Identification
NameSacubitril
Accession NumberDB09292
TypeSmall Molecule
GroupsApproved
Description

Sacubitril is a prodrug neprilysin inhibitor used in combination with valsartan to reduce the risk of cardiovascular events in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction. It was approved under the FDA's priority review process for use in heart failure on July 7, 2015.

Sacubitril's active metabolite, LBQ657 inhibits neprilysin, a neutral endopeptidase that would typically cleave natiuretic peptides such as atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and c-type natriuretic peptide (CNP). ANP and BNP are released under atrial and ventricle stress, which activate downstream receptors leading to vasodilation, natriuresis and diuresis. Under normal conditions, neprilysin breaks down other vasodilating peptides and also vasoconstrictors such as angiotensin I and II, endothelin-1 and peptide amyloid beta-protein. Inhibition of neprilysin therefore leads to reduced breakdown and increased concentration of endogenous natriuretic peptides in addition to increased levels of vasoconstricting hormones such as angiotensin II.

Structure
Thumb
SynonymsNot Available
External IDs AHU-377 / AHU377 / LCZ-696 / LCZ696
Product Ingredients Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
EntrestoTabletOralNovartis2015-11-13Not applicableCanada
Categories
UNII17ERJ0MKGI
CAS number149709-62-6
WeightAverage: 411.498
Monoisotopic: 411.204573038
Chemical FormulaC24H29NO5
InChI KeyPYNXFZCZUAOOQC-UTKZUKDTSA-N
InChI
InChI=1S/C24H29NO5/c1-3-30-24(29)17(2)15-21(25-22(26)13-14-23(27)28)16-18-9-11-20(12-10-18)19-7-5-4-6-8-19/h4-12,17,21H,3,13-16H2,1-2H3,(H,25,26)(H,27,28)/t17-,21+/m1/s1
IUPAC Name
3-{[(2S,4R)-1-{[1,1'-biphenyl]-4-yl}-5-ethoxy-4-methyl-5-oxopentan-2-yl]carbamoyl}propanoic acid
SMILES
[H][[email protected]@](CC1=CC=C(C=C1)C1=CC=CC=C1)(C[[email protected]@]([H])(C)C(=O)OCC)NC(=O)CCC(O)=O
Pharmacology
Indication

Used in combination with valsartan to reduce the risk of cardiovascular events in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction. It is usually administered in conjunction with other heart failure therapies, in place of an ACE inhibitor or other ARB.

Structured Indications
Pharmacodynamics

n a 7-day valsartan-controlled study in patients with reduced ejection fraction (HFrEF), administration of sacubitril + valsartan (Entresto) resulted in a significant non-sustained increase in natriuresis, increased urine cGMP, and decreased plasma MR-proANP and NT-proBNP compared to valsartan. In a 21-day study in HFrEF patients, it significantly increased urine ANP and cGMP and plasma cGMP, and decreased plasma NT-proBNP, aldosterone and endothelin-1. In clinical studies, this combination had no effect on QTc interval.

Mechanism of action

Sacubitril's active metabolite, LBQ657 inhibits neprilysin, a neutral endopeptidase that would typically cleave natiuretic peptides, which includes: atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and c-type natriuretic peptide (CNP). ANP and BNP are released under atrial and ventricle stress, which activate downstream receptors leading to vasodilation, natriuresis and diuresis. Under normal conditions, neprilysin breaks down other vasodilating peptides and also vasoconstrictors such as angiotensin I and II, endothelin-1 and peptide amyloid beta-protein. Therefore, the inhibition of neprilysin leads to reduced breakdown and increased concentration of endogenous natriuretic peptides in addition to increased levels of vasoconstricting hormones such as angiotensin II. (However, when combined with valsartan, would result in blocking of angiotensin II to its receptor, preventing the vasoconstrictive effects and resulting in a decrease in vascular resistance and blood pressure.) Cardiovascular and renal effects of sacubitril is a result of the increased levels of peptides that are normally degraded by neprilysin.

TargetKindPharmacological actionActionsOrganismUniProt ID
NeprilysinProteinyes
antagonist
inhibitor
HumanP08473 details
Related Articles
Absorption

Peak plasma concentrations of sacubitril and it's metabolite, LBQ657 are reached in 0.5 hours and 2 hours respectively. Food does not clinically affect the systemic exposure of sacubitril or LBQ657. The oral bioavailability of sacubitril is >60%. It should be noted that the valsartan found in this combination is more bioavailable than other market available valsartan.

Volume of distribution

103 L

Protein binding

Sacubitril and it's metabolite, LBQ657 are highly bound to plasma protein (94-97%).

Metabolism

Sacubitril is metabolized to LBQ657 by esterases. A low concentration (<10%) of a hydroxyl metabolite has been identified in plasma.

