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Identification
NameEplerenone
Accession NumberDB00700  (APRD00707)
TypeSmall Molecule
GroupsApproved
Description

Eplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors.

Structure
Thumb
Synonyms
Epoxymexrenone
Inspra
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eplerenonetablet, film coated25 mg/1oralAvera Mc Kennan Hospital2015-06-17Not applicableUs
Eplerenonetablet, film coated50 mg/1oralGreenstone LLC2002-09-27Not applicableUs
Eplerenonetablet, film coated25 mg/1oralGreenstone LLC2002-09-27Not applicableUs
Inspratablet, film coated25 mg/1oralG.D. Searle LLC Division of Pfizer Inc2002-09-27Not applicableUs
Inspratablet50 mgoralPfizer Canada Inc2009-05-05Not applicableCanada
Inspratablet25 mgoralPfizer Canada Inc2009-05-08Not applicableCanada
Inspratablet25 mg/1oralRebel Distributors Corp2002-09-27Not applicableUs
Inspratablet, film coated50 mg/1oralG.D. Searle LLC Division of Pfizer Inc2002-09-27Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eplerenonetablet25 mg/1oralAmerican Health Packaging2015-09-01Not applicableUs
Eplerenonetablet25 mg/1oralEon Labs, Inc.2008-08-01Not applicableUs
Eplerenonetablet50 mg/1oralApotex Corp2008-07-30Not applicableUs
Eplerenonetablet25 mg/1oralApotex Corp2008-07-30Not applicableUs
Eplerenonetablet25 mg/1oralPhysicians Total Care, Inc.2009-09-14Not applicableUs
Eplerenonetablet50 mg/1oralRebel Distributors Corp.2008-08-01Not applicableUs
Eplerenonetablet50 mg/1oralUpsher Smith Laboratories, Inc.2015-03-16Not applicableUs
Eplerenonetablet25 mg/1oralUpsher Smith Laboratories, Inc.2015-03-16Not applicableUs
Eplerenonetablet50 mg/1oralEon Labs, Inc.2008-08-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII6995V82D0B
CAS number107724-20-9
WeightAverage: 414.4914
Monoisotopic: 414.204238692
Chemical FormulaC24H30O6
InChI KeyInChIKey=JUKPWJGBANNWMW-VWBFHTRKSA-N
InChI
InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1
IUPAC Name
methyl (1'R,2R,2'S,9'R,10'R,11'S,15'S,17'R)-2',15'-dimethyl-5,5'-dioxo-18'-oxaspiro[oxolane-2,14'-pentacyclo[8.8.0.0¹,¹⁷.0²,⁷.0¹¹,¹⁵]octadecan]-6'-ene-9'-carboxylate
SMILES
[H][C@@]12CC[C@@]3(CCC(=O)O3)[C@@]1(C)C[[email protected]]1O[C@@]11[C@@]2([H])[C@@H](CC2=CC(=O)CC[C@]12C)C(=O)OC
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as spironolactones and derivatives. These are steroid lactones with a structure based on the spironolactone skeleton.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassSteroid lactones
Direct ParentSpironolactones and derivatives
Alternative Parents
Substituents
  • Spironolactone
  • Oxepane
  • Gamma butyrolactone
  • Dicarboxylic acid or derivatives
  • Methyl ester
  • Oxolane
  • Cyclic ketone
  • Lactone
  • Ketone
  • Carboxylic acid ester
  • Oxacycle
  • Organoheterocyclic compound
  • Ether
  • Oxirane
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of congestive heart failure after an acute myocardial infarction.
PharmacodynamicsEplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors.
Mechanism of actionEplerenone binds to the mineralocorticoid receptor and thereby blocks the binding of aldosterone (component of the renin-angiotensin-aldosterone-system, or RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms.
Related Articles
AbsorptionThe absolute bioavailability of eplerenone is unknown.
