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Identification
NameLumiracoxib
Accession NumberDB01283
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionLumiracoxib is a COX-2 selective inhibitor non-steroidal anti-inflammatory drug. On August 11, 2007, Australia's Therapeutic Goods Administration (TGA, the Australian equivalent of the FDA) cancelled the registration of lumiracoxib in Australia due to concerns that it may cause liver failure. New Zealand and Canada have also followed suit in recalling the drug.
Structure
Thumb
Synonyms
2-((2-chloro-6-Fluorophenyl)amino)-5-methylbenzeneacetic acid
COX 189
COX-189
COX189
Lumiracoxibum
Prexige
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PrexigeNovartis
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIV91T9204HU
CAS number220991-20-8
WeightAverage: 293.721
Monoisotopic: 293.061884577
Chemical FormulaC15H13ClFNO2
InChI KeyInChIKey=KHPKQFYUPIUARC-UHFFFAOYSA-N
InChI
InChI=1S/C15H13ClFNO2/c1-9-5-6-13(10(7-9)8-14(19)20)18-15-11(16)3-2-4-12(15)17/h2-7,18H,8H2,1H3,(H,19,20)
IUPAC Name
2-{2-[(2-chloro-6-fluorophenyl)amino]-5-methylphenyl}acetic acid
SMILES
CC1=CC=C(NC2=C(Cl)C=CC=C2F)C(CC(O)=O)=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylacetic acid derivatives. These are compounds containing a phenylacetic acid moiety, which consists of a phenyl group substituted at the second position by an acetic acid.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylacetic acid derivatives
Direct ParentPhenylacetic acid derivatives
Alternative Parents
Substituents
  • Phenylacetate
  • Aminotoluene
  • Substituted aniline
  • Toluene
  • Halobenzene
  • Fluorobenzene
  • Chlorobenzene
  • Aniline
  • Aryl halide
  • Aryl fluoride
  • Aryl chloride
  • Secondary amine
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the acute and chronic treatment of the signs and symptoms of osteoarthritis of the knee in adults.
PharmacodynamicsLumiracoxib has a different structure from the standard COX-2 inhibitors (e.g. celecoxib). It more closely resembles the structure of diclofenac (one chlorine substituted by fluorine, the phenylacetic acid has another methyl group in meta position), making it a member of the arylalkanoic acid family of NSAIDs. It binds to a different site on the COX-2 receptor than the standard COX-2 inhibitors. It displays extremely high COX-2 selectivity.
Mechanism of actionThe mechanism of action of lumiracoxib is due to inhibition of prostaglandin synthesis via inhibition of cyclooygenase-2 (COX-2). Lumiracoxib does not inhibit COX-1 at therapeutic concentrations.
Related Articles
AbsorptionRapidly absorbed following oral administration, with an absolute oral bioavailablity of 74%.
Volume of distributionNot Available
Protein bindingHighly bound to plasma proteins (>= 98%).
Metabolism

Hepatic oxidation and hydroxylation via CYP2C9. Three major metabolites have been identified in plasma: 4'-hydroxy-lumiracoxib, 5-carboxy-lumiracoxib, and 4'-hydroxy-5-carboxy-lumiracoxib.

SubstrateEnzymesProduct
Lumiracoxib
Lumiracoxib metabolite M21Details
Lumiracoxib metabolite M21
Not Available
5-Carboxylumiracoxib (M11)Details
5-Carboxylumiracoxib (M11)
Not Available
Lumiracoxib metabolite M15Details
Lumiracoxib metabolite M15
Lumiracoxib metabolite M16/17Details
5-Carboxylumiracoxib (M11)
5-Carboxylumiracoxib glucuronide (M3)Details
Lumiracoxib
Lumiracoxib glucuronide (M24)Details
Lumiracoxib
4'-hydroxylumiracoxib (M23)Details
4'-hydroxylumiracoxib (M23)
4'-Carboxylumiracoxib glucuronide (M22)Details
4'-hydroxylumiracoxib (M23)
Not Available
Lumiracoxib metabolite M25Details
Lumiracoxib metabolite M25
Lumiracoxib metabolite M25 glucuronide (M20)Details
4'-hydroxylumiracoxib (M23)
Not Available
Lumiracoxib metabolite M9Details
Lumiracoxib metabolite M9
Not Available
4'-Hydroxy-5-carboxylumiracoxib (M5)Details
4'-Hydroxy-5-carboxylumiracoxib (M5)
Lumiracoxib metabolite M2Details
4'-Hydroxy-5-carboxylumiracoxib (M5)
Not Available
Lumiracoxib metabolite M8Details
Lumiracoxib metabolite M8
Not Available
Lumiracoxib metabolite M4/M6Details
Lumiracoxib metabolite M8
Lumiracoxib metabolite M10Details
Lumiracoxib metabolite M8
Not Available
Hydroxylumiracoxib metabolite M8 (M12)Details
Hydroxylumiracoxib metabolite M8 (M12)
Lumiracoxib metabolite M12 glucuronide (M13)Details
5-Carboxylumiracoxib (M11)
Not Available
4'-Hydroxy-5-carboxylumiracoxib (M5)Details
Lumiracoxib metabolite M21
Not Available
Lumiracoxib metabolite M9Details
Lumiracoxib metabolite M15
Not Available
Lumiracoxib metabolite M8Details
Route of eliminationNot Available
Half lifeTerminal half-life is approximately 4 hours.
