Identification

Name
Levosalbutamol
Accession Number
DB13139  (DB05761)
Type
Small Molecule
Groups
Approved
Description

Levosalbutamol, also known as levalbuterol, is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). Salbutamol has been marketed as a racemic mixture, although beta2-agonist activity resides almost exclusively in the (R)-enantiomer. The enantioselective disposition of salbutamol and the possibility that (S)-salbutamol has adverse effects have led to the development of an enantiomerically pure (R)-salbutamol formulation known as levosalbutamol (levalbuterol).

Structure
Thumb
Synonyms
  • (-)-Albuterol
  • (-)-Salbutamol
  • (R)-salbutamol
  • Levalbuterol
  • R-salbutamol
External IDs
ASF-1096
Product Ingredients
IngredientUNIICASInChI Key
Levalbuterol hydrochlorideWDQ1526QJM50293-90-8OWNWYCOLFIFTLK-YDALLXLXSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
XopenexSolution1.25 mg/3mLRespiratory (inhalation)Remedy Repack2013-06-132017-11-04Us
XopenexSolution.63 mg/3mLRespiratory (inhalation)Akorn2015-02-27Not applicableUs
XopenexSolution, concentrate1.25 mg/.5mLRespiratory (inhalation)Akorn2015-02-26Not applicableUs
XopenexSolution1.25 mg/3mLRespiratory (inhalation)Akorn2015-02-27Not applicableUs
XopenexSolution.31 mg/3mLRespiratory (inhalation)Akorn2015-02-27Not applicableUs
XopenexSolution1.25 mg/3mLRespiratory (inhalation)Rebel Distributors1999-04-01Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LevalbuterolSolution, concentrate1.25 mg/.5mLRespiratory (inhalation)Mylan Pharmaceuticals2009-08-28Not applicableUs
LevalbuterolSolution.63 mg/3mLRespiratory (inhalation)A S Medication Solutions2013-04-292017-06-20Us
LevalbuterolSolution.31 mg/3mLRespiratory (inhalation)Mylan Pharmaceuticals2013-03-15Not applicableUs
LevalbuterolSolution.31 mg/3mLRespiratory (inhalation)Teva2013-04-29Not applicableUs
LevalbuterolSolution1.25 mg/3mLRespiratory (inhalation)Aurobindo Pharma2016-12-30Not applicableUs
LevalbuterolSolution1.25 mg/3mLRespiratory (inhalation)Teva2013-04-29Not applicableUs
LevalbuterolSolution.63 mg/3mLRespiratory (inhalation)The Ritedose Corporation2016-03-14Not applicableUs
LevalbuterolSolution.63 mg/3mLRespiratory (inhalation)Teva2013-04-29Not applicableUs
LevalbuterolSolution.31 mg/3mLRespiratory (inhalation)Aurobindo Pharma2016-12-30Not applicableUs
LevalbuterolSolution.63 mg/3mLRespiratory (inhalation)Mylan Pharmaceuticals2013-03-15Not applicableUs
Categories
UNII
EDN2NBH5SS
CAS number
34391-04-3
Weight
Average: 239.3107
Monoisotopic: 239.152143543
Chemical Formula
C13H21NO3
InChI Key
NDAUXUAQIAJITI-LBPRGKRZSA-N
InChI
InChI=1S/C13H21NO3/c1-13(2,3)14-7-12(17)9-4-5-11(16)10(6-9)8-15/h4-6,12,14-17H,7-8H2,1-3H3/t12-/m0/s1
IUPAC Name
4-[(1R)-2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
SMILES
CC(C)(C)NC[[email protected]](O)C1=CC(CO)=C(O)C=C1

Pharmacology

Indication

Levosalbutamol's bronchodilator properties give it indications in treatment of COPD (chronic obstructive pulmonary disease, also known as chronic obstructive lung disease) and asthma.

Structured Indications
Pharmacodynamics

Like other bronchodilators, it acts by relaxing smooth muscle in the bronchial tubes, and thus shortening or reversing an acute "attack" of shortness of breath or difficulty breathing.

Mechanism of action

Activation of β2 adrenergic receptors on airway smooth muscle leads to the activation of adenylate cyclase and to an increase in the intracellular concentration of 3',5'-cyclic adenosine monophosphate (cyclic AMP). The increase in cyclic AMP is associated with the activation of protein kinase A, which in turn, inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in muscle relaxation.

