib.Approved, Investigational
DebrisoquinDebrisoquin may increase the hypotensive activities of Aliskiren.Approved, Investigational
DeferasiroxThe serum concentration of Aliskiren can be decreased when it is combined with Deferasirox.Approved, Investigational
DelaprilAliskiren may increase the hyperkalemic activities of Delapril.Experimental
DelavirdineThe metabolism of Aliskiren can be decreased when combined with Delavirdine.Approved
DeserpidineAliskiren may increase the hypotensive activities of Deserpidine.Approved
DiazoxideDiazoxide may increase the hypotensive activities of Aliskiren.Approved
DiclofenacDiclofenac may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
DiethylnorspermineDiethylnorspermine may increase the hypotensive activities of Aliskiren.Investigational
DifenpiramideDifenpiramide may decrease the antihypertensive activities of Aliskiren.Experimental
DiflunisalDiflunisal may decrease the antihypertensive activities of Aliskiren.Approved
DihydralazineDihydralazine may increase the hypotensive activities of Aliskiren.Investigational
DihydroergotamineThe metabolism of Aliskiren can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Aliskiren can be decreased when combined with Diltiazem.Approved
DorzolamideDorzolamide may increase the hypotensive activities of Aliskiren.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Aliskiren.Approved
DoxycyclineThe metabolism of Aliskiren can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Aliskiren can be decreased when combined with Dronedarone.Approved
DrospirenoneDrospirenone may increase the hyperkalemic activities of Aliskiren.Approved
DroxicamDroxicam may decrease the antihypertensive activities of Aliskiren.Withdrawn
DuvelisibDuvelisib may decrease the antihypertensive activities of Aliskiren.Investigational
E-6201E-6201 may decrease the antihypertensive activities of Aliskiren.Investigational
EfonidipineAliskiren may increase the hypotensive activities of Efonidipine.Approved, Investigational
EnalaprilAliskiren may increase the hyperkalemic activities of Enalapril.Approved, Vet Approved
EnalaprilatAliskiren may increase the hyperkalemic activities of Enalaprilat.Approved
EndralazineEndralazine may increase the hypotensive activities of Aliskiren.Experimental
EnzalutamideThe serum concentration of Aliskiren can be decreased when it is combined with Enzalutamide.Approved
EpanololAliskiren may increase the hypotensive activities of Epanolol.Experimental
EpirizoleEpirizole may decrease the antihypertensive activities of Aliskiren.Approved
EpoprostenolEpoprostenol may increase the hypotensive activities of Aliskiren.Approved
EprosartanAliskiren may increase the hyperkalemic activities of Eprosartan.Approved
ErythromycinThe metabolism of Aliskiren can be decreased when combined with Erythromycin.Approved, Vet Approved
EtanerceptEtanercept may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
EthenzamideEthenzamide may decrease the antihypertensive activities of Aliskiren.Experimental
EtodolacEtodolac may decrease the antihypertensive activities of Aliskiren.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
EtoricoxibEtoricoxib may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
Evening primrose oilEvening primrose oil may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
ExisulindExisulind may decrease the antihypertensive activities of Aliskiren.Investigational
FelbinacFelbinac may decrease the antihypertensive activities of Aliskiren.Experimental
FelodipineFelodipine may increase the hypotensive activities of Aliskiren.Approved, Investigational
FenbufenFenbufen may decrease the antihypertensive activities of Aliskiren.Approved
FenoldopamFenoldopam may increase the hypotensive activities of Aliskiren.Approved
FenoprofenFenoprofen may decrease the antihypertensive activities of Aliskiren.Approved
FentiazacFentiazac may decrease the antihypertensive activities of Aliskiren.Experimental
FeprazoneFeprazone may decrease the antihypertensive activities of Aliskiren.Experimental
Ferulic acidFerulic acid may decrease the antihypertensive activities of Aliskiren.Experimental
FimasartanAliskiren may increase the hyperkalemic activities of Fimasartan.Approved, Investigational
FloctafenineFloctafenine may decrease the antihypertensive activities of Aliskiren.Approved, Withdrawn
