Identification

Name
Nebivolol
Accession Number
DB04861
Type
Small Molecule
Groups
Approved, Investigational
Description

Nebivolol is a highly cardioselective vasodilatory beta1 receptor blocker used in treatment of hypertension. In most countries, this medication is available only by prescription. [Wikipedia]

Structure
Thumb
Synonyms
  • 1,1'-[Bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)]-2,2'-iminodiethanol
  • 1,1'-Bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2,2'-iminodiethanol
  • alpha,alpha'-(iminobismethylene)bis-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol)
  • alpha,alpha'-(iminodimethylene)bis-(6-fluoro-2-chromanmethanol)
  • Narbivolol
  • Nebivolol
  • Nebivololum
External IDs
PI-21858 / R65,824
Product Ingredients
IngredientUNIICASInChI Key
Nebivolol hydrochlorideJGS34J7L9I152520-56-4JWEXHQAEWHKGCW-VCVZPGOSSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BystolicTablet2.5 mg/1OralMed Pharma Co., Ltd.2011-06-012012-06-21Us
BystolicTablet10 mg/1OralCardinal Health2008-01-22Not applicableUs00456 1410 01 nlmimage10 6d3a36a1
BystolicTablet2.5 mgOralForest Laboratories2013-04-02Not applicableCanada
BystolicTablet5 mg/1OralAvera McKennan Hospital2015-03-192018-06-08Us69189 140520180907 15195 1qisxa7
BystolicTablet10.0 mgOralForest Laboratories2013-04-02Not applicableCanada
BystolicTablet5 mg/1OralAllergan2008-01-22Not applicableUs0456 140520180907 15195 c8ricb
BystolicTablet10 mg/1OralMed Pharma Co., Ltd.2011-06-012012-06-21Us
BystolicTablet10 mg/1OralA-S Medication Solutions2008-01-222016-09-30Us50090 130720180913 8702 3ph42
BystolicTablet10 mg/1OralCarilion Materials Management2008-01-22Not applicableUs68151 513520180907 15195 1xnkwbb
BystolicTablet20 mg/1OralA-S Medication Solutions2008-01-22Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NebivololTablet2.5 mg/1OralAmerigen Pharmaceuticals Inc.2015-04-28Not applicableUs
NebivololTablet10 mg/1OralAmerigen Pharmaceuticals Inc.2015-04-28Not applicableUs
NebivololTablet5 mg/1OralAmerigen Pharmaceuticals Inc.2015-04-28Not applicableUs
NebivololTablet20 mg/1OralAmerigen Pharmaceuticals Inc.2015-04-28Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
ByvalsonNebivolol hydrochloride (5 mg/1) + Valsartan (80 mg/1)Tablet, film coatedOralAllergan2016-06-03Not applicableUs
International/Other Brands
Lobivon / Nebicard / Nebilet / Nebilong / Nodon / Nubeta
Categories
UNII
030Y90569U
CAS number
118457-14-0
Weight
Average: 405.435
Monoisotopic: 405.175164703
Chemical Formula
C22H25F2NO4
InChI Key
KOHIRBRYDXPAMZ-UHFFFAOYSA-N
InChI
InChI=1S/C22H25F2NO4/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2
IUPAC Name
1-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2-{[2-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2-hydroxyethyl]amino}ethan-1-ol
SMILES
OC(CNCC(O)C1CCC2=C(O1)C=CC(F)=C2)C1CCC2=C(O1)C=CC(F)=C2

Pharmacology

Indication

For the treatment of essential hypertension.

Associated Conditions
Pharmacodynamics

Nebivolol is a competitive and highly selective beta-1 receptor antagonist with mild vasodilating properties, possibly due to an interaction with the L-arginine/nitric oxide pathway. In preclinical studies, nebivolol has been shown to induce endothelium-dependent arterial relaxation in a dose dependent manner, by stimulation of the release of endothelial nitric oxide. Nitric oxide acts to relax vascular smooth muscle cells and inhibits platelet aggregation and adhesion.