Levosalbutamol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. Increased cyclic AMP concentrations are also associated with the inhibition of the release of mediators from mast cells in the airways. Levosalbutamol acts as a functional agonist that relaxes the airway irrespective of the spasmogen involved, thereby protecting against all bronchoconstrictor challenges.

TargetActionsOrganism
ABeta-2 adrenergic receptor
agonist
Human
Absorption

Inhalation delivers the medication directly into the airways and lungs, thereby minimizing side effects because of reduced systemic absorption of the inhaled medications.

Volume of distribution
Not Available
Protein binding

plasma protein binding is relatively low.

Metabolism

Pure (R)-salbutamol formulation known as levosalbutamol is metabolised up to 12 times faster than (S)-salbutamol by intestine.

Route of elimination

excreted into the urine.

Half life

3.3 - 4 hours

Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Levosalbutamol.Experimental
AcebutololAcebutolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
AlprenololAlprenolol may decrease the bronchodilatory activities of Levosalbutamol.Approved, Withdrawn
AmineptineThe risk or severity of adverse effects can be increased when Amineptine is combined with Levosalbutamol.Illicit, Withdrawn
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levosalbutamol.Approved
AtenololAtenolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
AtomoxetineAtomoxetine may increase the tachycardic activities of Levosalbutamol.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Levosalbutamol is combined with Atorvastatin.Approved
AtosibanThe risk or severity of adverse effects can be increased when Levosalbutamol is combined with Atosiban.Approved, Investigational
BendroflumethiazideLevosalbutamol may increase the hypokalemic activities of Bendroflumethiazide.Approved
BenmoxinThe risk or severity of adverse effects can be increased when Benmoxin is combined with Levosalbutamol.Withdrawn
BetahistineThe therapeutic efficacy of Levosalbutamol can be decreased when used in combination with Betahistine.Approved
BetaxololBetaxolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
BisoprololBisoprolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
BopindololBopindolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
BrofaromineThe risk or severity of adverse effects can be increased when Brofaromine is combined with Levosalbutamol.Experimental
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Levosalbutamol.Approved, Investigational
BumetanideLevosalbutamol may increase the hypokalemic activities of Bumetanide.Approved
BupranololBupranolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Levosalbutamol.Approved
CaroxazoneThe risk or severity of adverse effects can be increased when Caroxazone is combined with Levosalbutamol.Withdrawn
CarteololCarteolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
CeliprololCeliprolol may decrease the bronchodilatory activities of Levosalbutamol.Approved, Investigational
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Levosalbutamol.Withdrawn
ChlorothiazideLevosalbutamol may increase the hypokalemic activities of Chlorothiazide.Approved, Vet Approved
ChlorthalidoneLevosalbutamol may increase the hypokalemic activities of Chlorthalidone.Approved
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Levosalbutamol.Approved, Vet Approved
CloranololCloranolol may decrease the bronchodilatory activities of Levosalbutamol.Experimental
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Levosalbutamol.Approved
CyclopenthiazideLevosalbutamol may increase the hypokalemic activities of Cyclopenthiazide.Experimental
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Levosalbutamol.Approved
DibenzepinThe risk or severity of adverse effects can be increased when Dibenzepin is combined with Levosalbutamol.Experimental
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Levosalbutamol.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Levosalbutamol.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Levosalbutamol.Experimental
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Levosalbutamol.Approved
DosulepinThe risk or severity of adverse effects can be increased when Dosulepin is combined with Levosalbutamol.Approved
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Levosalbutamol.Approved
EltrombopagThe serum concentration of Levosalbutamol can be increased when it is combined with Eltrombopag.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Levosalbutamol.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Levosalbutamol.Approved
EsmirtazapineThe risk or severity of adverse effects can be increased when Esmirtazapine is combined with Levosalbutamol.Investigational
EsmololEsmolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
Etacrynic acidLevosalbutamol may increase the hypokalemic activities of Etacrynic acid.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Levosalbutamol.Approved
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Levosalbutamol.Approved
FurazolidoneThe risk or severity of adverse effects can be increased when Furazolidone is combined with Levosalbutamol.Approved, Investigational, Vet Approved
FurosemideLevosalbutamol may increase the hypokalemic activities of Furosemide.Approved, Vet Approved
HarmalineThe risk or severity of adverse effects can be increased when Harmaline is combined with Levosalbutamol.Experimental
HydracarbazineThe risk or severity of adverse effects can be increased when Hydracarbazine is combined with Levosalbutamol.Experimental
HydrochlorothiazideLevosalbutamol may increase the hypokalemic activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideLevosalbutamol may increase the hypokalemic activities of Hydroflumethiazide.Approved, Investigational
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Levosalbutamol.Approved
IndapamideLevosalbutamol may increase the hypokalemic activities of Indapamide.Approved