SubstrateEnzymesProduct
Sacubitril
Not Available
Sacubitrilat (LBQ657)Details
Route of elimination

52% to 68% of sacubitril (primarily as the active metabolite LBQ657) is excreted in urine. 37% to 48% of sacubitril (primarily as LBQ657) is excreted in feces

Half life

The half life of sacubitril is 1.1 to 3.6 hours, and the half life of it's metabolite LBQ657 is 9.9 to 11.1 hours.

ClearanceNot Available
Toxicity

The most common adverse reactions (≥5%) are hypotension, hyperkalemia, cough, dizziness, and renal failure.

Affected organismsNot Available
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Sacubitril.Approved
AceclofenacThe risk or severity of adverse effects can be increased when Sacubitril is combined with Aceclofenac.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Sacubitril is combined with Acetazolamide.Approved, Vet Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Sacubitril is combined with Acetylsalicylic acid.Approved, Vet Approved
AdapaleneThe risk or severity of adverse effects can be increased when Sacubitril is combined with Adapalene.Approved
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Sacubitril.Approved
AliskirenAliskiren may increase the hyperkalemic activities of Sacubitril.Approved, Investigational
AmifostineThe risk or severity of adverse effects can be increased when Amifostine is combined with Sacubitril.Approved, Investigational
AmilorideSacubitril may increase the hyperkalemic activities of Amiloride.Approved
AmiodaroneThe risk or severity of adverse effects can be increased when Amiodarone is combined with Sacubitril.Approved, Investigational
AmlodipineThe risk or severity of adverse effects can be increased when Amlodipine is combined with Sacubitril.Approved
AmobarbitalAmobarbital may increase the hypotensive activities of Sacubitril.Approved, Illicit
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Sacubitril.Approved, Investigational
Amyl NitriteThe risk or severity of adverse effects can be increased when Amyl Nitrite is combined with Sacubitril.Approved
AndrographolideThe risk or severity of adverse effects can be increased when Sacubitril is combined with HMPL-004.Investigational
AnisodamineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Anisodamine.Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Antipyrine.Approved
ApocyninThe risk or severity of adverse effects can be increased when Sacubitril is combined with Acetovanillone.Investigational
ApomorphineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Sacubitril.Approved, Investigational
ApraclonidineThe risk or severity of adverse effects can be increased when Apraclonidine is combined with Sacubitril.Approved
ApremilastThe risk or severity of adverse effects can be increased when Sacubitril is combined with Apremilast.Approved, Investigational
ArdeparinArdeparin may increase the hyperkalemic activities of Sacubitril.Approved, Withdrawn
AripiprazoleAripiprazole may increase the hypotensive activities of Sacubitril.Approved, Investigational
ArotinololThe risk or severity of adverse effects can be increased when Arotinolol is combined with Sacubitril.Approved
Arsenic trioxideThe risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Sacubitril.Approved, Investigational
AtenololThe risk or severity of adverse effects can be increased when Atenolol is combined with Sacubitril.Approved
AzapropazoneThe risk or severity of adverse effects can be increased when Sacubitril is combined with Azapropazone.Withdrawn
AzelastineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Azelastine.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Sacubitril.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Sacubitril is combined with Balsalazide.Approved, Investigational
BarbexacloneBarbexaclone may increase the hypotensive activities of Sacubitril.Experimental
BarbitalBarbital may increase the hypotensive activities of Sacubitril.Illicit
BarnidipineThe risk or severity of adverse effects can be increased when Barnidipine is combined with Sacubitril.Approved
BemiparinBemiparin may increase the hyperkalemic activities of Sacubitril.Approved
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Sacubitril.Approved, Investigational
BendroflumethiazideThe risk or severity of adverse effects can be increased when Bendroflumethiazide is combined with Sacubitril.Approved
BenoxaprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Benoxaprofen.Withdrawn
BepridilThe risk or severity of adverse effects can be increased when Bepridil is combined with Sacubitril.Approved, Withdrawn
BetaxololThe risk or severity of adverse effects can be increased when Betaxolol is combined with Sacubitril.Approved
Betulinic AcidThe risk or severity of adverse effects can be increased when Sacubitril is combined with Betulinic Acid.Investigational
BisoprololThe risk or severity of adverse effects can be increased when Bisoprolol is combined with Sacubitril.Approved
BortezomibThe risk or severity of adverse effects can be increased when Bortezomib is combined with Sacubitril.Approved, Investigational
BretyliumThe risk or severity of adverse effects can be increased when Bretylium is combined with Sacubitril.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Sacubitril.Approved
BromfenacThe risk or severity of adverse effects can be increased when Sacubitril is combined with Bromfenac.Approved
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Sacubitril.Approved, Investigational
BucillamineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Bucillamine.Investigational
BumetanideThe risk or severity of adverse effects can be increased when Bumetanide is combined with Sacubitril.Approved
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Sacubitril.Approved, Investigational