Mechanism of action

Nebivolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Nebivolol blocks these receptors which reverses the effects of epinephrine, lowering the heart rate and blood pressure. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. At high enough concentrations, this drug may also bind beta 2 receptors.

TargetActionsOrganism
ABeta-1 adrenergic receptor
antagonist
Human
UBeta-2 adrenergic receptor
antagonist
Human
Absorption

The absorption of nebivolol is rapid and not affected by food.

Volume of distribution
Not Available
Protein binding

98%

Metabolism

Hepatic (CYP2D6-mediated)

Route of elimination
Not Available
Half life

10 hours

Clearance
Not Available
Toxicity

The most common signs and symptoms associated with nebivolol overdosage are bradycardia and hypotension. Other important adverse events reported with nebivolol overdose include cardiac failure, dizziness, hypoglycemia, fatigue and vomiting. Other adverse events associated with β-blocker overdose include bronchospasm and heart block. The largest known ingestion of nebivolol worldwide involved a patient who ingested up to 500 mg of nebivolol along with several 100 mg tablets of acetylsalicylic acid in a suicide attempt. The patient experienced hyperhydrosis, pallor, depressed level of consciousness, hypokinesia, hypotension, sinus bradycardia, hypoglycemia, hypokalemia, respiratory failure and vomiting. The patient recovered.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Nebivolol Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*3Not AvailableC alleleEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableC alleleEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Nebivolol.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Nebivolol.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may increase the hypotensive activities of Nebivolol.
1-benzylimidazoleThe risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Nebivolol.
1,10-Phenanthroline1,10-Phenanthroline may increase the bradycardic activities of Nebivolol.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of hypertension can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Nebivolol.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of hypertension can be increased when Nebivolol is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthineThe risk or severity of adverse effects can be increased when Nebivolol is combined with 3-isobutyl-1-methyl-7H-xanthine.
3,4-MethylenedioxyamphetamineThe risk or severity of hypertension can be increased when 3,4-Methylenedioxyamphetamine is combined with Nebivolol.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Nebivolol.
Food Interactions
Not Available

References

Synthesis Reference

Thomas Bader, Alfred Stutz, Harald Hofmeier, Hans-Ulrich Bichsel, "Process for preparation of racemic Nebivolol." U.S. Patent US20070149612, issued June 28, 2007.