IprindoleThe risk or severity of adverse effects can be increased when Iprindole is combined with Levosalbutamol.Experimental
IproclozideThe risk or severity of adverse effects can be increased when Iproclozide is combined with Levosalbutamol.Withdrawn
IproniazidThe risk or severity of adverse effects can be increased when Iproniazid is combined with Levosalbutamol.Withdrawn
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Levosalbutamol.Approved
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Levosalbutamol.Approved, Investigational
LofepramineThe risk or severity of adverse effects can be increased when Lofepramine is combined with Levosalbutamol.Experimental
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Levosalbutamol.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Levosalbutamol is combined with Loxapine.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Levosalbutamol.Illicit, Investigational, Withdrawn
MebanazineThe risk or severity of adverse effects can be increased when Mebanazine is combined with Levosalbutamol.Withdrawn
MepindololMepindolol may decrease the bronchodilatory activities of Levosalbutamol.Experimental
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Levosalbutamol.Experimental
MethyclothiazideLevosalbutamol may increase the hypokalemic activities of Methyclothiazide.Approved
Methylene blueThe risk or severity of adverse effects can be increased when Methylene blue is combined with Levosalbutamol.Approved, Investigational
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Levosalbutamol.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Levosalbutamol.Approved
MetolazoneLevosalbutamol may increase the hypokalemic activities of Metolazone.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Levosalbutamol.Approved, Investigational
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Levosalbutamol.Experimental
MinaprineThe risk or severity of adverse effects can be increased when Minaprine is combined with Levosalbutamol.Approved
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Levosalbutamol.Approved
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Levosalbutamol.Approved
NebivololNebivolol may decrease the bronchodilatory activities of Levosalbutamol.Approved, Investigational
NialamideThe risk or severity of adverse effects can be increased when Nialamide is combined with Levosalbutamol.Withdrawn
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Levosalbutamol.Approved, Investigational
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Levosalbutamol.Approved
OctamoxinThe risk or severity of adverse effects can be increased when Octamoxin is combined with Levosalbutamol.Withdrawn
OpipramolThe risk or severity of adverse effects can be increased when Opipramol is combined with Levosalbutamol.Investigational
OxprenololOxprenolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
PargylineThe risk or severity of adverse effects can be increased when Pargyline is combined with Levosalbutamol.Approved
PenbutololPenbutolol may decrease the bronchodilatory activities of Levosalbutamol.Approved, Investigational
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Levosalbutamol.Approved, Investigational, Vet Approved, Withdrawn
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Levosalbutamol.Approved
PheniprazineThe risk or severity of adverse effects can be increased when Pheniprazine is combined with Levosalbutamol.Withdrawn
PhenoxypropazineThe risk or severity of adverse effects can be increased when Phenoxypropazine is combined with Levosalbutamol.Withdrawn
PiretanideLevosalbutamol may increase the hypokalemic activities of Piretanide.Experimental
PirlindoleThe risk or severity of adverse effects can be increased when Pirlindole is combined with Levosalbutamol.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Levosalbutamol.Approved
PivhydrazineThe risk or severity of adverse effects can be increased when Pivhydrazine is combined with Levosalbutamol.Withdrawn
PolythiazideLevosalbutamol may increase the hypokalemic activities of Polythiazide.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Levosalbutamol.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Levosalbutamol.Approved
QuinethazoneLevosalbutamol may increase the hypokalemic activities of Quinethazone.Approved
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Levosalbutamol.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Levosalbutamol.Approved
SafrazineThe risk or severity of adverse effects can be increased when Safrazine is combined with Levosalbutamol.Withdrawn
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Levosalbutamol.Approved, Investigational, Vet Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Levosalbutamol.Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Levosalbutamol.Experimental
TeriflunomideThe serum concentration of Levosalbutamol can be increased when it is combined with Teriflunomide.Approved
TertatololTertatolol may decrease the bronchodilatory activities of Levosalbutamol.Experimental
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Levosalbutamol.Approved, Withdrawn
TianeptineThe risk or severity of adverse effects can be increased when Tianeptine is combined with Levosalbutamol.Approved, Investigational
TimololTimolol may decrease the bronchodilatory activities of Levosalbutamol.Approved
ToloxatoneThe risk or severity of adverse effects can be increased when Toloxatone is combined with Levosalbutamol.Approved
TorasemideLevosalbutamol may increase the hypokalemic activities of Torasemide.Approved
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Levosalbutamol.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Levosalbutamol.Approved
TrichlormethiazideLevosalbutamol may increase the hypokalemic activities of Trichlormethiazide.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Levosalbutamol.Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Levosalbutamol.Approved, Experimental
Food Interactions
Not Available