FluconazoleThe metabolism of Aliskiren can be decreased when combined with Fluconazole.Approved
FlunixinFlunixin may decrease the antihypertensive activities of Aliskiren.Vet Approved
FlunoxaprofenFlunoxaprofen may decrease the antihypertensive activities of Aliskiren.Experimental
FlurbiprofenFlurbiprofen may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
FluvoxamineThe metabolism of Aliskiren can be decreased when combined with Fluvoxamine.Approved, Investigational
ForasartanAliskiren may increase the hyperkalemic activities of Forasartan.Experimental
FosamprenavirThe metabolism of Aliskiren can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Aliskiren can be increased when it is combined with Fosaprepitant.Approved
FosinoprilAliskiren may increase the hyperkalemic activities of Fosinopril.Approved
FosphenytoinThe metabolism of Aliskiren can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Aliskiren.Approved, Investigational, Vet Approved
FurosemideThe serum concentration of Furosemide can be decreased when it is combined with Aliskiren.Approved, Vet Approved
Fusidic AcidThe serum concentration of Aliskiren can be increased when it is combined with Fusidic Acid.Approved
GuacetisalGuacetisal may decrease the antihypertensive activities of Aliskiren.Experimental
GuanabenzGuanabenz may increase the hypotensive activities of Aliskiren.Approved, Investigational
GuanadrelGuanadrel may increase the hypotensive activities of Aliskiren.Approved
GuanazodineAliskiren may increase the hypotensive activities of Guanazodine.Experimental
GuanethidineGuanethidine may increase the hypotensive activities of Aliskiren.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Aliskiren.Approved, Investigational
GuanoclorAliskiren may increase the hypotensive activities of Guanoclor.Experimental
GuanoxabenzAliskiren may increase the hypotensive activities of Guanoxabenz.Experimental
GuanoxanAliskiren may increase the hypotensive activities of Guanoxan.Experimental
HarmalineHarmaline may increase the hypotensive activities of Aliskiren.Experimental
HeparinHeparin may increase the hyperkalemic activities of Aliskiren.Approved, Investigational
HexamethoniumHexamethonium may increase the hypotensive activities of Aliskiren.Experimental
HigenamineHigenamine may decrease the antihypertensive activities of Aliskiren.Investigational
HydralazineHydralazine may increase the hypotensive activities of Aliskiren.Approved
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Aliskiren.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Aliskiren.Approved, Investigational
IbuprofenIbuprofen may decrease the antihypertensive activities of Aliskiren.Approved
IbuproxamIbuproxam may decrease the antihypertensive activities of Aliskiren.Withdrawn
IcatibantIcatibant may decrease the antihypertensive activities of Aliskiren.Approved
IdelalisibThe metabolism of Aliskiren can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Aliskiren can be decreased when combined with Imatinib.Approved
ImidaprilAliskiren may increase the hyperkalemic activities of Imidapril.Investigational
Imidazole salicylateImidazole salicylate may decrease the antihypertensive activities of Aliskiren.Experimental
IndapamideIndapamide may increase the hypotensive activities of Aliskiren.Approved
IndenololIndenolol may increase the hypotensive activities of Aliskiren.Withdrawn
IndinavirThe metabolism of Aliskiren can be decreased when combined with Indinavir.Approved
IndobufenIndobufen may decrease the antihypertensive activities of Aliskiren.Investigational
IndomethacinIndomethacin may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
IndoprofenIndoprofen may decrease the antihypertensive activities of Aliskiren.Withdrawn
IndoraminIndoramin may increase the hypotensive activities of Aliskiren.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Aliskiren.Withdrawn
IrbesartanAliskiren may increase the hyperkalemic activities of Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Aliskiren can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Aliskiren.Approved
IsoxicamIsoxicam may decrease the antihypertensive activities of Aliskiren.Withdrawn
IsradipineThe metabolism of Aliskiren can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Aliskiren can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Aliskiren can be increased when it is combined with Ivacaftor.Approved