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Sacubitril.Approved
CandesartanThe risk or severity of adverse effects can be increased when Candesartan is combined with Sacubitril.Approved
CandoxatrilThe risk or severity of adverse effects can be increased when Candoxatril is combined with Sacubitril.Experimental
CaptoprilThe risk or severity of adverse effects can be increased when Captopril is combined with Sacubitril.Approved
CarbetocinThe risk or severity of adverse effects can be increased when Carbetocin is combined with Sacubitril.Approved
CarprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Carprofen.Approved, Vet Approved, Withdrawn
CarteololThe risk or severity of adverse effects can be increased when Carteolol is combined with Sacubitril.Approved
CarvedilolThe risk or severity of adverse effects can be increased when Carvedilol is combined with Sacubitril.Approved, Investigational
CastanospermineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Castanospermine.Experimental
CelecoxibThe risk or severity of adverse effects can be increased when Sacubitril is combined with Celecoxib.Approved, Investigational
CertoparinCertoparin may increase the hyperkalemic activities of Sacubitril.Approved
ChloroquineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Chloroquine.Approved, Vet Approved
ChlorothiazideThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Sacubitril.Approved, Vet Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Sacubitril.Approved, Vet Approved
ChlorthalidoneThe risk or severity of adverse effects can be increased when Chlorthalidone is combined with Sacubitril.Approved
Choline magnesium trisalicylateThe risk or severity of adverse effects can be increased when Sacubitril is combined with Trisalicylate-choline.Approved
CilazaprilThe risk or severity of adverse effects can be increased when Cilazapril is combined with Sacubitril.Approved
CilnidipineThe risk or severity of adverse effects can be increased when Cilnidipine is combined with Sacubitril.Approved
CiprofloxacinSacubitril may increase the arrhythmogenic activities of Ciprofloxacin.Approved, Investigational
ClevidipineThe risk or severity of adverse effects can be increased when Clevidipine is combined with Sacubitril.Approved
ClofarabineThe risk or severity of adverse effects can be increased when Clofarabine is combined with Sacubitril.Approved, Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Sacubitril.Approved, Vet Approved
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Sacubitril.Approved
ClonixinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Clonixin.Approved
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Sacubitril.Approved
ConivaptanThe risk or severity of adverse effects can be increased when Conivaptan is combined with Sacubitril.Approved, Investigational
CurcuminThe risk or severity of adverse effects can be increased when Sacubitril is combined with Curcumin.Investigational
CyclosporineSacubitril may increase the hyperkalemic activities of Cyclosporine.Approved, Investigational, Vet Approved
D-LimoneneThe risk or severity of adverse effects can be increased when Sacubitril is combined with D-Limonene.Investigational
DalteparinDalteparin may increase the hyperkalemic activities of Sacubitril.Approved
DapagliflozinThe risk or severity of adverse effects can be increased when Dapagliflozin is combined with Sacubitril.Approved
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Sacubitril.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Sacubitril.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Sacubitril.Approved, Vet Approved
DiclofenacThe risk or severity of adverse effects can be increased when Sacubitril is combined with Diclofenac.Approved, Vet Approved
DiclofenamideThe risk or severity of adverse effects can be increased when Diclofenamide is combined with Sacubitril.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Sacubitril is combined with Diflunisal.Approved
DiltiazemThe risk or severity of adverse effects can be increased when Diltiazem is combined with Sacubitril.Approved
DinutuximabThe risk or severity of adverse effects can be increased when Dinutuximab is combined with Sacubitril.Approved
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Sacubitril.Approved
DoxazosinThe risk or severity of adverse effects can be increased when Doxazosin is combined with Sacubitril.Approved
DrospirenoneSacubitril may increase the hyperkalemic activities of Drospirenone.Approved
DroxicamThe risk or severity of adverse effects can be increased when Sacubitril is combined with Droxicam.Approved
DuloxetineSacubitril may increase the orthostatic hypotensive activities of Duloxetine.Approved
DuvelisibThe risk or severity of adverse effects can be increased when Sacubitril is combined with Duvelisib.Investigational
E-6201The risk or severity of adverse effects can be increased when Sacubitril is combined with E6201.Investigational
EbselenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Ebselen.Investigational
EfonidipineThe risk or severity of adverse effects can be increased when Efonidipine is combined with Sacubitril.Approved
EmpagliflozinThe risk or severity of adverse effects can be increased when Empagliflozin is combined with Sacubitril.Approved
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Sacubitril.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Enalaprilat is combined with Sacubitril.Approved
EnoxaparinEnoxaparin may increase the hyperkalemic activities of Sacubitril.Approved
EpirizoleThe risk or severity of adverse effects can be increased when Sacubitril is combined with Epirizole.Approved
EplerenoneEplerenone may increase the hyperkalemic activities of Sacubitril.Approved