References

General References
  1. Boulton DW, Fawcett JP: The pharmacokinetics of levosalbutamol: what are the clinical implications? Clin Pharmacokinet. 2001 Jan;40(1):23-40. [PubMed:11236808]
  2. Wikipedia [Link]
  3. Sciencedirect [Link]
External Links
KEGG Drug
D08124
KEGG Compound
C11770
PubChem Compound
123600
PubChem Substance
347829257
ChemSpider
110192
BindingDB
50361247
ChEBI
8746
ChEMBL
CHEMBL1002
HET
68H
Wikipedia
Levalbuterol
PDB Entries
2y04

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentAsthma Bronchial3
3CompletedTreatmentAsthma Bronchial3
3CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
4CompletedHealth Services ResearchAsthma Bronchial / Chronic Obstructive Pulmonary Disease (COPD)1
4CompletedSupportive CareChronic Obstructive Pulmonary Disease (COPD) / Sepsis / Shock1
4CompletedTreatmentAsthma Bronchial4
4TerminatedTreatmentAcute Asthma1
4WithdrawnTreatmentAsthma Bronchial1
Not AvailableCompletedHealth Services ResearchChronic Obstructive Pulmonary Disease (COPD)1
Not AvailableEnrolling by InvitationBasic ScienceOxygen Consumption1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
SolutionRespiratory (inhalation).31 mg/3mL
SolutionRespiratory (inhalation).63 mg/3mL
Solution, concentrateRespiratory (inhalation)1.25 mg/.5mL
SolutionRespiratory (inhalation)1.25 mg/3mL
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.15 mg/mLALOGPS
logP0.44ALOGPS
logP0.34ChemAxon
logS-2ALOGPS
pKa (Strongest Acidic)10.12ChemAxon
pKa (Strongest Basic)9.4ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area72.72 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity67.87 m3·mol-1ChemAxon
Polarizability26.87 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
MS/MS Spectrum - Quattro_QQQ 10V, N/ALC-MS/MSsplash10-052r-4960000000-11e534d73f624db9d896
MS/MS Spectrum - Quattro_QQQ 25V, N/ALC-MS/MSsplash10-0002-0900000000-1320ba6a3f38ebdb80a3
MS/MS Spectrum - Quattro_QQQ 40V, N/ALC-MS/MSsplash10-002f-8900000000-4735e41255f39d1d99d4
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
1H NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzyl alcohols. These are organic compounds containing the phenylmethanol substructure.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzyl alcohols
Direct Parent
Benzyl alcohols
Alternative Parents
Aralkylamines / 1-hydroxy-2-unsubstituted benzenoids / Secondary alcohols / 1,2-aminoalcohols / Dialkylamines / Primary alcohols / Organopnictogen compounds / Hydrocarbon derivatives / Aromatic alcohols
Substituents
Benzyl alcohol / Phenol / Aralkylamine / 1-hydroxy-2-unsubstituted benzenoid / Secondary alcohol / 1,2-aminoalcohol / Secondary amine / Secondary aliphatic amine / Hydrocarbon derivative / Alcohol
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
albuterol (CHEBI:8746)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
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. UniProt [Link]
  2. KEGG [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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. UniProt [Link]
  2. ChEMBL [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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. ChEMBL [Link]
  2. KEGG [Link]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. UniProt [Link]
  2. ChEMBL [Link]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Substrate
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), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. ChEMBL [Link]
  2. UniProt [Link]

Drug created on October 27, 2016 11:42 / Updated on November 09, 2017 05:19