KebuzoneKebuzone may decrease the antihypertensive activities of Aliskiren.Experimental
KetanserinKetanserin may increase the hypotensive activities of Aliskiren.Investigational
KetoconazoleThe serum concentration of Aliskiren can be increased when it is combined with Ketoconazole.Approved, Investigational
KetoprofenKetoprofen may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
KetorolacKetorolac may decrease the antihypertensive activities of Aliskiren.Approved
LabetalolLabetalol may increase the hypotensive activities of Aliskiren.Approved
LacidipineAliskiren may increase the hypotensive activities of Lacidipine.Approved, Investigational
LatanoprostLatanoprost may increase the hypotensive activities of Aliskiren.Approved, Investigational
LeflunomideLeflunomide may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
LercanidipineLercanidipine may increase the hypotensive activities of Aliskiren.Approved, Investigational
LinsidomineAliskiren may increase the hypotensive activities of Linsidomine.Experimental
LisinoprilAliskiren may increase the hyperkalemic activities of Lisinopril.Approved, Investigational
LisofyllineLisofylline may decrease the antihypertensive activities of Aliskiren.Investigational
LofexidineLofexidine may increase the hypotensive activities of Aliskiren.Approved, Investigational
LonazolacLonazolac may decrease the antihypertensive activities of Aliskiren.Experimental
LopinavirThe metabolism of Aliskiren can be decreased when combined with Lopinavir.Approved
LornoxicamLornoxicam may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
LorpiprazoleThe serum concentration of Aliskiren can be increased when it is combined with Lorpiprazole.Approved
LosartanAliskiren may increase the hyperkalemic activities of Losartan.Approved
LovastatinThe metabolism of Aliskiren can be decreased when combined with Lovastatin.Approved, Investigational
LoxoprofenLoxoprofen may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
LuliconazoleThe serum concentration of Aliskiren can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Aliskiren can be increased when combined with Lumacaftor.Approved
LumiracoxibLumiracoxib may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
MacitentanAliskiren may increase the hypotensive activities of Macitentan.Approved
Magnesium salicylateMagnesium salicylate may decrease the antihypertensive activities of Aliskiren.Approved
ManidipineAliskiren may increase the hypotensive activities of Manidipine.Approved, Investigational
MasoprocolMasoprocol may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
MecamylamineMecamylamine may increase the hypotensive activities of Aliskiren.Approved
Meclofenamic acidMeclofenamic acid may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
Mefenamic acidMefenamic acid may decrease the antihypertensive activities of Aliskiren.Approved
MeloxicamMeloxicam may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
MesalazineMesalazine may decrease the antihypertensive activities of Aliskiren.Approved
MetamizoleMetamizole may decrease the antihypertensive activities of Aliskiren.Investigational, Withdrawn
MethoserpidineAliskiren may increase the hypotensive activities of Methoserpidine.Experimental
MethyldopaMethyldopa may increase the hypotensive activities of Aliskiren.Approved
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
MetipranololMetipranolol may increase the hypotensive activities of Aliskiren.Approved
MetolazoneMetolazone may increase the hypotensive activities of Aliskiren.Approved
MetoprololMetoprolol may increase the hypotensive activities of Aliskiren.Approved, Investigational
MetyrosineAliskiren may increase the hypotensive activities of Metyrosine.Approved
MibefradilMibefradil may increase the hypotensive activities of Aliskiren.Investigational, Withdrawn
MifepristoneThe serum concentration of Aliskiren can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineMinaprine may increase the hypotensive activities of Aliskiren.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Aliskiren.Approved
MirodenafilMirodenafil may increase the antihypertensive activities of Aliskiren.Investigational
MitotaneThe serum concentration of Aliskiren can be decreased when it is combined with Mitotane.Approved
MizoribineMizoribine may decrease the antihypertensive activities of Aliskiren.Investigational