EpoprostenolThe risk or severity of adverse effects can be increased when Epoprostenol is combined with Sacubitril.Approved
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Sacubitril.Approved
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Sacubitril.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Etacrynic acid is combined with Sacubitril.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Sacubitril is combined with Etanercept.Approved, Investigational
EtodolacThe risk or severity of adverse effects can be increased when Sacubitril is combined with Etodolac.Approved, Investigational, Vet Approved
EtofenamateThe risk or severity of adverse effects can be increased when Sacubitril is combined with Etofenamate.Approved
EtoricoxibThe risk or severity of adverse effects can be increased when Sacubitril is combined with Etoricoxib.Approved, Investigational
Evening primrose oilThe risk or severity of adverse effects can be increased when Sacubitril is combined with Evening primrose oil.Approved
exisulindThe risk or severity of adverse effects can be increased when Sacubitril is combined with exisulind.Investigational
FelodipineThe risk or severity of adverse effects can be increased when Felodipine is combined with Sacubitril.Approved, Investigational
FenbufenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Fenbufen.Approved
FenoldopamThe risk or severity of adverse effects can be increased when Fenoldopam is combined with Sacubitril.Approved
FenoprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Fenoprofen.Approved
FimasartanThe risk or severity of adverse effects can be increased when Fimasartan is combined with Sacubitril.Approved
FloctafenineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Floctafenine.Approved, Withdrawn
FlunixinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Flunixin.Vet Approved
FlurbiprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Flurbiprofen.Approved, Investigational
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Sacubitril.Approved
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Sacubitril.Approved, Vet Approved
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Sacubitril.Approved, Investigational
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Sacubitril.Approved, Vet Approved
HeparinHeparin may increase the hyperkalemic activities of Sacubitril.Approved, Investigational
HexobarbitalHexobarbital may increase the hypotensive activities of Sacubitril.Approved
HigenamineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Higenamine.Investigational
HydralazineThe risk or severity of adverse effects can be increased when Hydralazine is combined with Sacubitril.Approved
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Hydrochlorothiazide is combined with Sacubitril.Approved, Vet Approved
HydroflumethiazideThe risk or severity of adverse effects can be increased when Hydroflumethiazide is combined with Sacubitril.Approved
IbuprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Ibuprofen.Approved
IbuproxamThe risk or severity of adverse effects can be increased when Sacubitril is combined with Ibuproxam.Withdrawn
IcatibantThe risk or severity of adverse effects can be increased when Sacubitril is combined with Icatibant.Approved
IloprostThe risk or severity of adverse effects can be increased when Iloprost is combined with Sacubitril.Approved, Investigational
ImidaprilThe risk or severity of adverse effects can be increased when Imidapril is combined with Sacubitril.Investigational
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Sacubitril.Approved
IndapamideThe risk or severity of adverse effects can be increased when Indapamide is combined with Sacubitril.Approved
IndomethacinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Indomethacin.Approved, Investigational
IndoprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Indoprofen.Withdrawn
IndoraminThe risk or severity of adverse effects can be increased when Indoramin is combined with Sacubitril.Withdrawn
IrbesartanThe risk or severity of adverse effects can be increased when Irbesartan is combined with Sacubitril.Approved, Investigational
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Sacubitril.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Sacubitril.Approved, Vet Approved
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Sacubitril.Approved
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Isosorbide Mononitrate is combined with Sacubitril.Approved
IsoxicamThe risk or severity of adverse effects can be increased when Sacubitril is combined with Isoxicam.Withdrawn
IsoxsuprineThe risk or severity of adverse effects can be increased when Isoxsuprine is combined with Sacubitril.Approved, Withdrawn
IsradipineThe risk or severity of adverse effects can be increased when Isradipine is combined with Sacubitril.Approved
KebuzoneThe risk or severity of adverse effects can be increased when Sacubitril is combined with Kebuzone.Experimental
KetoprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Ketoprofen.Approved, Vet Approved
KetorolacThe risk or severity of adverse effects can be increased when Sacubitril is combined with Ketorolac.Approved
LabetalolThe risk or severity of adverse effects can be increased when Labetalol is combined with Sacubitril.Approved
LacidipineThe risk or severity of adverse effects can be increased when Lacidipine is combined with Sacubitril.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Sacubitril is combined with Leflunomide.Approved, Investigational
LercanidipineThe risk or severity of adverse effects can be increased when Lercanidipine is combined with Sacubitril.Approved, Investigational
LevobunololThe risk or severity of adverse effects can be increased when Levobunolol is combined with Sacubitril.Approved