ClearanceNot Available
ToxicitySingle oral doses in mice and rats resulted in mortality and/or moribundity at doses of 600 mg/kg and 500 mg/kg, respectively. Single intraperitoneal doses in mice and rats results in mortality/moribundity at 750 mg/kg and 1000 mg/kg, respectively. The maximum non-lethal single oral and intraperitoneal dose in mouse was 300 mg/kg and 250 mg/kg, respectively. In the rat it was 150 mg/kg and 250 mg/kg, respectively.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Lumiracoxib Action PathwayDrug actionSMP00699
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9825
Blood Brain Barrier+0.9715
Caco-2 permeable+0.818
P-glycoprotein substrateNon-substrate0.7336
P-glycoprotein inhibitor INon-inhibitor0.7134
P-glycoprotein inhibitor IINon-inhibitor0.9389
Renal organic cation transporterNon-inhibitor0.916
CYP450 2C9 substrateNon-substrate0.7247
CYP450 2D6 substrateNon-substrate0.8639
CYP450 3A4 substrateNon-substrate0.5964
CYP450 1A2 substrateInhibitor0.5208
CYP450 2C9 inhibitorInhibitor0.6844
CYP450 2D6 inhibitorNon-inhibitor0.8163
CYP450 2C19 inhibitorNon-inhibitor0.8576
CYP450 3A4 inhibitorNon-inhibitor0.8063
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6222
Ames testNon AMES toxic0.8453
CarcinogenicityNon-carcinogens0.6326
BiodegradationNot ready biodegradable0.9954
Rat acute toxicity3.5160 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9512
hERG inhibition (predictor II)Non-inhibitor0.7169
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP3.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00549 mg/mLALOGPS
logP4.56ALOGPS
logP4.31ChemAxon
logS-4.7ALOGPS
pKa (Strongest Acidic)4.11ChemAxon
pKa (Strongest Basic)-1.9ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area49.33 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity75.91 m3·mol-1ChemAxon
Polarizability28.53 Å3ChemAxon
Number of Rings2ChemAxon
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
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesM01AH06
AHFS Codes
  • 28:08.04.08
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabLumiracoxib may increase the anticoagulant activities of Abciximab.
AbirateroneThe serum concentration of Lumiracoxib can be increased when it is combined with Abiraterone.
AcebutololLumiracoxib may decrease the antihypertensive activities of Acebutolol.
AceclofenacThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Aceclofenac.
AcenocoumarolLumiracoxib may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Lumiracoxib.
AdapaleneThe risk or severity of adverse effects can be increased when Adapalene is combined with Lumiracoxib.
Alendronic acidThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Alendronic acid.
AliskirenLumiracoxib may decrease the antihypertensive activities of Aliskiren.
AlprenololLumiracoxib may decrease the antihypertensive activities of Alprenolol.
AlprostadilThe therapeutic efficacy of Alprostadil can be decreased when used in combination with Lumiracoxib.
AmikacinLumiracoxib may decrease the excretion rate of Amikacin which could result in a lower serum level and potentially a reduction in efficacy.
AmilorideLumiracoxib may decrease the antihypertensive activities of Amiloride.
AmiodaroneThe metabolism of Lumiracoxib can be decreased when combined with Amiodarone.
AncrodLumiracoxib may increase the anticoagulant activities of Ancrod.
AntipyrineThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Antipyrine.
Antithrombin III humanLumiracoxib may increase the anticoagulant activities of Antithrombin III human.
ApixabanLumiracoxib may increase the anticoagulant activities of Apixaban.
ApremilastThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Apremilast.
AprepitantThe metabolism of Lumiracoxib can be increased when combined with Aprepitant.
ArdeparinLumiracoxib may increase the anticoagulant activities of Ardeparin.
ArgatrobanLumiracoxib may increase the anticoagulant activities of Argatroban.
ArmodafinilThe metabolism of Lumiracoxib can be decreased when combined with Armodafinil.
ArotinololLumiracoxib may decrease the antihypertensive activities of Arotinolol.
AtenololLumiracoxib may decrease the antihypertensive activities of Atenolol.
AzapropazoneThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Azapropazone.
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Lumiracoxib.
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Lumiracoxib.
AzithromycinThe metabolism of Lumiracoxib can be decreased when combined with Azithromycin.
BalsalazideLumiracoxib may increase the nephrotoxic activities of Balsalazide.
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Lumiracoxib.
BecaplerminLumiracoxib may increase the anticoagulant activities of Becaplermin.
BefunololLumiracoxib may decrease the antihypertensive activities of Befunolol.
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Lumiracoxib.
BendroflumethiazideThe therapeutic efficacy of Bendroflumethiazide can be decreased when used in combination with Lumiracoxib.
BenoxaprofenThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Benoxaprofen.
BetaxololLumiracoxib may decrease the antihypertensive activities of Betaxolol.
BevantololLumiracoxib may decrease the antihypertensive activities of Bevantolol.
BimatoprostThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Lumiracoxib.
BisoprololLumiracoxib may decrease the antihypertensive activities of Bisoprolol.
BivalirudinLumiracoxib may increase the anticoagulant activities of Bivalirudin.
BopindololLumiracoxib may decrease the antihypertensive activities of Bopindolol.
BortezomibThe metabolism of Lumiracoxib can be decreased when combined with Bortezomib.
BromfenacThe risk or severity of adverse effects can be increased when Bromfenac is combined with Lumiracoxib.
BufuralolLumiracoxib may decrease the antihypertensive activities of Bufuralol.
BumetanideLumiracoxib may decrease the diuretic activities of Bumetanide.
BupranololLumiracoxib may decrease the antihypertensive activities of Bupranolol.
CaffeineThe metabolism of Lumiracoxib can be decreased when combined with Caffeine.
CandesartanThe risk or severity of adverse effects can be increased when Candesartan is combined with Lumiracoxib.
CandoxatrilThe risk or severity of adverse effects can be increased when Candoxatril is combined with Lumiracoxib.
CapecitabineThe metabolism of Lumiracoxib can be decreased when combined with Capecitabine.
CaptoprilThe risk or severity of adverse effects can be increased when Captopril is combined with Lumiracoxib.
CarbamazepineThe metabolism of Lumiracoxib can be increased when combined with Carbamazepine.
Carboprost TromethamineThe therapeutic efficacy of Carboprost Tromethamine can be decreased when used in combination with Lumiracoxib.
CarprofenThe risk or severity of adverse effects can be increased when Carprofen is combined with Lumiracoxib.
CarteololLumiracoxib may decrease the antihypertensive activities of Carteolol.
CarvedilolLumiracoxib may decrease the antihypertensive activities of Carvedilol.
CastanospermineThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Castanospermine.
CelecoxibThe risk or severity of adverse effects can be increased when Celecoxib is combined with Lumiracoxib.
CeliprololLumiracoxib may decrease the antihypertensive activities of Celiprolol.
CeritinibThe serum concentration of Lumiracoxib can be increased when it is combined with Ceritinib.
CertoparinLumiracoxib may increase the anticoagulant activities of Certoparin.
ChloramphenicolThe metabolism of Lumiracoxib can be decreased when combined with Chloramphenicol.
ChloroquineThe risk or severity of adverse effects can be increased when Chloroquine is combined with Lumiracoxib.
ChlorothiazideThe therapeutic efficacy of Chlorothiazide can be decreased when used in combination with Lumiracoxib.
ChlorthalidoneThe therapeutic efficacy of Chlorthalidone can be decreased when used in combination with Lumiracoxib.
CholecalciferolThe metabolism of Lumiracoxib can be decreased when combined with Cholecalciferol.
CholestyramineCholestyramine can cause a decrease in the absorption of Lumiracoxib resulting in a reduced serum concentration and potentially a decrease in efficacy.
CilazaprilThe risk or severity of adverse effects can be increased when Cilazapril is combined with Lumiracoxib.
CimetidineThe metabolism of Lumiracoxib can be decreased when combined with Cimetidine.
CitalopramThe metabolism of Lumiracoxib can be decreased when combined with Citalopram.
Citric AcidLumiracoxib may increase the anticoagulant activities of Citric Acid.
ClodronateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Clodronate.
ClonixinThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Clonixin.
CloprostenolThe therapeutic efficacy of Cloprostenol can be decreased when used in combination with Lumiracoxib.
ClotrimazoleThe metabolism of Lumiracoxib can be decreased when combined with Clotrimazole.
ColesevelamColesevelam can cause a decrease in the absorption of Lumiracoxib resulting in a reduced serum concentration and potentially a decrease in efficacy.
ColestipolColestipol can cause a decrease in the absorption of Lumiracoxib resulting in a reduced serum concentration and potentially a decrease in efficacy.
CyclosporineLumiracoxib may increase the nephrotoxic activities of Cyclosporine.
CyclosporineThe metabolism of Lumiracoxib can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Lumiracoxib can be decreased when it is combined with Cyproterone acetate.
D-LimoneneThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with D-Limonene.
Dabigatran etexilateLumiracoxib may increase the anticoagulant activities of Dabigatran etexilate.
DabrafenibThe serum concentration of Lumiracoxib can be decreased when it is combined with Dabrafenib.
DalteparinLumiracoxib may increase the anticoagulant activities of Dalteparin.
DanaparoidLumiracoxib may increase the anticoagulant activities of Danaparoid.
DaunorubicinLumiracoxib may decrease the excretion rate of Daunorubicin which could result in a lower serum level and potentially a reduction in efficacy.
DeferasiroxThe serum concentration of Lumiracoxib can be increased when it is combined with Deferasirox.
DeferasiroxThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Deferasirox.
DelavirdineThe metabolism of Lumiracoxib can be decreased when combined with Delavirdine.
DesirudinLumiracoxib may increase the anticoagulant activities of Desirudin.
DesmopressinThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Desmopressin.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Lumiracoxib.
DextranLumiracoxib may increase the anticoagulant activities of Dextran.
Dextran 40Lumiracoxib may increase the anticoagulant activities of Dextran 40.
Dextran 70Lumiracoxib may increase the anticoagulant activities of Dextran 70.
Dextran 75Lumiracoxib may increase the anticoagulant activities of Dextran 75.
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Lumiracoxib.
DicoumarolLumiracoxib may increase the anticoagulant activities of Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Lumiracoxib.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Lumiracoxib.
DihydrostreptomycinLumiracoxib may decrease the excretion rate of Dihydrostreptomycin which could result in a lower serum level and potentially a reduction in efficacy.
DinoprostoneThe therapeutic efficacy of Dinoprostone can be decreased when used in combination with Lumiracoxib.
DoxorubicinLumiracoxib may decrease the excretion rate of Doxorubicin which could result in a lower serum level and potentially a reduction in efficacy.
DrospirenoneLumiracoxib may increase the hyperkalemic activities of Drospirenone.
DroxicamThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Droxicam.
Edetic AcidLumiracoxib may increase the anticoagulant activities of Edetic Acid.
EdoxabanLumiracoxib may increase the anticoagulant activities of Edoxaban.
EfavirenzThe metabolism of Lumiracoxib can be decreased when combined with Efavirenz.
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Lumiracoxib.
EnalaprilatThe risk or severity of adverse effects can be increased when Enalaprilat is combined with Lumiracoxib.
EnoxaparinLumiracoxib may increase the anticoagulant activities of Enoxaparin.
EpirizoleThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Epirizole.
EpirubicinLumiracoxib may decrease the excretion rate of Epirubicin which could result in a lower serum level and potentially a reduction in efficacy.
EplerenoneLumiracoxib may decrease the antihypertensive activities of Eplerenone.
EpoprostenolThe therapeutic efficacy of Epoprostenol can be decreased when used in combination with Lumiracoxib.
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Lumiracoxib.
Eslicarbazepine acetateThe metabolism of Lumiracoxib can be decreased when combined with Eslicarbazepine acetate.
EsmololLumiracoxib may decrease the antihypertensive activities of Esmolol.
EsomeprazoleThe metabolism of Lumiracoxib can be decreased when combined with Esomeprazole.
Etacrynic acidLumiracoxib may decrease the diuretic activities of Etacrynic acid.
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Lumiracoxib.
Ethyl biscoumacetateLumiracoxib may increase the anticoagulant activities of Ethyl biscoumacetate.
Etidronic acidThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Etidronic acid.
EtodolacThe risk or severity of adverse effects can be increased when Etodolac is combined with Lumiracoxib.
EtofenamateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Etofenamate.
EtoricoxibThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Etoricoxib.
EtravirineThe metabolism of Lumiracoxib can be decreased when combined with Etravirine.
Evening primrose oilThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Evening primrose oil.
exisulindThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with exisulind.
FenbufenThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Fenbufen.
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Lumiracoxib.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Lumiracoxib.
FloxuridineThe metabolism of Lumiracoxib can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Lumiracoxib can be decreased when combined with Fluconazole.
FlunixinThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Flunixin.
FluorouracilThe metabolism of Lumiracoxib can be decreased when combined with Fluorouracil.
FluoxetineThe metabolism of Lumiracoxib can be decreased when combined with Fluoxetine.
FlurbiprofenThe risk or severity of adverse effects can be increased when Flurbiprofen is combined with Lumiracoxib.
FluvastatinThe metabolism of Lumiracoxib can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Lumiracoxib can be decreased when combined with Fluvoxamine.
Folic AcidThe therapeutic efficacy of Folic Acid can be decreased when used in combination with Lumiracoxib.
Fondaparinux sodiumLumiracoxib may increase the anticoagulant activities of Fondaparinux sodium.
ForasartanThe risk or severity of adverse effects can be increased when Forasartan is combined with Lumiracoxib.
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Lumiracoxib.
FosphenytoinThe metabolism of Lumiracoxib can be increased when combined with Fosphenytoin.
FramycetinLumiracoxib may decrease the excretion rate of Framycetin which could result in a lower serum level and potentially a reduction in efficacy.
FurosemideLumiracoxib may decrease the diuretic activities of Furosemide.
GemeprostThe therapeutic efficacy of Gemeprost can be decreased when used in combination with Lumiracoxib.
GemfibrozilThe metabolism of Lumiracoxib can be decreased when combined with Gemfibrozil.
GentamicinLumiracoxib may decrease the excretion rate of Gentamicin which could result in a lower serum level and potentially a reduction in efficacy.
HaloperidolThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Haloperidol.
HeparinLumiracoxib may increase the anticoagulant activities of Heparin.
HirulogLumiracoxib may increase the anticoagulant activities of Hirulog.
