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Identification
NameLevomilnacipran
Accession NumberDB08918
TypeSmall Molecule
GroupsApproved
Description

Levomilnacipran is a selective serotonin and norepinephrine reuptake inhibitor. Chemically, levomilnacipran is the 1S,2R-enantiomer of milnacipran. FDA approved on July 25, 2013.

Structure
Thumb
Synonyms
(1S,2R)-milnacipran
External Identifiers
  • F 2695
  • F-2695
  • F2695
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Fetzimacapsule (extended release)40 mgoralActavis Specialty Pharmaceuticals Co2015-11-19Not applicableCanada
FetzimakitoralForest Laboratories, Inc.2013-07-25Not applicableUs
Fetzimacapsule (extended release)20 mgoralActavis Specialty Pharmaceuticals Co2015-11-19Not applicableCanada
Fetzimacapsule (extended release)120 mgoralActavis Specialty Pharmaceuticals CoNot applicableNot applicableCanada
Fetzimacapsule (extended release)80 mgoralActavis Specialty Pharmaceuticals CoNot applicableNot applicableCanada
Fetzimacapsule, extended release80 mg/1oralForest Laboratories, Inc.2013-07-25Not applicableUs
Fetzimacapsule, extended release40 mg/1oralForest Laboratories, Inc.2013-07-25Not applicableUs
Fetzimacapsule, extended release20 mg/1oralForest Laboratories, Inc.2013-07-25Not applicableUs
Fetzimacapsule, extended release40 mg/1oralAvera Mc Kennan Hospital2015-03-09Not applicableUs
Fetzimacapsule, extended release120 mg/1oralForest Laboratories, Inc.2013-07-25Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Levomilnacipran hydrochloride
175131-60-9
Thumb
  • InChI Key: XNCDYJFPRPDERF-NQQJLSKUSA-N
  • Monoisotopic Mass: 282.149891075
  • Average Mass: 282.809
DBSALT000107
Categories
UNIIUGM0326TXX
CAS number96847-54-0
WeightAverage: 246.348
Monoisotopic: 246.173213336
Chemical FormulaC15H22N2O
InChI KeyGJJFMKBJSRMPLA-DZGCQCFKSA-N
InChI
InChI=1S/C15H22N2O/c1-3-17(4-2)14(18)15(10-13(15)11-16)12-8-6-5-7-9-12/h5-9,13H,3-4,10-11,16H2,1-2H3/t13-,15+/m0/s1
IUPAC Name
(1S,2R)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropane-1-carboxamide
SMILES
CCN(CC)C(=O)[C@]1(C[[email protected]]1CN)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylacetamides. These are amide derivatives of phenylacetic acids.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylacetamides
Direct ParentPhenylacetamides
Alternative Parents
Substituents
  • Phenylacetamide
  • Aralkylamine
  • Cyclopropanecarboxylic acid or derivatives
  • Tertiary carboxylic acid amide
  • Tertiary amine
  • Carboxamide group
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationLevomilnacipran is a serotonin and norepinephrine reuptake inhibitor and is indicated for the treatment of major depressive disorder (MDD).
PharmacodynamicsLevomilnacipran binds with high affinity to human serotonin (5-HT) and norepinephrine (NE) transporters (Ki = 11 and 91 nM, respectively). It potently inhibits 5-HT and NE reuptake (IC50 = 16 - 19 and 11 nM, respectively). Levomilnacipran does not bind to any other receptors, ion channels, or transporters, including serotonergic (5HT1-7), α- and β adrenergic, muscarinic, or histaminergic receptors and Ca2+, Na+, K+ or Cl- channels to a significant degree. Levomilnacipran did not inhibit monoamine oxidase (MAO). Furthermore, levomilnacipran does not prolong the QTc interval to a clinically relevant extent.
Mechanism of actionThe exact mechanism of the antidepressant action of levomilnacipran is unknown but is thought to be related to the potentiation of serotonin and norephinephrine in the central nervous system through inhibition of reuptake at serotonin and norepinephrine transporters.
Related Articles
AbsorptionThe relative bioavailability after administration of the extended-release capsule was 92% when compared to oral solution. Food does not affect the concentration of levomilnacipran. After daily dosing of levomilnacipran (extended-release capsule) the mean Cmax is 341 ng/mL, and the mean steady-state AUC value is 5196 ng·h/mL. The Tmax is 6 - 8 hours after oral administration. Interconversion of stereoisomers does not occur in humans.
Volume of distribution
  • 387 – 473 L [apparent volume of distribution]
Protein binding22% bound to human plasma protein over concentration range of 10 to 1000 ng/mL.
Metabolism

Hepatic. Levomilnacipran undergoes desethylation to form desethyl levomilnacipran and hydroxylation to form p-hydroxy-levomilnacipran. Desethylation is facilitated primarily by CYP3A4 and by CYP2C8, 2C19, 2D6, and 2J2 to a lesser extent. Both metabolites undergo further conjugation with glucuronide to form conjugates.