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Sacubitril.Approved
LevodopaSacubitril may increase the orthostatic hypotensive activities of Levodopa.Approved
LevosimendanThe risk or severity of adverse effects can be increased when Levosimendan is combined with Sacubitril.Approved, Investigational
LisinoprilThe risk or severity of adverse effects can be increased when Lisinopril is combined with Sacubitril.Approved, Investigational
LisofyllineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Lisofylline.Investigational
LithiumThe serum concentration of Lithium can be increased when it is combined with Sacubitril.Approved
LofexidineThe risk or severity of adverse effects can be increased when Lofexidine is combined with Sacubitril.Approved, Investigational
LornoxicamThe risk or severity of adverse effects can be increased when Sacubitril is combined with Lornoxicam.Approved
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Sacubitril.Approved
LoxoprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Loxoprofen.Approved
LumiracoxibThe risk or severity of adverse effects can be increased when Sacubitril is combined with Lumiracoxib.Approved, Investigational
Magnesium salicylateThe risk or severity of adverse effects can be increased when Sacubitril is combined with Magnesium salicylate.Approved
MannitolThe risk or severity of adverse effects can be increased when Mannitol is combined with Sacubitril.Approved, Investigational
MasoprocolThe risk or severity of adverse effects can be increased when Sacubitril is combined with Masoprocol.Approved
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Sacubitril.Approved
Meclofenamic acidThe risk or severity of adverse effects can be increased when Sacubitril is combined with Meclofenamic acid.Approved, Vet Approved
Mefenamic acidThe risk or severity of adverse effects can be increased when Sacubitril is combined with Mefenamic acid.Approved
MeloxicamThe risk or severity of adverse effects can be increased when Sacubitril is combined with Meloxicam.Approved, Vet Approved
MesalazineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Mesalazine.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Sacubitril is combined with Metamizole.Withdrawn
MethazolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Sacubitril.Approved
MethohexitalMethohexital may increase the hypotensive activities of Sacubitril.Approved
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Sacubitril.Approved
MethyldopaThe risk or severity of adverse effects can be increased when Methyldopa is combined with Sacubitril.Approved
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Sacubitril.Approved
MetipranololThe risk or severity of adverse effects can be increased when Metipranolol is combined with Sacubitril.Approved
MetolazoneThe risk or severity of adverse effects can be increased when Metolazone is combined with Sacubitril.Approved
MetoprololThe risk or severity of adverse effects can be increased when Metoprolol is combined with Sacubitril.Approved, Investigational
MinoxidilThe risk or severity of adverse effects can be increased when Minoxidil is combined with Sacubitril.Approved
MizoribineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Mizoribine.Investigational
MoexiprilThe risk or severity of adverse effects can be increased when Moexipril is combined with Sacubitril.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Sacubitril.Approved, Investigational
MoxonidineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Sacubitril.Approved
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Sacubitril is combined with Mycophenolate mofetil.Approved, Investigational
Mycophenolic acidThe risk or severity of adverse effects can be increased when Sacubitril is combined with Mycophenolic acid.Approved
NabiloneThe risk or severity of adverse effects can be increased when Nabilone is combined with Sacubitril.Approved, Investigational
NabumetoneThe risk or severity of adverse effects can be increased when Sacubitril is combined with Nabumetone.Approved
NadololThe risk or severity of adverse effects can be increased when Nadolol is combined with Sacubitril.Approved
NadroparinNadroparin may increase the hyperkalemic activities of Sacubitril.Approved
NafamostatThe risk or severity of adverse effects can be increased when Sacubitril is combined with Nafamostat.Approved, Investigational
NaftifineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Naftifine.Approved
NaproxenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Naproxen.Approved, Vet Approved
NebivololThe risk or severity of adverse effects can be increased when Nebivolol is combined with Sacubitril.Approved, Investigational
NepafenacThe risk or severity of adverse effects can be increased when Sacubitril is combined with Nepafenac.Approved
NesiritideThe risk or severity of adverse effects can be increased when Nesiritide is combined with Sacubitril.Approved, Investigational
NicardipineThe risk or severity of adverse effects can be increased when Nicardipine is combined with Sacubitril.Approved
NicorandilNicorandil may increase the hyperkalemic activities of Sacubitril.Approved
NifedipineThe risk or severity of adverse effects can be increased when Nifedipine is combined with Sacubitril.Approved
Niflumic AcidThe risk or severity of adverse effects can be increased when Sacubitril is combined with Niflumic Acid.Approved
NilvadipineThe risk or severity of adverse effects can be increased when Nilvadipine is combined with Sacubitril.Approved
NimesulideThe risk or severity of adverse effects can be increased when Sacubitril is combined with Nimesulide.Approved, Withdrawn
NimodipineThe risk or severity of adverse effects can be increased when Nimodipine is combined with Sacubitril.Approved