HMPL-004The risk or severity of adverse effects can be increased when Lumiracoxib is combined with HMPL-004.
HydralazineLumiracoxib may decrease the antihypertensive activities of Hydralazine.
HydrochlorothiazideThe therapeutic efficacy of Hydrochlorothiazide can be decreased when used in combination with Lumiracoxib.
HydroflumethiazideThe therapeutic efficacy of Hydroflumethiazide can be decreased when used in combination with Lumiracoxib.
Hygromycin BLumiracoxib may decrease the excretion rate of Hygromycin B which could result in a lower serum level and potentially a reduction in efficacy.
IbandronateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Ibandronate.
IbuprofenThe risk or severity of adverse effects can be increased when Ibuprofen is combined with Lumiracoxib.
IbuproxamThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Ibuproxam.
IcatibantThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Icatibant.
IdarubicinLumiracoxib may decrease the excretion rate of Idarubicin which could result in a lower serum level and potentially a reduction in efficacy.
IloprostThe therapeutic efficacy of Iloprost can be decreased when used in combination with Lumiracoxib.
IndapamideThe therapeutic efficacy of Indapamide can be decreased when used in combination with Lumiracoxib.
IndenololLumiracoxib may decrease the antihypertensive activities of Indenolol.
IndinavirThe metabolism of Lumiracoxib can be decreased when combined with Indinavir.
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Lumiracoxib.
IndoprofenThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Indoprofen.
IrbesartanThe risk or severity of adverse effects can be increased when Irbesartan is combined with Lumiracoxib.
IsoniazidThe metabolism of Lumiracoxib can be decreased when combined with Isoniazid.
IsoxicamThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Isoxicam.
KanamycinLumiracoxib may decrease the excretion rate of Kanamycin which could result in a lower serum level and potentially a reduction in efficacy.
KebuzoneThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Kebuzone.
KetoconazoleThe metabolism of Lumiracoxib can be decreased when combined with Ketoconazole.
KetoprofenThe risk or severity of adverse effects can be increased when Ketoprofen is combined with Lumiracoxib.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Lumiracoxib.
LabetalolLumiracoxib may decrease the antihypertensive activities of Labetalol.
LeflunomideThe risk or severity of adverse effects can be increased when Leflunomide is combined with Lumiracoxib.
LepirudinLumiracoxib may increase the anticoagulant activities of Lepirudin.
LevobunololLumiracoxib may decrease the antihypertensive activities of Levobunolol.
LidocaineThe metabolism of Lumiracoxib can be decreased when combined with Lidocaine.
LisinoprilThe risk or severity of adverse effects can be increased when Lisinopril is combined with Lumiracoxib.
LithiumThe serum concentration of Lithium can be increased when it is combined with Lumiracoxib.
LopinavirThe metabolism of Lumiracoxib can be increased when combined with Lopinavir.
LornoxicamThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Lornoxicam.
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Lumiracoxib.
LovastatinThe metabolism of Lumiracoxib can be decreased when combined with Lovastatin.
LoxoprofenThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Loxoprofen.
LubiprostoneThe therapeutic efficacy of Lubiprostone can be decreased when used in combination with Lumiracoxib.
LuliconazoleThe serum concentration of Lumiracoxib can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Lumiracoxib can be decreased when it is combined with Lumacaftor.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Magnesium salicylate.
MasoprocolThe risk or severity of adverse effects can be increased when Masoprocol is combined with Lumiracoxib.
Meclofenamic acidThe risk or severity of adverse effects can be increased when Meclofenamic acid is combined with Lumiracoxib.
Mefenamic acidThe risk or severity of adverse effects can be increased when Mefenamic acid is combined with Lumiracoxib.
MeloxicamThe risk or severity of adverse effects can be increased when Meloxicam is combined with Lumiracoxib.
MesalazineLumiracoxib may increase the nephrotoxic activities of Mesalazine.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Lumiracoxib.
MetamizoleThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Metamizole.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Lumiracoxib.
MethyclothiazideThe therapeutic efficacy of Methyclothiazide can be decreased when used in combination with Lumiracoxib.
MetipranololLumiracoxib may decrease the antihypertensive activities of Metipranolol.
MetolazoneThe therapeutic efficacy of Metolazone can be decreased when used in combination with Lumiracoxib.
MetoprololLumiracoxib may decrease the antihypertensive activities of Metoprolol.
MetrizamideLumiracoxib may decrease the excretion rate of Metrizamide which could result in a lower serum level and potentially a reduction in efficacy.
MexiletineThe metabolism of Lumiracoxib can be decreased when combined with Mexiletine.
MifepristoneThe serum concentration of Lumiracoxib can be increased when it is combined with Mifepristone.
MisoprostolThe therapeutic efficacy of Misoprostol can be decreased when used in combination with Lumiracoxib.
MoclobemideThe metabolism of Lumiracoxib can be decreased when combined with Moclobemide.
ModafinilThe metabolism of Lumiracoxib can be decreased when combined with Modafinil.