Route of eliminationLevomilnacipran and its metabolites are eliminated primarily by renal excretion. 58% of the dose is excreted in urine as unchanged levomilnacipran. N-desethyl levomilnacipran is the major metabolite excreted in the urine and accounted for approximately 18% of the dose. Other identifiable metabolites excreted in the urine are levomilnacipran glucuronide (4%), desethyl-levomilnacipran glucuronide (3%), p-hydroxy levomilnacipran glucuronide (1%), and p-hydroxylevomilnacipran (1%). The metabolites are inactive.
Half life12 hours
Clearance
  • 21 – 29 L/h [mean apparent total clearance]
ToxicityThe most common adverse reactions are nausea, constipation, hyperhidrosis, heart rate increase, erectile dysfunction, tachycardia, vomiting, and palpitations.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9889
Caco-2 permeable+0.5914
P-glycoprotein substrateSubstrate0.5928
P-glycoprotein inhibitor INon-inhibitor0.902
P-glycoprotein inhibitor IINon-inhibitor0.8787
Renal organic cation transporterNon-inhibitor0.8119
CYP450 2C9 substrateNon-substrate0.8494
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6514
CYP450 1A2 substrateNon-inhibitor0.6383
CYP450 2C9 inhibitorNon-inhibitor0.7697
CYP450 2D6 inhibitorNon-inhibitor0.7718
CYP450 2C19 inhibitorNon-inhibitor0.8587
CYP450 3A4 inhibitorNon-inhibitor0.6327
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7004
Ames testNon AMES toxic0.8013
CarcinogenicityNon-carcinogens0.5456
BiodegradationNot ready biodegradable0.9972
Rat acute toxicity2.6162 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.993
hERG inhibition (predictor II)Non-inhibitor0.6823
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Capsule (extended release)oral120 mg
Capsule (extended release)oral20 mg
Capsule (extended release)oral40 mg
Capsule (extended release)oral80 mg
Capsule, extended releaseoral120 mg/1
Capsule, extended releaseoral20 mg/1
Capsule, extended releaseoral40 mg/1
Capsule, extended releaseoral80 mg/1
Kitoral
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8481598 No2011-03-022031-03-02Us
US8865937 No2012-05-232032-05-23Us
USRE43879 No2003-06-032023-06-03Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
logP1.42ChemAxon
pKa (Strongest Basic)9.83ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area46.33 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity73.81 m3·mol-1ChemAxon
Polarizability28.33 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS Codes
  • 28:16.04.16
PDB EntriesNot Available
FDA labelDownload (530 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabLevomilnacipran may increase the anticoagulant activities of Abciximab.
AcenocoumarolThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Acenocoumarol.
AcepromazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Acetophenazine.
Acetylsalicylic acidLevomilnacipran may increase the antiplatelet activities of Acetylsalicylic acid.
AlteplaseLevomilnacipran may increase the anticoagulant activities of Alteplase.
AmisulprideThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Amisulpride.
AnistreplaseLevomilnacipran may increase the anticoagulant activities of Anistreplase.
ApixabanThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Apixaban.
AprepitantThe serum concentration of Levomilnacipran can be increased when it is combined with Aprepitant.
AripiprazoleThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Aripiprazole.
AtazanavirThe serum concentration of Levomilnacipran can be increased when it is combined with Atazanavir.
BenzquinamideThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Benzquinamide.
BoceprevirThe serum concentration of Levomilnacipran can be increased when it is combined with Boceprevir.
CarphenazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Carphenazine.
CeritinibThe serum concentration of Levomilnacipran can be increased when it is combined with Ceritinib.
ChlormezanoneThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Chlorprothixene.
Citric AcidLevomilnacipran may increase the anticoagulant activities of Citric Acid.
ClarithromycinThe serum concentration of Levomilnacipran can be increased when it is combined with Clarithromycin.
ClozapineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Clozapine.
CobicistatThe serum concentration of Levomilnacipran can be increased when it is combined with Cobicistat.
CollagenaseThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Collagenase.
ConivaptanThe serum concentration of Levomilnacipran can be increased when it is combined with Conivaptan.
Dabigatran etexilateLevomilnacipran may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinLevomilnacipran may increase the anticoagulant activities of Dalteparin.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Levomilnacipran.
DarunavirThe serum concentration of Levomilnacipran can be increased when it is combined with Darunavir.
DasatinibDasatinib may increase the anticoagulant activities of Levomilnacipran.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Deoxycholic Acid.
DesmopressinLevomilnacipran may increase the antiplatelet activities of Desmopressin.
DicoumarolThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Dicoumarol.
DipivefrinLevomilnacipran may decrease the antihypertensive activities of Dipivefrin.
DroperidolThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Droperidol.
Edetic AcidLevomilnacipran may increase the anticoagulant activities of Edetic Acid.
EnoxaparinLevomilnacipran may increase the anticoagulant activities of Enoxaparin.
EthanolEthanol can cause an increase in the absorption of Levomilnacipran resulting in an increased serum concentration and potentially a worsening of adverse effects.
Ethyl biscoumacetateLevomilnacipran may increase the anticoagulant activities of Ethyl biscoumacetate.
FencamfamineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Fencamfamine.
FluconazoleThe metabolism of Levomilnacipran can be decreased when combined with Fluconazole.
FlupentixolThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Levomilnacipran.
Fondaparinux sodiumLevomilnacipran may increase the anticoagulant activities of Fondaparinux sodium.
FosaprepitantThe serum concentration of Levomilnacipran can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Levomilnacipran can be increased when it is combined with Fusidic Acid.
GlucosamineGlucosamine may increase the antiplatelet activities of Levomilnacipran.