US20070149612
General References
  1. Gielen W, Cleophas TJ, Agrawal R: Nebivolol: a review of its clinical and pharmacological characteristics. Int J Clin Pharmacol Ther. 2006 Aug;44(8):344-57. [PubMed:16961165]
External Links
Human Metabolome Database
HMDB0015594
KEGG Drug
D05127
PubChem Compound
71301
PubChem Substance
99443225
ChemSpider
64421
BindingDB
84735
ChEBI
64019
ChEMBL
CHEMBL434394
Therapeutic Targets Database
DAP000942
PharmGKB
PA151958426
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Nebivolol
ATC Codes
C07FB12 — Nebivolol and other antihypertensivesC07AB12 — NebivololC07BB12 — Nebivolol and thiazides
AHFS Codes
  • 24:24.00 — Beta-adrenergic Blocking Agents
MSDS
Download (69.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingBasic ScienceBone, Age-related / Osteoporosis, Age-Related1
0CompletedTreatmentCardiac Steatosis and Lipotoxicity1
1CompletedTreatmentHigh Blood Pressure (Hypertension)2
2CompletedTreatmentHigh Blood Pressure (Hypertension)2
2CompletedTreatmentHypertension,Essential1
2RecruitingTreatmentStroke, Ischemic1
2, 3CompletedPreventionDiabetes Mellitus (DM) / High Blood Pressure (Hypertension)1
2, 3WithdrawnHealth Services ResearchHigh Blood Pressure (Hypertension)1
3Active Not RecruitingPreventionDuchenne's Muscular Dystrophy (DMD) / Heart Failure, Unspecified / Prophylaxis of cardiomyopathy1
3CompletedTreatmentHigh Blood Pressure (Hypertension)9
3CompletedTreatmentHigh Blood Pressure (Hypertension) / Peripheral Artery Disease (PAD)1
3CompletedTreatmentPrimary Arterial Hypertension1
3CompletedTreatmentStage 1 Hypertension / Stage 2 Hypertension1
3Unknown StatusTreatmentMarfan Syndrome1
4CompletedBasic ScienceMetabolic Syndromes1
4CompletedDiagnosticHigh Blood Pressure (Hypertension)2
4CompletedOtherHigh Blood Pressure (Hypertension) / Prehypertension2
4CompletedPreventionBlood Pressures / Hypertension Complicated / Left Ventricular Hypertrophy1
4CompletedTreatmentAltitude / Arterial hypoxia / Heart Failure, Unspecified1
4CompletedTreatmentAtherosclerosis / Endothelial Function1
4CompletedTreatmentChronic Heart Failure (CHF)1
4CompletedTreatmentCoronary Artery Disease / High Blood Pressure (Hypertension)1
4CompletedTreatmentHigh Blood Pressure (Hypertension)14
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Left Ventricular Diastolic Dysfunction1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Pre-Hypertension1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedTreatmentMicrovascular Angina1
4CompletedTreatmentStage 2 Diastolic Hypertension1
4RecruitingTreatmentDiastolic Heart Failure / Heart Failure With Preserved Ejection Fraction (HFpEF) / Pulmonary Hypertension (PH)1
4TerminatedTreatmentCoronary Artery Disease1
4TerminatedTreatmentHigh Blood Pressure (Hypertension)2
4Unknown StatusTreatmentEndothelial Dysfunction / High Blood Pressure (Hypertension) / Obstructive Sleep Apnea (OSA)1
4Unknown StatusTreatmentErectile Dysfunction (ED)1
4Unknown StatusTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableCompletedNot AvailableHeart Failure, Unspecified / High Blood Pressure (Hypertension)1
Not AvailableCompletedNot AvailableHigh Blood Pressure (Hypertension) / Multiple System Atrophy (MSA) / Progressive autonomic failure1
Not AvailableCompletedDiagnosticArterial Hypertension1
Not AvailableCompletedDiagnosticHigh Blood Pressure (Hypertension)1
Not AvailableCompletedTreatmentHigh Blood Pressure (Hypertension)2
Not AvailableRecruitingTreatmentHeart Failure, Unspecified1
Not AvailableTerminatedTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableTerminatedTreatmentHigh Blood Pressure (Hypertension) / Transplant; Failure, Kidney1
Not AvailableUnknown StatusNot AvailableHeart Failure, Unspecified1
Not AvailableUnknown StatusNot AvailableHigh Blood Pressure (Hypertension)1
Not AvailableUnknown StatusTreatmentFemale Sexual Dysfunction (FSD) / High Blood Pressure (Hypertension)1
Not AvailableWithdrawnTreatmentCentral Aortic Pressure1
Not AvailableWithdrawnTreatmentHigh Blood Pressure (Hypertension)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Forest Laboratories Inc.
  • Forest Pharmaceuticals
  • Mylan
  • Physicians Total Care Inc.
Dosage forms
FormRouteStrength
TabletOral10 mg/1
TabletOral10.0 mg
TabletOral2.5 mg
TabletOral2.5 mg/1
TabletOral20 mg/1
TabletOral20.0 mg
TabletOral5 mg/1
TabletOral5.0 mg
Tablet, film coatedOral
Prices
Unit descriptionCostUnit
Bystolic 10 mg tablet2.09USD tablet
Bystolic 20 mg tablet2.09USD tablet
Bystolic 2.5 mg tablet2.06USD tablet
Bystolic 5 mg tablet2.06USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5759580No1998-06-022015-06-02Us
US6545040No2003-04-082021-12-17Us
US7803838No2010-09-282026-08-29Us
US7838552No2010-11-232027-10-04Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0403 mg/mLALOGPS
logP2.44ALOGPS
logP3.21ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)13.52ChemAxon
pKa (Strongest Basic)8.9ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area70.95 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity103.32 m3·mol-1ChemAxon
Polarizability41.98 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8483
Blood Brain Barrier+0.7802
Caco-2 permeable-0.5549
P-glycoprotein substrateSubstrate0.7928
P-glycoprotein inhibitor INon-inhibitor0.7443
P-glycoprotein inhibitor IINon-inhibitor0.567
Renal organic cation transporterNon-inhibitor0.8016
CYP450 2C9 substrateNon-substrate0.8738
CYP450 2D6 substrateNon-substrate0.7248
CYP450 3A4 substrateNon-substrate0.6822
CYP450 1A2 substrateInhibitor0.5145
CYP450 2C9 inhibitorNon-inhibitor0.7876
CYP450 2D6 inhibitorNon-inhibitor0.5994
CYP450 2C19 inhibitorNon-inhibitor0.5923
CYP450 3A4 inhibitorNon-inhibitor0.9441
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8336
Ames testNon AMES toxic0.7132
CarcinogenicityNon-carcinogens0.9402
BiodegradationNot ready biodegradable0.9953
Rat acute toxicity2.7228 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.5769
hERG inhibition (predictor II)Inhibitor0.8381
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