MoclobemideMoclobemide may increase the hypotensive activities of Aliskiren.Approved
MoexiprilAliskiren may increase the hyperkalemic activities of Moexipril.Approved
MofebutazoneMofebutazone may decrease the antihypertensive activities of Aliskiren.Experimental
MolsidomineMolsidomine may increase the hypotensive activities of Aliskiren.Approved, Investigational
MoxonidineMoxonidine may increase the hypotensive activities of Aliskiren.Approved, Investigational
MuzolimineAliskiren may increase the hypotensive activities of Muzolimine.Experimental
Mycophenolate mofetilMycophenolate mofetil may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
Mycophenolic acidMycophenolic acid may decrease the antihypertensive activities of Aliskiren.Approved
NabumetoneNabumetone may decrease the antihypertensive activities of Aliskiren.Approved
NadololNadolol may increase the hypotensive activities of Aliskiren.Approved
NafamostatNafamostat may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
NaftifineNaftifine may decrease the antihypertensive activities of Aliskiren.Approved
NaftopidilAliskiren may increase the hypotensive activities of Naftopidil.Investigational
NaproxenNaproxen may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
NebivololNebivolol may increase the hypotensive activities of Aliskiren.Approved, Investigational
NefazodoneThe metabolism of Aliskiren can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Aliskiren can be decreased when combined with Nelfinavir.Approved
NepafenacNepafenac may decrease the antihypertensive activities of Aliskiren.Approved
NetupitantThe serum concentration of Aliskiren can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Aliskiren can be increased when combined with Nevirapine.Approved
NialamideNialamide may increase the hypotensive activities of Aliskiren.Withdrawn
NicardipineNicardipine may increase the hypotensive activities of Aliskiren.Approved
NicorandilNicorandil may increase the hyperkalemic activities of Aliskiren.Approved, Investigational
NifenazoneNifenazone may decrease the antihypertensive activities of Aliskiren.Experimental
Niflumic AcidNiflumic Acid may decrease the antihypertensive activities of Aliskiren.Approved
NiguldipineAliskiren may increase the hypotensive activities of Niguldipine.Experimental
NilotinibThe metabolism of Aliskiren can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineNilvadipine may increase the hypotensive activities of Aliskiren.Approved, Investigational
NimesulideNimesulide may decrease the antihypertensive activities of Aliskiren.Approved, Investigational, Withdrawn
NimodipineNimodipine may increase the hypotensive activities of Aliskiren.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Aliskiren.Approved
NitrendipineNitrendipine may increase the hypotensive activities of Aliskiren.Approved, Investigational
NitroaspirinNitroaspirin may decrease the antihypertensive activities of Aliskiren.Investigational
NitroprussideNitroprusside may increase the hypotensive activities of Aliskiren.Approved
ObinutuzumabAliskiren may increase the hypotensive activities of Obinutuzumab.Approved
OlaparibThe metabolism of Aliskiren can be decreased when combined with Olaparib.Approved
OlmesartanAliskiren may increase the hyperkalemic activities of Olmesartan.Approved, Investigational
OlopatadineOlopatadine may decrease the antihypertensive activities of Aliskiren.Approved
OlsalazineOlsalazine may decrease the antihypertensive activities of Aliskiren.Approved
OmapatrilatAliskiren may increase the hyperkalemic activities of Omapatrilat.Investigational
OrgoteinOrgotein may decrease the antihypertensive activities of Aliskiren.Vet Approved
OsimertinibThe serum concentration of Aliskiren can be increased when it is combined with Osimertinib.Approved
OxaprozinOxaprozin may decrease the antihypertensive activities of Aliskiren.Approved
OxprenololOxprenolol may increase the hypotensive activities of Aliskiren.Approved
OxyphenbutazoneOxyphenbutazone may decrease the antihypertensive activities of Aliskiren.Approved, Withdrawn
PalbociclibThe serum concentration of Aliskiren can be increased when it is combined with Palbociclib.Approved
ParecoxibParecoxib may decrease the antihypertensive activities of Aliskiren.Approved
PargylinePargyline may increase the hypotensive activities of Aliskiren.Approved