GranisetronGranisetron may increase the serotonergic activities of Levomilnacipran.
HaloperidolThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Haloperidol.
HeparinLevomilnacipran may increase the anticoagulant activities of Heparin.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Levomilnacipran.
IdelalisibThe serum concentration of Levomilnacipran can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Levomilnacipran can be increased when it is combined with Indinavir.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Levomilnacipran.
Ioflupane I 123Levomilnacipran may decrease effectiveness of Ioflupane I 123 as a diagnostic agent.
ItraconazoleThe serum concentration of Levomilnacipran can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Levomilnacipran can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Levomilnacipran can be increased when it is combined with Ketoconazole.
LimaprostLimaprost may increase the antiplatelet activities of Levomilnacipran.
LinezolidLinezolid may increase the serotonergic activities of Levomilnacipran.
LoxapineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Loxapine.
LuliconazoleThe serum concentration of Levomilnacipran can be increased when it is combined with Luliconazole.
MesoridazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Methotrimeprazine.
Methylene blueLevomilnacipran may increase the serotonergic activities of Methylene blue.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Levomilnacipran.
MifepristoneThe serum concentration of Levomilnacipran can be increased when it is combined with Mifepristone.
MolindoneThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Molindone.
NefazodoneThe serum concentration of Levomilnacipran can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Levomilnacipran can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Levomilnacipran can be increased when it is combined with Netupitant.
ObinutuzumabThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Obinutuzumab.
OlanzapineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Olanzapine.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Levomilnacipran.
OndansetronThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Ondansetron.
PalbociclibThe serum concentration of Levomilnacipran can be increased when it is combined with Palbociclib.
PaliperidoneThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Paliperidone.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Levomilnacipran.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Levomilnacipran.
PerphenazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Perphenazine.
PhenelzinePhenelzine may increase the serotonergic activities of Levomilnacipran.
PhenindioneLevomilnacipran may increase the anticoagulant activities of Phenindione.
PhenprocoumonLevomilnacipran may increase the anticoagulant activities of Phenprocoumon.
PimozideThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Piperacetazine.
PosaconazoleThe serum concentration of Levomilnacipran can be increased when it is combined with Posaconazole.
ProchlorperazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Quetiapine.
RemoxiprideThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Reserpine.
ReteplaseLevomilnacipran may increase the anticoagulant activities of Reteplase.
RidogrelLevomilnacipran may increase the anticoagulant activities of Ridogrel.
RisperidoneThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Risperidone.
RitonavirThe serum concentration of Levomilnacipran can be increased when it is combined with Ritonavir.
RivaroxabanLevomilnacipran may increase the anticoagulant activities of Rivaroxaban.
SaquinavirThe serum concentration of Levomilnacipran can be increased when it is combined with Saquinavir.
SertindoleThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Sertindole.
SimeprevirThe serum concentration of Levomilnacipran can be increased when it is combined with Simeprevir.
StiripentolThe serum concentration of Levomilnacipran can be increased when it is combined with Stiripentol.
StreptokinaseLevomilnacipran may increase the anticoagulant activities of Streptokinase.
SulodexideLevomilnacipran may increase the anticoagulant activities of Sulodexide.
SulpirideThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Sulpiride.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Levomilnacipran.
TelaprevirThe serum concentration of Levomilnacipran can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Levomilnacipran can be increased when it is combined with Telithromycin.
TenecteplaseLevomilnacipran may increase the anticoagulant activities of Tenecteplase.
ThioridazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Thiothixene.
TipranavirTipranavir may increase the antiplatelet activities of Levomilnacipran.
TositumomabThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Tositumomab.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Levomilnacipran.
TranylcypromineTranylcypromine may increase the serotonergic activities of Levomilnacipran.
TreprostinilLevomilnacipran may increase the anticoagulant activities of Treprostinil.
TrifluoperazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Triflupromazine.
UrokinaseLevomilnacipran may increase the anticoagulant activities of Urokinase.
Vitamin EVitamin E may increase the antiplatelet activities of Levomilnacipran.
VoriconazoleThe serum concentration of Levomilnacipran can be increased when it is combined with Voriconazole.
WarfarinThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Warfarin.
ZiprasidoneThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Ziprasidone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Zuclopenthixol.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 Da

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
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
This enzyme metabolizes arachidonic acid predominantly via a NADPH-dependent olefin epoxidation to all four regioisomeric cis-epoxyeicosatrienoic acids. One of the predominant enzymes responsible for the epoxidation of endogenous cardiac arachidonic acid pools.
Gene Name:
CYP2J2
Uniprot ID:
P51589
Molecular Weight:
57610.165 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
Comments
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Drug created on August 01, 2013 14:17 / Updated on June 29, 2016 01:52