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

Taxonomy

Description
This compound belongs to the class of organic compounds known as 1-benzopyrans. These are organic aromatic compounds that 1-benzopyran, a bicyclic compound made up of a benzene ring fused to a pyran, so that the oxygen atom is at the 1-position.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzopyrans
Sub Class
1-benzopyrans
Direct Parent
1-benzopyrans
Alternative Parents
Aralkylamines / Alkyl aryl ethers / Benzenoids / Aryl fluorides / Secondary alcohols / 1,2-aminoalcohols / Oxacyclic compounds / Dialkylamines / Organopnictogen compounds / Organofluorides
show 1 more
Substituents
1-benzopyran / Alkyl aryl ether / Aralkylamine / Aryl fluoride / Aryl halide / Benzenoid / 1,2-aminoalcohol / Secondary alcohol / Oxacycle / Secondary amine
show 13 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organofluorine compound, secondary alcohol, secondary amino compound, diol, chromanes (CHEBI:64019)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Receptor signaling protein activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...
Gene Name
ADRB1
Uniprot ID
P08588
Uniprot Name
Beta-1 adrenergic receptor
Molecular Weight
51322.1 Da
References
  1. Gielen W, Cleophas TJ, Agrawal R: Nebivolol: a review of its clinical and pharmacological characteristics. Int J Clin Pharmacol Ther. 2006 Aug;44(8):344-57. [PubMed:16961165]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  3. de Boer RA, Voors AA, van Veldhuisen DJ: Nebivolol: third-generation beta-blockade. Expert Opin Pharmacother. 2007 Jul;8(10):1539-50. [PubMed:17661735]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein homodimerization activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately ...
Gene Name
ADRB2
Uniprot ID
P07550
Uniprot Name
Beta-2 adrenergic receptor
Molecular Weight
46458.32 Da
References
  1. Nuttall SL, Routledge HC, Kendall MJ: A comparison of the beta1-selectivity of three beta1-selective beta-blockers. J Clin Pharm Ther. 2003 Jun;28(3):179-86. [PubMed:12795776]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 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
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. Kiser JJ, Burton JR, Anderson PL, Everson GT: Review and management of drug interactions with boceprevir and telaprevir. Hepatology. 2012 May;55(5):1620-8. doi: 10.1002/hep.25653. [PubMed:22331658]
  2. Hocht C, Bertera FM, Mayer MA, Taira CA: Issues in drug metabolism of major antihypertensive drugs: beta-blockers, calcium channel antagonists and angiotensin receptor blockers. Expert Opin Drug Metab Toxicol. 2010 Feb;6(2):199-211. doi: 10.1517/17425250903397381. [PubMed:20095790]

Drug created on October 19, 2007 15:00 / Updated on December 14, 2018 17:10