NisoldipineThe risk or severity of adverse effects can be increased when Nisoldipine is combined with Sacubitril.Approved
NitrendipineThe risk or severity of adverse effects can be increased when Nitrendipine is combined with Sacubitril.Approved
Nitric OxideThe risk or severity of adverse effects can be increased when Nitric Oxide is combined with Sacubitril.Approved
NitroaspirinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Nitroaspirin.Investigational
NitroglycerinThe risk or severity of adverse effects can be increased when Nitroglycerin is combined with Sacubitril.Approved, Investigational
NitroprussideThe risk or severity of adverse effects can be increased when Nitroprusside is combined with Sacubitril.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Obinutuzumab is combined with Sacubitril.Approved
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Sacubitril.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Olopatadine.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Olsalazine.Approved
OmapatrilatThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Sacubitril.Investigational
OrgoteinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Orgotein.Vet Approved
OxaprozinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Oxaprozin.Approved
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Sacubitril.Approved
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Sacubitril is combined with Oxyphenbutazone.Withdrawn
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Sacubitril.Approved, Vet Approved
PapaverineThe risk or severity of adverse effects can be increased when Papaverine is combined with Sacubitril.Approved
ParecoxibThe risk or severity of adverse effects can be increased when Sacubitril is combined with Parecoxib.Approved
ParnaparinParnaparin may increase the hyperkalemic activities of Sacubitril.Approved
PenbutololThe risk or severity of adverse effects can be increased when Penbutolol is combined with Sacubitril.Approved, Investigational
PentobarbitalPentobarbital may increase the hypotensive activities of Sacubitril.Approved, Vet Approved
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Sacubitril.Approved
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Sacubitril.Approved
PhenobarbitalPhenobarbital may increase the hypotensive activities of Sacubitril.Approved
PhenoxybenzamineThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Sacubitril.Approved
PhentolamineThe risk or severity of adverse effects can be increased when Phentolamine is combined with Sacubitril.Approved
PhenylbutazoneThe risk or severity of adverse effects can be increased when Sacubitril is combined with Phenylbutazone.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Sacubitril is combined with Pimecrolimus.Approved, Investigational
PindololThe risk or severity of adverse effects can be increased when Pindolol is combined with Sacubitril.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Sacubitril.Approved
PirfenidoneThe risk or severity of adverse effects can be increased when Sacubitril is combined with Pirfenidone.Investigational
PiroxicamThe risk or severity of adverse effects can be increased when Sacubitril is combined with Piroxicam.Approved, Investigational
PramipexoleThe risk or severity of adverse effects can be increased when Pramipexole is combined with Sacubitril.Approved, Investigational
PrazosinThe risk or severity of adverse effects can be increased when Prazosin is combined with Sacubitril.Approved
PrimidonePrimidone may increase the hypotensive activities of Sacubitril.Approved, Vet Approved
PropacetamolThe risk or severity of adverse effects can be increased when Sacubitril is combined with Propacetamol.Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Sacubitril.Approved, Investigational, Vet Approved
PropranololThe risk or severity of adverse effects can be increased when Propranolol is combined with Sacubitril.Approved, Investigational
PTC299The risk or severity of adverse effects can be increased when Sacubitril is combined with PTC299.Investigational
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Sacubitril.Approved
QuinaprilThe risk or severity of adverse effects can be increased when Quinapril is combined with Sacubitril.Approved, Investigational
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Sacubitril.Approved
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Sacubitril.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Sacubitril.Approved
RescinnamineThe risk or severity of adverse effects can be increased when Rescinnamine is combined with Sacubitril.Approved
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Sacubitril.Approved
ResveratrolThe risk or severity of adverse effects can be increased when Sacubitril is combined with Resveratrol.Experimental, Investigational
ReviparinReviparin may increase the hyperkalemic activities of Sacubitril.Approved
RiociguatThe risk or severity of adverse effects can be increased when Riociguat is combined with Sacubitril.Approved
RisperidoneSacubitril may increase the hypotensive activities of Risperidone.Approved, Investigational
RofecoxibThe risk or severity of adverse effects can be increased when Sacubitril is combined with Rofecoxib.Investigational, Withdrawn
RopiniroleThe risk or severity of adverse effects can be increased when Ropinirole is combined with Sacubitril.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Sacubitril.Approved
RotigotineThe risk or severity of adverse effects can be increased when Rotigotine is combined with Sacubitril.Approved
SalicylamideThe risk or severity of adverse effects can be increased when Sacubitril is combined with Salicylamide.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Sacubitril is combined with Salicylic acid.Approved, Vet Approved