ParthenolideParthenolide may decrease the antihypertensive activities of Aliskiren.Investigational
PenbutololPenbutolol may increase the hypotensive activities of Aliskiren.Approved, Investigational
PentobarbitalThe metabolism of Aliskiren can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoliniumPentolinium may increase the hypotensive activities of Aliskiren.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Aliskiren.Approved, Investigational
PerindoprilAliskiren may increase the hyperkalemic activities of Perindopril.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Aliskiren.Approved
PhenobarbitalThe metabolism of Aliskiren can be increased when combined with Phenobarbital.Approved
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Aliskiren.Approved
PhentolaminePhentolamine may increase the hypotensive activities of Aliskiren.Approved
PhenylbutazonePhenylbutazone may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
PhenytoinThe metabolism of Aliskiren can be increased when combined with Phenytoin.Approved, Vet Approved
PimecrolimusPimecrolimus may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
PinacidilPinacidil may increase the hypotensive activities of Aliskiren.Withdrawn
PindololPindolol may increase the hypotensive activities of Aliskiren.Approved
PirfenidonePirfenidone may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
PirlindolePirlindole may increase the hypotensive activities of Aliskiren.Approved
PiroxicamPiroxicam may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
PirprofenPirprofen may decrease the antihypertensive activities of Aliskiren.Experimental
Platelet Activating FactorPlatelet Activating Factor may increase the hypotensive activities of Aliskiren.Experimental
PolythiazidePolythiazide may increase the hypotensive activities of Aliskiren.Approved
PosaconazoleThe metabolism of Aliskiren can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PranoprofenPranoprofen may decrease the antihypertensive activities of Aliskiren.Experimental, Investigational
PrazosinPrazosin may increase the hypotensive activities of Aliskiren.Approved
PrimidoneThe metabolism of Aliskiren can be increased when combined with Primidone.Approved, Vet Approved
ProcarbazineProcarbazine may increase the hypotensive activities of Aliskiren.Approved
ProglumetacinProglumetacin may decrease the antihypertensive activities of Aliskiren.Experimental
PropacetamolPropacetamol may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
PropranololPropranolol may increase the hypotensive activities of Aliskiren.Approved, Investigational
PropyphenazonePropyphenazone may decrease the antihypertensive activities of Aliskiren.Experimental
ProquazoneProquazone may decrease the antihypertensive activities of Aliskiren.Experimental
PTC299PTC299 may decrease the antihypertensive activities of Aliskiren.Investigational
QuinaprilAliskiren may increase the hyperkalemic activities of Quinapril.Approved, Investigational
RamiprilAliskiren may increase the hyperkalemic activities of Ramipril.Approved
RanolazineThe metabolism of Aliskiren can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypotensive activities of Aliskiren.Approved
RemikirenRemikiren may increase the hypotensive activities of Aliskiren.Approved
RescinnamineAliskiren may increase the hyperkalemic activities of Rescinnamine.Approved
ReserpineReserpine may increase the hypotensive activities of Aliskiren.Approved, Investigational
ResveratrolResveratrol may decrease the antihypertensive activities of Aliskiren.Approved, Experimental, Investigational
RifabutinThe metabolism of Aliskiren can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Aliskiren can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Aliskiren can be increased when combined with Rifapentine.Approved
RilmenidineRilmenidine may increase the hypotensive activities of Aliskiren.Investigational
RiociguatAliskiren may increase the hypotensive activities of Riociguat.Approved
RituximabAliskiren may increase the hypotensive activities of Rituximab.Approved
RofecoxibRofecoxib may decrease the antihypertensive activities of Aliskiren.Investigational, Withdrawn
RucaparibThe metabolism of Aliskiren can be decreased when combined with Rucaparib.Approved, Investigational
SacubitrilAliskiren may increase the hyperkalemic activities of Sacubitril.Approved