MoexiprilThe risk or severity of adverse effects can be increased when Moexipril is combined with Lumiracoxib.
MorniflumateThe risk or severity of adverse effects can be increased when Morniflumate is combined with Lumiracoxib.
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Lumiracoxib.
Mycophenolic acidThe risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Lumiracoxib.
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Lumiracoxib.
NadololLumiracoxib may decrease the antihypertensive activities of Nadolol.
NadroparinLumiracoxib may increase the anticoagulant activities of Nadroparin.
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Lumiracoxib.
NaproxenThe risk or severity of adverse effects can be increased when Naproxen is combined with Lumiracoxib.
NCX 4016The risk or severity of adverse effects can be increased when Lumiracoxib is combined with NCX 4016.
NelfinavirThe metabolism of Lumiracoxib can be decreased when combined with Nelfinavir.
NeomycinLumiracoxib may decrease the excretion rate of Neomycin which could result in a lower serum level and potentially a reduction in efficacy.
NepafenacThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Nepafenac.
NetilmicinLumiracoxib may decrease the excretion rate of Netilmicin which could result in a lower serum level and potentially a reduction in efficacy.
NevirapineThe metabolism of Lumiracoxib can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Lumiracoxib can be decreased when combined with Nicardipine.
Niflumic AcidThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Niflumic Acid.
NimesulideThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Nimesulide.
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Lumiracoxib.
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Lumiracoxib.
OlsalazineLumiracoxib may increase the nephrotoxic activities of Olsalazine.
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Lumiracoxib.
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Omacetaxine mepesuccinate.
OmapatrilatThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Lumiracoxib.
OmeprazoleThe metabolism of Lumiracoxib can be decreased when combined with Omeprazole.
OrgoteinThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Orgotein.
OsimertinibThe serum concentration of Lumiracoxib can be decreased when it is combined with Osimertinib.
OtamixabanLumiracoxib may increase the anticoagulant activities of Otamixaban.
OxaprozinThe risk or severity of adverse effects can be increased when Oxaprozin is combined with Lumiracoxib.
OxprenololLumiracoxib may decrease the antihypertensive activities of Oxprenolol.
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Oxyphenbutazone.
PamidronateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Pamidronate.
PantoprazoleThe metabolism of Lumiracoxib can be decreased when combined with Pantoprazole.
ParecoxibThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Parecoxib.
ParomomycinLumiracoxib may decrease the excretion rate of Paromomycin which could result in a lower serum level and potentially a reduction in efficacy.
Peginterferon alfa-2bThe serum concentration of Lumiracoxib can be increased when it is combined with Peginterferon alfa-2b.
PenbutololLumiracoxib may decrease the antihypertensive activities of Penbutolol.
Pentosan PolysulfateLumiracoxib may increase the anticoagulant activities of Pentosan Polysulfate.
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Lumiracoxib.
PhenindioneLumiracoxib may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe metabolism of Lumiracoxib can be increased when combined with Phenobarbital.
PhenprocoumonLumiracoxib may increase the anticoagulant activities of Phenprocoumon.
PhenylbutazoneThe risk or severity of adverse effects can be increased when Phenylbutazone is combined with Lumiracoxib.
PhenytoinThe metabolism of Lumiracoxib can be increased when combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Lumiracoxib.
PindololLumiracoxib may decrease the antihypertensive activities of Pindolol.
PiretanideLumiracoxib may decrease the diuretic activities of Piretanide.
PirfenidoneThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Pirfenidone.
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Lumiracoxib.
PlicamycinLumiracoxib may decrease the excretion rate of Plicamycin which could result in a lower serum level and potentially a reduction in efficacy.
PolythiazideThe therapeutic efficacy of Polythiazide can be decreased when used in combination with Lumiracoxib.
PractololLumiracoxib may decrease the antihypertensive activities of Practolol.
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Lumiracoxib.
PrimidoneThe metabolism of Lumiracoxib can be increased when combined with Primidone.
ProbenecidThe serum concentration of Lumiracoxib can be increased when it is combined with Probenecid.
PropacetamolThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Propacetamol.
PropranololLumiracoxib may decrease the antihypertensive activities of Propranolol.
Prostaglandin D2The therapeutic efficacy of Prostaglandin D2 can be decreased when used in combination with Lumiracoxib.
Protein CLumiracoxib may increase the anticoagulant activities of Protein C.
ProtocatechualdehydeLumiracoxib may increase the anticoagulant activities of Protocatechualdehyde.
PTC299The risk or severity of adverse effects can be increased when Lumiracoxib is combined with PTC299.
PuromycinLumiracoxib may decrease the excretion rate of Puromycin which could result in a lower serum level and potentially a reduction in efficacy.
PyrimethamineThe metabolism of Lumiracoxib can be decreased when combined with Pyrimethamine.
QuinaprilThe risk or severity of adverse effects can be increased when Quinapril is combined with Lumiracoxib.
QuinethazoneThe therapeutic efficacy of Quinethazone can be decreased when used in combination with Lumiracoxib.