SalsalateThe risk or severity of adverse effects can be increased when Sacubitril is combined with Salsalate.Approved
SecobarbitalSecobarbital may increase the hypotensive activities of Sacubitril.Approved, Vet Approved
SelegilineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Selegiline.Approved, Investigational, Vet Approved
SeratrodastThe risk or severity of adverse effects can be increased when Sacubitril is combined with Seratrodast.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sacubitril is combined with Sevoflurane.Approved, Vet Approved
Sodium NitriteThe risk or severity of adverse effects can be increased when Sacubitril is combined with Sodium Nitrite.Approved
SotalolThe risk or severity of adverse effects can be increased when Sotalol is combined with Sacubitril.Approved
SpiraprilThe risk or severity of adverse effects can be increased when Spirapril is combined with Sacubitril.Approved
SpironolactoneSacubitril may increase the hyperkalemic activities of Spironolactone.Approved
SRT501The risk or severity of adverse effects can be increased when Sacubitril is combined with SRT501.Investigational
StreptokinaseThe risk or severity of adverse effects can be increased when Sacubitril is combined with Streptokinase.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sacubitril is combined with Sufentanil.Approved, Investigational
SulfasalazineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Sulfasalazine.Approved
SulindacThe risk or severity of adverse effects can be increased when Sacubitril is combined with Sulindac.Approved
SuprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Suprofen.Approved, Withdrawn
TamsulosinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tamsulosin.Approved, Investigational
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Sacubitril.Approved, Investigational
TemocaprilThe risk or severity of adverse effects can be increased when Temocapril is combined with Sacubitril.Experimental, Investigational
TenoxicamThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tenoxicam.Approved
TepoxalinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tepoxalin.Vet Approved
TerazosinThe risk or severity of adverse effects can be increased when Terazosin is combined with Sacubitril.Approved
TeriflunomideThe risk or severity of adverse effects can be increased when Sacubitril is combined with Teriflunomide.Approved
ThalidomideThe risk or severity of adverse effects can be increased when Sacubitril is combined with Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThiamylal may increase the hypotensive activities of Sacubitril.Approved, Vet Approved
ThiopentalThiopental may increase the hypotensive activities of Sacubitril.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Thioridazine.Withdrawn
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tiaprofenic acid.Approved
TimololThe risk or severity of adverse effects can be increased when Timolol is combined with Sacubitril.Approved
TinoridineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tinoridine.Investigational
TinzaparinTinzaparin may increase the hyperkalemic activities of Sacubitril.Approved
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Sacubitril.Approved
TolazolineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tolazoline.Approved, Vet Approved
TolcaponeThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tolcapone.Approved, Withdrawn
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tolfenamic Acid.Approved
TolmetinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tolmetin.Approved
TolvaptanTolvaptan may increase the hyperkalemic activities of Sacubitril.Approved
TorasemideThe risk or severity of adverse effects can be increased when Torasemide is combined with Sacubitril.Approved
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Sacubitril.Approved
TranilastThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tranilast.Approved, Investigational
TranylcypromineThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tranylcypromine.Approved
TretinoinThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamtereneSacubitril may increase the hyperkalemic activities of Triamterene.Approved
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Sacubitril.Approved, Vet Approved
ValdecoxibThe risk or severity of adverse effects can be increased when Sacubitril is combined with Valdecoxib.Investigational, Withdrawn
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Sacubitril.Approved, Investigational
VerapamilThe risk or severity of adverse effects can be increased when Verapamil is combined with Sacubitril.Approved
ZaltoprofenThe risk or severity of adverse effects can be increased when Sacubitril is combined with Zaltoprofen.Approved
ZileutonThe risk or severity of adverse effects can be increased when Sacubitril is combined with Zileuton.Approved, Investigational, Withdrawn
ZomepiracThe risk or severity of adverse effects can be increased when Sacubitril is combined with Zomepirac.Withdrawn
Food InteractionsNo interactions found.
References
Synthesis ReferenceNot Available
General References
  1. Gu J, Noe A, Chandra P, Al-Fayoumi S, Ligueros-Saylan M, Sarangapani R, Maahs S, Ksander G, Rigel DF, Jeng AY, Lin TH, Zheng W, Dole WP: Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14. doi: 10.1177/0091270009343932. Epub 2009 Nov 23. [PubMed:19934029 ]
  2. Mills J, Vardeny O: The Role of Neprilysin Inhibitors in Cardiovascular Disease. Curr Heart Fail Rep. 2015 Dec;12(6):389-94. doi: 10.1007/s11897-015-0270-8. [PubMed:26466607 ]