Volume of distribution
  • 43 to 90 L
Protein binding50%
Metabolism

Eplerenone is metabolized primarily by CYP3A4, however, no active metabolites have been identified in human plasma.

Route of eliminationNot Available
Half life4-6 hours
Clearance
  • Apparent plasma cl=10 L/hr
ToxicityThe most likely symptoms of human overdosage would be anticipated to be hypotension or hyperkalemia. However, no cases of human overdosage with eplerenone have been reported.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Eplerenone Action PathwayDrug actionSMP00135
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9839
Blood Brain Barrier+0.8556
Caco-2 permeable+0.5076
P-glycoprotein substrateSubstrate0.7017
P-glycoprotein inhibitor IInhibitor0.8166
P-glycoprotein inhibitor IIInhibitor0.8066
Renal organic cation transporterNon-inhibitor0.7209
CYP450 2C9 substrateNon-substrate0.8229
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.6978
CYP450 2C9 inhibitorNon-inhibitor0.7982
CYP450 2D6 inhibitorNon-inhibitor0.931
CYP450 2C19 inhibitorNon-inhibitor0.839
CYP450 3A4 inhibitorNon-inhibitor0.8368
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8902
Ames testNon AMES toxic0.7496
CarcinogenicityNon-carcinogens0.9441
BiodegradationNot ready biodegradable0.9891
Rat acute toxicity2.4761 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9453
hERG inhibition (predictor II)Non-inhibitor0.7742
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Apotex inc
  • Sandoz inc
  • Gd searle llc
Packagers
Dosage forms
FormRouteStrength
Tabletoral25 mg/1
Tabletoral50 mg/1
Tabletoral25 mg
Tabletoral50 mg
Tablet, film coatedoral25 mg/1
Tablet, film coatedoral50 mg/1
Prices
Unit descriptionCostUnit
Inspra 25 mg tablet4.87USD tablet
Inspra 50 mg tablet4.87USD tablet
Eplerenone 25 mg tablet4.18USD tablet
Eplerenone 50 mg tablet4.18USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6410054 Yes2000-06-082020-06-08Us
US6410524 Yes2000-05-052020-05-05Us
US6495165 Yes2000-06-082020-06-08Us
US6534093 Yes2000-06-082020-06-08Us
US6558707 Yes2000-06-082020-06-08Us
US6747020 Yes2000-05-052020-05-05Us
US6863902 No2000-10-102020-10-10Us
US7157101 Yes2000-06-082020-06-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySlightly solubleNot Available
logP1.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00903 mg/mLALOGPS
logP1.67ALOGPS
logP2.33ChemAxon
logS-4.7ALOGPS
pKa (Strongest Acidic)15.11ChemAxon
pKa (Strongest Basic)-4.2ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area82.2 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity106.68 m3·mol-1ChemAxon
Polarizability43.79 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
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
References
Synthesis Reference

Bhaskar Reddy Guntoori, Svetoslav S. Bratovanov, Mohamed Ibrahim Zaki, Elena Bejan, Stephen E. Horne, “Process for the preparation and purification of eplerenone.” U.S. Patent US20080234478, issued September 25, 2008.

US20080234478
General ReferencesNot Available
External Links
ATC CodesC03DA04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (136 KB)
MSDSDownload (68.2 KB)
Interactions
Drug Interactions
Drug
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Eplerenone.
AlfuzosinAlfuzosin may increase the hypotensive activities of Eplerenone.
AmifostineEplerenone may increase the hypotensive activities of Amifostine.
AmilorideEplerenone may increase the hyperkalemic activities of Amiloride.
Ammonium chlorideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Ammonium chloride.
AprepitantThe serum concentration of Eplerenone can be increased when it is combined with Aprepitant.
ArdeparinArdeparin may increase the hyperkalemic activities of Eplerenone.
AtazanavirThe serum concentration of Eplerenone can be increased when it is combined with Atazanavir.