SalicylamideSalicylamide may decrease the antihypertensive activities of Aliskiren.Approved
Salicylic acidSalicylic acid may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
SalsalateSalsalate may decrease the antihypertensive activities of Aliskiren.Approved
SaprisartanAliskiren may increase the hyperkalemic activities of Saprisartan.Experimental
SaquinavirThe metabolism of Aliskiren can be decreased when combined with Saquinavir.Approved, Investigational
SaralasinAliskiren may increase the hyperkalemic activities of Saralasin.Investigational
SarilumabThe therapeutic efficacy of Aliskiren can be decreased when used in combination with Sarilumab.Approved
SelegilineSelegiline may increase the hypotensive activities of Aliskiren.Approved, Investigational, Vet Approved
SelexipagAliskiren may increase the hypotensive activities of Selexipag.Approved
SemapimodSemapimod may decrease the antihypertensive activities of Aliskiren.Investigational
SeratrodastSeratrodast may decrease the antihypertensive activities of Aliskiren.Approved
SerrapeptaseSerrapeptase may decrease the antihypertensive activities of Aliskiren.Investigational
SildenafilSildenafil may increase the antihypertensive activities of Aliskiren.Approved, Investigational
SiltuximabThe serum concentration of Aliskiren can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Aliskiren can be increased when it is combined with Simeprevir.Approved
SitaxentanAliskiren may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
SpiraprilAliskiren may increase the hyperkalemic activities of Spirapril.Approved
SRT501SRT501 may decrease the antihypertensive activities of Aliskiren.Investigational
St. John's WortThe serum concentration of Aliskiren can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Aliskiren can be increased when it is combined with Stiripentol.Approved
SulfasalazineSulfasalazine may decrease the antihypertensive activities of Aliskiren.Approved
SulfisoxazoleThe metabolism of Aliskiren can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulindacSulindac may decrease the antihypertensive activities of Aliskiren.Approved
SuprofenSuprofen may decrease the antihypertensive activities of Aliskiren.Approved, Withdrawn
SuxibuzoneSuxibuzone may decrease the antihypertensive activities of Aliskiren.Experimental
TadalafilTadalafil may increase the antihypertensive activities of Aliskiren.Approved, Investigational
TalinololAliskiren may increase the hypotensive activities of Talinolol.Investigational
TarenflurbilTarenflurbil may decrease the antihypertensive activities of Aliskiren.Investigational
TasosartanAliskiren may increase the hyperkalemic activities of Tasosartan.Approved
TelaprevirThe metabolism of Aliskiren can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Aliskiren can be decreased when combined with Telithromycin.Approved
TelmisartanAliskiren may increase the hyperkalemic activities of Telmisartan.Approved, Investigational
TemocaprilAliskiren may increase the hyperkalemic activities of Temocapril.Experimental, Investigational
TenidapTenidap may decrease the antihypertensive activities of Aliskiren.Experimental
TenoxicamTenoxicam may decrease the antihypertensive activities of Aliskiren.Approved
TepoxalinTepoxalin may decrease the antihypertensive activities of Aliskiren.Vet Approved
TeriflunomideTeriflunomide may decrease the antihypertensive activities of Aliskiren.Approved
TerlipressinTerlipressin may increase the hypotensive activities of Aliskiren.Approved, Investigational
TetrahydropalmatineAliskiren may increase the hypotensive activities of Tetrahydropalmatine.Investigational
TheodrenalineAliskiren may increase the hypotensive activities of Theodrenaline.Investigational
Tiaprofenic acidTiaprofenic acid may decrease the antihypertensive activities of Aliskiren.Approved
TiboloneAliskiren may increase the hypotensive activities of Tibolone.Approved, Investigational
TiclopidineThe metabolism of Aliskiren can be decreased when combined with Ticlopidine.Approved
TicrynafenTicrynafen may increase the hypotensive activities of Aliskiren.Withdrawn
TimololTimolol may increase the hypotensive activities of Aliskiren.Approved
TinoridineTinoridine may decrease the antihypertensive activities of Aliskiren.Investigational
TocilizumabThe serum concentration of Aliskiren can be decreased when it is combined with Tocilizumab.Approved