QuinineThe metabolism of Lumiracoxib can be decreased when combined with Quinine.
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Lumiracoxib.
RescinnamineThe risk or severity of adverse effects can be increased when Rescinnamine is combined with Lumiracoxib.
ResveratrolThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Resveratrol.
ReviparinLumiracoxib may increase the anticoagulant activities of Reviparin.
RibostamycinLumiracoxib may decrease the excretion rate of Ribostamycin which could result in a lower serum level and potentially a reduction in efficacy.
RifampicinThe metabolism of Lumiracoxib can be increased when combined with Rifampicin.
RifapentineThe metabolism of Lumiracoxib can be increased when combined with Rifapentine.
RisedronateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Risedronate.
RivaroxabanLumiracoxib may increase the anticoagulant activities of Rivaroxaban.
RofecoxibThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Lumiracoxib.
RopiniroleThe metabolism of Lumiracoxib can be decreased when combined with Ropinirole.
SalicylamideThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Salicylamide.
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Lumiracoxib.
SalsalateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Salsalate.
SaprisartanThe risk or severity of adverse effects can be increased when Saprisartan is combined with Lumiracoxib.
SaralasinThe risk or severity of adverse effects can be increased when Saralasin is combined with Lumiracoxib.
SecobarbitalThe metabolism of Lumiracoxib can be increased when combined with Secobarbital.
SeratrodastThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Seratrodast.
SertralineThe metabolism of Lumiracoxib can be decreased when combined with Sertraline.
SildenafilThe metabolism of Lumiracoxib can be decreased when combined with Sildenafil.
SimeprevirThe metabolism of Lumiracoxib can be decreased when combined with Simeprevir.
SorafenibThe metabolism of Lumiracoxib can be decreased when combined with Sorafenib.
SotalolLumiracoxib may decrease the antihypertensive activities of Sotalol.
SpectinomycinLumiracoxib may decrease the excretion rate of Spectinomycin which could result in a lower serum level and potentially a reduction in efficacy.
SpiraprilThe risk or severity of adverse effects can be increased when Spirapril is combined with Lumiracoxib.
SpironolactoneLumiracoxib may decrease the antihypertensive activities of Spironolactone.
SRT501The risk or severity of adverse effects can be increased when Lumiracoxib is combined with SRT501.
StiripentolThe metabolism of Lumiracoxib can be decreased when combined with Stiripentol.
StreptomycinLumiracoxib may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
StreptozocinLumiracoxib may decrease the excretion rate of Streptozocin which could result in a lower serum level and potentially a reduction in efficacy.
SulfadiazineThe metabolism of Lumiracoxib can be decreased when combined with Sulfadiazine.
SulfamethoxazoleThe metabolism of Lumiracoxib can be decreased when combined with Sulfamethoxazole.
SulfasalazineLumiracoxib may increase the nephrotoxic activities of Sulfasalazine.
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Lumiracoxib.
SulfisoxazoleThe metabolism of Lumiracoxib can be decreased when combined with Sulfisoxazole.
SulindacThe risk or severity of adverse effects can be increased when Sulindac is combined with Lumiracoxib.
SulodexideLumiracoxib may increase the anticoagulant activities of Sulodexide.
SuprofenThe risk or severity of adverse effects can be increased when Suprofen is combined with Lumiracoxib.
TacrolimusLumiracoxib may increase the nephrotoxic activities of Tacrolimus.
TalniflumateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Lumiracoxib.
TasosartanThe risk or severity of adverse effects can be increased when Tasosartan is combined with Lumiracoxib.
Technetium Tc-99m MedronateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Technetium Tc-99m Medronate.
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Lumiracoxib.
TemocaprilThe risk or severity of adverse effects can be increased when Temocapril is combined with Lumiracoxib.
TenofovirThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Tenofovir.
TenofovirThe metabolism of Lumiracoxib can be decreased when combined with Tenofovir.
TenoxicamThe risk or severity of adverse effects can be increased when Tenoxicam is combined with Lumiracoxib.
TepoxalinThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Tepoxalin.
TeriflunomideThe serum concentration of Lumiracoxib can be decreased when it is combined with Teriflunomide.
TeriflunomideThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Teriflunomide.
TheophyllineThe metabolism of Lumiracoxib can be decreased when combined with Theophylline.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Tiaprofenic acid.
TicagrelorThe metabolism of Lumiracoxib can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Lumiracoxib can be decreased when combined with Ticlopidine.
TiludronateThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Tiludronate.
TimololLumiracoxib may decrease the antihypertensive activities of Timolol.
TobramycinLumiracoxib may decrease the excretion rate of Tobramycin which could result in a lower serum level and potentially a reduction in efficacy.
TolbutamideThe metabolism of Lumiracoxib can be decreased when combined with Tolbutamide.
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Tolfenamic Acid.
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Lumiracoxib.
TopiramateThe metabolism of Lumiracoxib can be decreased when combined with Topiramate.
TorasemideLumiracoxib may decrease the diuretic activities of Torasemide.
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Lumiracoxib.
TranilastThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Tranilast.