Azilsartan medoxomilEplerenone may increase the hyperkalemic activities of Azilsartan medoxomil.
BenazeprilEplerenone may increase the hyperkalemic activities of Benazepril.
BexaroteneThe serum concentration of Eplerenone can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Eplerenone can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Eplerenone can be decreased when it is combined with Bosentan.
BrimonidineBrimonidine may increase the antihypertensive activities of Eplerenone.
ButabarbitalButabarbital may increase the hypotensive activities of Eplerenone.
ButethalButethal may increase the hypotensive activities of Eplerenone.
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Eplerenone.
CandesartanEplerenone may increase the hyperkalemic activities of Candesartan.
CaptoprilEplerenone may increase the hyperkalemic activities of Captopril.
CelecoxibCelecoxib may decrease the antihypertensive activities of Eplerenone.
CeritinibThe serum concentration of Eplerenone can be increased when it is combined with Ceritinib.
CilazaprilEplerenone may increase the hyperkalemic activities of Cilazapril.
ClarithromycinThe serum concentration of Eplerenone can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Eplerenone can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Eplerenone can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Eplerenone can be increased when it is combined with Crizotinib.
CyclosporineEplerenone may increase the hyperkalemic activities of Cyclosporine.
DabrafenibThe serum concentration of Eplerenone can be decreased when it is combined with Dabrafenib.
DalteparinDalteparin may increase the hyperkalemic activities of Eplerenone.
DarunavirThe serum concentration of Eplerenone can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Eplerenone can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Eplerenone can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Eplerenone can be increased when it is combined with Delavirdine.
DiazoxideDiazoxide may increase the hypotensive activities of Eplerenone.
DiclofenacDiclofenac may decrease the antihypertensive activities of Eplerenone.
DiflunisalDiflunisal may decrease the antihypertensive activities of Eplerenone.
DigoxinThe therapeutic efficacy of Digoxin can be decreased when used in combination with Eplerenone.
DiltiazemThe serum concentration of Eplerenone can be increased when it is combined with Diltiazem.
DronedaroneThe serum concentration of Eplerenone can be increased when it is combined with Dronedarone.
DrospirenoneDrospirenone may increase the hyperkalemic activities of Eplerenone.
DuloxetineEplerenone may increase the orthostatic hypotensive activities of Duloxetine.
EnalaprilEplerenone may increase the hyperkalemic activities of Enalapril.
EnalaprilatEplerenone may increase the hyperkalemic activities of Enalaprilat.
EnoxaparinEnoxaparin may increase the hyperkalemic activities of Eplerenone.
EprosartanEplerenone may increase the hyperkalemic activities of Eprosartan.
ErythromycinThe serum concentration of Eplerenone can be increased when it is combined with Erythromycin.
EtodolacEtodolac may decrease the antihypertensive activities of Eplerenone.
FenoprofenFenoprofen may decrease the antihypertensive activities of Eplerenone.
FloctafenineFloctafenine may decrease the antihypertensive activities of Eplerenone.
FluconazoleThe serum concentration of Eplerenone can be increased when it is combined with Fluconazole.
FlurbiprofenFlurbiprofen may decrease the antihypertensive activities of Eplerenone.
FosamprenavirThe serum concentration of Eplerenone can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Eplerenone can be increased when it is combined with Fosaprepitant.
FosinoprilEplerenone may increase the hyperkalemic activities of Fosinopril.
Fusidic AcidThe serum concentration of Eplerenone can be increased when it is combined with Fusidic Acid.
HeparinHeparin may increase the hyperkalemic activities of Eplerenone.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Eplerenone.
HexobarbitalHexobarbital may increase the hypotensive activities of Eplerenone.
IbuprofenIbuprofen may decrease the antihypertensive activities of Eplerenone.
IdelalisibThe serum concentration of Eplerenone can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Eplerenone can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Eplerenone can be increased when it is combined with Indinavir.