TolazolineTolazoline may increase the hypotensive activities of Aliskiren.Approved, Vet Approved
Tolfenamic AcidTolfenamic Acid may decrease the antihypertensive activities of Aliskiren.Approved
TolmetinTolmetin may decrease the antihypertensive activities of Aliskiren.Approved
TolonidineAliskiren may increase the hypotensive activities of Tolonidine.Experimental
ToloxatoneToloxatone may increase the hypotensive activities of Aliskiren.Approved
TorasemideTorasemide may increase the hypotensive activities of Aliskiren.Approved
TrandolaprilAliskiren may increase the hyperkalemic activities of Trandolapril.Approved
TranilastTranilast may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Aliskiren.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Aliskiren.Approved
TravoprostTravoprost may increase the hypotensive activities of Aliskiren.Approved
TreprostinilTreprostinil may increase the hypotensive activities of Aliskiren.Approved, Investigational
TribenosideTribenoside may decrease the antihypertensive activities of Aliskiren.Experimental
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Aliskiren.Approved, Vet Approved
TrimazosinTrimazosin may increase the hypotensive activities of Aliskiren.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Aliskiren.Approved, Investigational
TriptolideTriptolide may decrease the antihypertensive activities of Aliskiren.Investigational
UdenafilUdenafil may increase the antihypertensive activities of Aliskiren.Approved, Investigational
UnoprostoneUnoprostone may increase the hypotensive activities of Aliskiren.Approved, Investigational
UrapidilUrapidil may increase the hypotensive activities of Aliskiren.Investigational
ValdecoxibValdecoxib may decrease the antihypertensive activities of Aliskiren.Investigational, Withdrawn
ValsartanAliskiren may increase the hyperkalemic activities of Valsartan.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Aliskiren.Approved
VemurafenibThe serum concentration of Aliskiren can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Aliskiren can be decreased when combined with Venlafaxine.Approved
VerapamilThe serum concentration of Aliskiren can be increased when it is combined with Verapamil.Approved
VincamineAliskiren may increase the hypotensive activities of Vincamine.Experimental
VinpocetineAliskiren may increase the hypotensive activities of Vinpocetine.Investigational
VoriconazoleThe metabolism of Aliskiren can be decreased when combined with Voriconazole.Approved, Investigational
XipamideAliskiren may increase the hypotensive activities of Xipamide.Experimental
XylometazolineXylometazoline may increase the hypotensive activities of Aliskiren.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Aliskiren.Approved, Vet Approved
ZaltoprofenZaltoprofen may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
ZileutonZileuton may decrease the antihypertensive activities of Aliskiren.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Aliskiren can be decreased when combined with Ziprasidone.Approved
ZofenoprilAliskiren may increase the hyperkalemic activities of Zofenopril.Experimental
ZomepiracZomepirac may decrease the antihypertensive activities of Aliskiren.Withdrawn
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 aliskirenC09XA02 — AliskirenC09XA52 — Aliskiren and hydrochlorothiazideC09XA53 — Aliskiren and amlodipineC09XA54 — Aliskiren, amlodipine and hydrochlorothiazide
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 Infarction (MI)1
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
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
4TerminatedTreatmentKidney Diseases / Kidney Failure,Chronic1
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
TabletOral150 mg
TabletOral300 mg
Tablet, film coatedOral150 mg
Tablet, film coatedOral300 mg
TabletOral
Tablet, film coatedOral
Tablet, film coatedOral150 mg/1
Tablet, film coatedOral300 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2147056No2005-10-252015-04-13Canada
US5559111Yes1999-01-212019-01-21Us
US8617595Yes2006-08-192026-08-19Us
US8618172No2008-07-132028-07-13Us
US8168616No2006-07-032026-07-03Us
US8613949No2009-12-212029-12-21Us
US8618174No2001-11-152021-11-15Us
US8183295No2003-05-162023-05-16Us
US9023893No2002-03-032022-03-03Us

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 January 23, 2018 12:20