TranylcypromineThe metabolism of Lumiracoxib can be decreased when combined with Tranylcypromine.
TravoprostThe therapeutic efficacy of Travoprost can be decreased when used in combination with Lumiracoxib.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Lumiracoxib.
TriamtereneLumiracoxib may decrease the antihypertensive activities of Triamterene.
TrichlormethiazideThe therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Lumiracoxib.
TrimethoprimThe metabolism of Lumiracoxib can be decreased when combined with Trimethoprim.
Trisalicylate-cholineThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Trisalicylate-choline.
ValdecoxibThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Lumiracoxib.
Valproic AcidThe metabolism of Lumiracoxib can be decreased when combined with Valproic Acid.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Lumiracoxib.
VancomycinThe serum concentration of Vancomycin can be increased when it is combined with Lumiracoxib.
VemurafenibThe serum concentration of Lumiracoxib can be increased when it is combined with Vemurafenib.
VoriconazoleThe metabolism of Lumiracoxib can be decreased when combined with Voriconazole.
WarfarinLumiracoxib may increase the anticoagulant activities of Warfarin.
XimelagatranLumiracoxib may increase the anticoagulant activities of Ximelagatran.
ZafirlukastThe metabolism of Lumiracoxib can be decreased when combined with Zafirlukast.
ZaltoprofenThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Zaltoprofen.
ZileutonThe risk or severity of adverse effects can be increased when Zileuton is combined with Lumiracoxib.
Zoledronic acidThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Zoledronic acid.
ZomepiracThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Zomepirac.
Food Interactions
  • Take with or without food. Food has no effect on the absorption of the product.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, p...
Gene Name:
PTGS2
Uniprot ID:
P35354
Molecular Weight:
68995.625 Da
References
  1. Capone ML, Tacconelli S, Sciulli MG, Patrignani P: Clinical pharmacology of selective COX-2 inhibitors. Int J Immunopathol Pharmacol. 2003 May-Aug;16(2 Suppl):49-58. [PubMed:14552704 ]
  2. Tacconelli S, Capone ML, Patrignani P: Clinical pharmacology of novel selective COX-2 inhibitors. Curr Pharm Des. 2004;10(6):589-601. [PubMed:14965322 ]
  3. Atherton C, Jones J, McKaig B, Bebb J, Cunliffe R, Burdsall J, Brough J, Stevenson D, Bonner J, Rordorf C, Scott G, Branson J, Hawkey CJ: Pharmacology and gastrointestinal safety of lumiracoxib, a novel cyclooxygenase-2 selective inhibitor: An integrated study. Clin Gastroenterol Hepatol. 2004 Feb;2(2):113-20. [PubMed:15017615 ]
  4. Kalbag J, Yeh CM, Milosavljev S, Lasseter K, Oberstein S, Rordorf C: No influence of moderate hepatic impairment on the pharmacokinetics of lumiracoxib, an oral COX-2 selective inhibitor. Pharmacol Res. 2004 Aug;50(2):181-6. [PubMed:15177307 ]
  5. Esser R, Berry C, Du Z, Dawson J, Fox A, Fujimoto RA, Haston W, Kimble EF, Koehler J, Peppard J, Quadros E, Quintavalla J, Toscano K, Urban L, van Duzer J, Zhang X, Zhou S, Marshall PJ: Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2. Br J Pharmacol. 2005 Feb;144(4):538-50. [PubMed:15655513 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Capone ML, Tacconelli S, Sciulli MG, Patrignani P: Clinical pharmacology of selective COX-2 inhibitors. Int J Immunopathol Pharmacol. 2003 May-Aug;16(2 Suppl):49-58. [PubMed:14552704 ]
  2. Esser R, Berry C, Du Z, Dawson J, Fox A, Fujimoto RA, Haston W, Kimble EF, Koehler J, Peppard J, Quadros E, Quintavalla J, Toscano K, Urban L, van Duzer J, Zhang X, Zhou S, Marshall PJ: Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2. Br J Pharmacol. 2005 Feb;144(4):538-50. [PubMed:15655513 ]
  3. Jermany J, Branson J, Schmouder R, Guillaume M, Rordorf C: Lumiracoxib does not affect the ex vivo antiplatelet aggregation activity of low-dose aspirin in healthy subjects. J Clin Pharmacol. 2005 Oct;45(10):1172-8. [PubMed:16172182 ]
  4. Warner TD, Vojnovic I, Bishop-Bailey D, Mitchell JA: Influence of plasma protein on the potencies of inhibitors of cyclooxygenase-1 and -2. FASEB J. 2006 Mar;20(3):542-4. Epub 2006 Jan 10. [PubMed:16403783 ]
  5. Blobaum AL, Marnett LJ: Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib. J Biol Chem. 2007 Jun 1;282(22):16379-90. Epub 2007 Apr 12. [PubMed:17434872 ]

Enzymes

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. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
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
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A9
Uniprot ID:
O60656
Molecular Weight:
59940.495 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 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 May 17, 2007 10:57 / Updated on August 17, 2016 12:23