  3. King JB, Bress AP, Reese AD, Munger MA: Neprilysin Inhibition in Heart Failure with Reduced Ejection Fraction: A Clinical Review. Pharmacotherapy. 2015 Sep;35(9):823-37. doi: 10.1002/phar.1629. [PubMed:26406774 ]
External Links
ATC CodesC09DX04 — Valsartan and sacubitril
AHFS Codes
  • 24:32.92
PDB EntriesNot Available
FDA labelDownload (1.28 MB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceMild and Moderate Renal Impairment1
2CompletedNot AvailableConcurrent Obesity / Hypertensive1
2CompletedNot AvailableHepatic Impairment1
2CompletedNot AvailableMild to Moderate Hypertension1
2CompletedNot AvailableSalt-sensitive Hypertension1
2CompletedTreatmentChronic Heart Failure (CHF)1
2CompletedTreatmentHeart Failure With Reduced Ejection Fraction (HFrEF)1
2CompletedTreatmentHeart Failure, Unspecified1
2CompletedTreatmentHypertension,Essential1
2CompletedTreatmentHypertensive5
2CompletedTreatmentSystolic Hypertension1
2Not Yet RecruitingTreatmentPeripheral Arterial Disease (PAD)1
2RecruitingTreatmentDiastolic Dysfunction1
2, 3RecruitingTreatmentPediatric Heart Failure1
3Active Not RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)1
3Active Not RecruitingTreatmentHeart Failure With Reduced Ejection Fraction (HFrEF)1
3CompletedTreatmentHypertension With Renal Dysfunction1
3CompletedTreatmentHypertension,Essential4
3CompletedTreatmentHypertensive1
3CompletedTreatmentSevere Hypertension1
3RecruitingTreatmentAcute Myocardial Infarction (AMI)1
3RecruitingTreatmentChronic Heart Failure With Reduced Ejection Fraction (HFrEF)2
3RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)1
3RecruitingTreatmentHeart Failure, Unspecified1
3TerminatedTreatmentHeart Failure With Reduced Ejection Fraction (HFrEF)1
3WithdrawnTreatmentHypertensive1
4Active Not RecruitingSupportive CareHearth Failure With Reduced Ejection Fraction (HFrEF)1
4Active Not RecruitingTreatmentMitral Valve Insufficiency / Symptomatic left ventricular ejection fraction ≤ 35% Chronic heart failure1
4Not Yet RecruitingTreatmentCongestive Heart Failure (CHF) / Hypertensive1
4RecruitingNot AvailableHeart Failure With Reduced Ejection Fraction (HFrEF)1
4RecruitingOtherHeart Failure, Unspecified1
4RecruitingSupportive CareAcute Heart Failure (AHF)1
4RecruitingSupportive CareHeart Failure With Reduced Ejection Fraction (HFrEF)1
4RecruitingTreatmentBody Composition / Exercise Tolerance / Heart Failure, Unspecified / Strength, Muscle / Vasodilation1
4RecruitingTreatmentChronic Heart Failure With Reduced Ejection Fraction (HFrEF)1
4RecruitingTreatmentHeart Failure With Reduced Ejection Fraction (HFrEF)1
4RecruitingTreatmentHeart Failure, Unspecified3
Not AvailableAvailableNot AvailableHeart Failure With Reduced Ejection Fraction (HFrEF)1
Not AvailableRecruitingNot AvailableHeart Failure, Unspecified1
Not AvailableRecruitingOtherChronic Heart Failure (CHF) / Sleep Apnea Syndrome1
Not AvailableRecruitingTreatmentCongestive Heart Failure (CHF)1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral
Tablet, film coatedOral
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8796331 No2003-01-142023-01-14Us
US8101659 No2003-01-142023-01-14Us
US7468390 No2003-11-272023-11-27Us
US8404744 No2003-01-142023-01-14Us
US8877938 No2007-05-272027-05-27Us
US9388134 No2006-11-082026-11-08Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.000942 mg/mLALOGPS
logP3.9ALOGPS
logP3.79ChemAxon
logS-5.6ALOGPS
pKa (Strongest Acidic)4.18ChemAxon
pKa (Strongest Basic)-1.6ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area92.7 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity114.06 m3·mol-1ChemAxon
Polarizability45.41 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET featuresNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as biphenyls and derivatives. These are organic compounds containing to benzene rings linked together by a C-C bond.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBiphenyls and derivatives
Direct ParentBiphenyls and derivatives
Alternative ParentsGamma amino acids and derivatives / Amphetamines and derivatives / Fatty acid esters / N-acyl amines / Dicarboxylic acids and derivatives / Secondary carboxylic acid amides / Carboxylic acid esters / Carboxylic acids / Organonitrogen compounds / Organic oxides
SubstituentsBiphenyl / Gamma amino acid or derivatives / Amphetamine or derivatives / Fatty acid ester / Dicarboxylic acid or derivatives / Fatty acyl / Fatty amide / N-acyl-amine / Carboxamide group / Carboxylic acid ester
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonistinhibitor
General Function:
Zinc ion binding
Specific Function:
Thermolysin-like specificity, but is almost confined on acting on polypeptides of up to 30 amino acids (PubMed:15283675, PubMed:8168535). Biologically important in the destruction of opioid peptides such as Met- and Leu-enkephalins by cleavage of a Gly-Phe bond (PubMed:17101991). Able to cleave angiotensin-1, angiotensin-2 and angiotensin 1-9 (PubMed:15283675). Involved in the degradation of at...
Gene Name:
MME
Uniprot ID:
P08473
Uniprot Name:
Neprilysin
Molecular Weight:
85513.225 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Uniprot Name:
Solute carrier organic anion transporter family member 1B1
Molecular Weight:
76447.99 Da
References
  1. Mills J, Vardeny O: The Role of Neprilysin Inhibitors in Cardiovascular Disease. Curr Heart Fail Rep. 2015 Dec;12(6):389-94. doi: 10.1007/s11897-015-0270-8. [PubMed:26466607 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Uniprot Name:
Solute carrier organic anion transporter family member 1B3
Molecular Weight:
77402.175 Da
References
  1. Mills J, Vardeny O: The Role of Neprilysin Inhibitors in Cardiovascular Disease. Curr Heart Fail Rep. 2015 Dec;12(6):389-94. doi: 10.1007/s11897-015-0270-8. [PubMed:26466607 ]
Drug created on October 29, 2015 15:43 / Updated on September 01, 2017 12:04