IndomethacinIndomethacin may decrease the antihypertensive activities of Eplerenone.
InfliximabInfliximab may decrease the antihypertensive activities of Eplerenone.
IrbesartanEplerenone may increase the hyperkalemic activities of Irbesartan.
IsavuconazoniumThe serum concentration of Eplerenone can be increased when it is combined with Isavuconazonium.
ItraconazoleThe serum concentration of Eplerenone can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Eplerenone can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Eplerenone can be increased when it is combined with Ketoconazole.
KetoprofenKetoprofen may decrease the antihypertensive activities of Eplerenone.
KetorolacKetorolac may decrease the antihypertensive activities of Eplerenone.
LevodopaEplerenone may increase the orthostatic hypotensive activities of Levodopa.
LisinoprilEplerenone may increase the hyperkalemic activities of Lisinopril.
LithiumThe serum concentration of Lithium can be increased when it is combined with Eplerenone.
LosartanEplerenone may increase the hyperkalemic activities of Losartan.
LuliconazoleThe serum concentration of Eplerenone can be increased when it is combined with Luliconazole.
Mefenamic acidMefenamic acid may decrease the antihypertensive activities of Eplerenone.
MeloxicamMeloxicam may decrease the antihypertensive activities of Eplerenone.
MethohexitalMethohexital may increase the hypotensive activities of Eplerenone.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Eplerenone.
MifepristoneThe serum concentration of Eplerenone can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Eplerenone can be decreased when it is combined with Mitotane.
MoexiprilEplerenone may increase the hyperkalemic activities of Moexipril.
MolsidomineMolsidomine may increase the hypotensive activities of Eplerenone.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Eplerenone.
MoxonidineMoxonidine may increase the hypotensive activities of Eplerenone.
NabumetoneNabumetone may decrease the antihypertensive activities of Eplerenone.
NadroparinNadroparin may increase the hyperkalemic activities of Eplerenone.
NaproxenNaproxen may decrease the antihypertensive activities of Eplerenone.
NefazodoneThe serum concentration of Eplerenone can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Eplerenone can be increased when it is combined with Nelfinavir.
NicorandilNicorandil may increase the hypotensive activities of Eplerenone.
NilotinibThe serum concentration of Eplerenone can be increased when it is combined with Nilotinib.
NitrofurantoinNitrofurantoin may increase the hyperkalemic activities of Eplerenone.
ObinutuzumabEplerenone may increase the hypotensive activities of Obinutuzumab.
OlmesartanEplerenone may increase the hyperkalemic activities of Olmesartan.
OxaprozinOxaprozin may decrease the antihypertensive activities of Eplerenone.
PalbociclibThe serum concentration of Eplerenone can be increased when it is combined with Palbociclib.
PentobarbitalPentobarbital may increase the hypotensive activities of Eplerenone.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Eplerenone.
PerindoprilEplerenone may increase the hyperkalemic activities of Perindopril.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Eplerenone.
PhenytoinThe metabolism of Eplerenone can be increased when combined with Phenytoin.
PiroxicamPiroxicam may decrease the antihypertensive activities of Eplerenone.
PosaconazoleThe serum concentration of Eplerenone can be increased when it is combined with Posaconazole.
Potassium ChlorideEplerenone may increase the hyperkalemic activities of Potassium Chloride.
Potassium CitrateEplerenone may increase the hyperkalemic activities of Potassium Citrate.
Potassium IodideEplerenone may increase the hyperkalemic activities of Potassium Iodide.
PrimidonePrimidone may increase the hypotensive activities of Eplerenone.
QuinaprilEplerenone may increase the hyperkalemic activities of Quinapril.
QuinidineThe therapeutic efficacy of Quinidine can be decreased when used in combination with Eplerenone.
QuinineQuinine may increase the hypotensive activities of Eplerenone.
RamiprilEplerenone may increase the hyperkalemic activities of Ramipril.
RisperidoneEplerenone may increase the hypotensive activities of Risperidone.
RitonavirThe serum concentration of Eplerenone can be increased when it is combined with Ritonavir.
RituximabEplerenone may increase the hypotensive activities of Rituximab.
SaquinavirThe serum concentration of Eplerenone can be increased when it is combined with Saquinavir.
SecobarbitalSecobarbital may increase the hypotensive activities of Eplerenone.
SiltuximabThe serum concentration of Eplerenone can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Eplerenone can be increased when it is combined with Simeprevir.
SpironolactoneEplerenone may increase the hyperkalemic activities of Spironolactone.
St. John's WortThe serum concentration of Eplerenone can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe serum concentration of Eplerenone can be increased when it is combined with Stiripentol.
SulindacSulindac may decrease the antihypertensive activities of Eplerenone.
TacrolimusEplerenone may increase the hyperkalemic activities of Tacrolimus.
TadalafilTadalafil may increase the antihypertensive activities of Eplerenone.
TelaprevirThe serum concentration of Eplerenone can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Eplerenone can be increased when it is combined with Telithromycin.
TelmisartanEplerenone may increase the hyperkalemic activities of Telmisartan.
Tiaprofenic acidTiaprofenic acid may decrease the antihypertensive activities of Eplerenone.
TinzaparinTinzaparin may increase the hyperkalemic activities of Eplerenone.
TocilizumabThe serum concentration of Eplerenone can be decreased when it is combined with Tocilizumab.
TolmetinTolmetin may decrease the antihypertensive activities of Eplerenone.
TolvaptanTolvaptan may increase the hyperkalemic activities of Eplerenone.
TrandolaprilEplerenone may increase the hyperkalemic activities of Trandolapril.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Eplerenone.
TreprostinilTreprostinil may increase the hypotensive activities of Eplerenone.
TriamtereneEplerenone may increase the hyperkalemic activities of Triamterene.
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Eplerenone.
ValsartanEplerenone may increase the hyperkalemic activities of Valsartan.
VardenafilVardenafil may increase the antihypertensive activities of Eplerenone.
VerapamilThe serum concentration of Eplerenone can be increased when it is combined with Verapamil.
VoriconazoleThe serum concentration of Eplerenone can be increased when it is combined with Voriconazole.
YohimbineYohimbine may decrease the antihypertensive activities of Eplerenone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates target genes. The effect of MC is to increase ion and water transport and thus raise extracellular fluid volume and blood pressure and lower potassium levels.
Gene Name:
NR3C2
Uniprot ID:
P08235
Molecular Weight:
107066.575 Da
References
  1. Moore TD, Nawarskas JJ, Anderson JR: Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure. Heart Dis. 2003 Sep-Oct;5(5):354-63. [PubMed:14503934 ]
  2. Fraccarollo D, Galuppo P, Hildemann S, Christ M, Ertl G, Bauersachs J: Additive improvement of left ventricular remodeling and neurohormonal activation by aldosterone receptor blockade with eplerenone and ACE inhibition in rats with myocardial infarction. J Am Coll Cardiol. 2003 Nov 5;42(9):1666-73. [PubMed:14607457 ]
  3. Rogerson FM, Yao Y, Smith BJ, Fuller PJ: Differences in the determinants of eplerenone, spironolactone and aldosterone binding to the mineralocorticoid receptor. Clin Exp Pharmacol Physiol. 2004 Oct;31(10):704-9. [PubMed:15554912 ]
  4. 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
unknown
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 11-beta-monooxygenase activity
Specific Function:
Preferentially catalyzes the conversion of 11-deoxycorticosterone to aldosterone via corticosterone and 18-hydroxycorticosterone.
Gene Name:
CYP11B2
Uniprot ID:
P19099
Molecular Weight:
57559.62 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on June 24, 2016 03:04