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Identification
NameValdecoxib
Accession NumberDB00580  (APRD00183, DB07576)
TypeSmall Molecule
GroupsInvestigational, Withdrawn
DescriptionValdecoxib was removed from the Canadian, U.S., and E.U. markets in 2005 due to concerns about possible increased risk of heart attack and stroke.
Structure
Thumb
SynonymsNot Available
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
BextraNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII2919279Q3W
CAS number181695-72-7
WeightAverage: 314.359
Monoisotopic: 314.072513014
Chemical FormulaC16H14N2O3S
InChI KeyInChIKey=LNPDTQAFDNKSHK-UHFFFAOYSA-N
InChI
InChI=1S/C16H14N2O3S/c1-11-15(12-7-9-14(10-8-12)22(17,19)20)16(18-21-11)13-5-3-2-4-6-13/h2-10H,1H3,(H2,17,19,20)
IUPAC Name
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzene-1-sulfonamide
SMILES
CC1=C(C(=NO1)C1=CC=CC=C1)C1=CC=C(C=C1)S(N)(=O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzenesulfonamides. These are organic compounds containing a sulfonamide group that is S-linked to a benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzenesulfonamides
Direct ParentBenzenesulfonamides
Alternative Parents
Substituents
  • Benzenesulfonamide
  • Heteroaromatic compound
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Oxazole
  • Isoxazole
  • Azole
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of osteoarthritis and dysmenorrhoea
PharmacodynamicsValdecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Valdecoxib is used for its anti-inflammatory, analgesic, and antipyretic activities in the management of osteoarthritis (OA) and for the treatment of dysmenorrhea or acute pain. Unlike celecoxib, valdecoxib lacks a sulfonamide chain and does not require CYP450 enzymes for metabolism.
Mechanism of actionBoth COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane. Valdecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, important for the mediation of inflammation and pain. Unlike non-selective NSAIDs, valdecoxib does not inhibit platelet aggregation.
Related Articles
AbsorptionOral bioavailability is 83%.
Volume of distribution
  • 86 L
Protein binding98%
Metabolism

Hepatic (involves CYP3A4 and 2C9)

SubstrateEnzymesProduct
Valdecoxib
Valdecoxib N-glucuronideDetails
Valdecoxib
Not Available
Valdecoxib metabolite M2Details
Valdecoxib metabolite M2
Valdecoxib metabolite M2 glucuronideDetails
Valdecoxib metabolite M2
Not Available
Valdecoxib metabolite M7Details
Valdecoxib metabolite M7
Not Available
Valdecoxib metabolite M8Details
Valdecoxib metabolite M2
Not Available
Valdecoxib metabolite M5Details
Valdecoxib metabolite M5
Valdecoxib metabolite M5 glucuronideDetails
Valdecoxib
Valdecoxib metabolite M1Details
Valdecoxib metabolite M1
Valdecoxib metabolite M1 glucuronideDetails
Valdecoxib metabolite M1
Not Available
Valdecoxib metabolite M5Details
Valdecoxib metabolite M1
Not Available
Valdecoxib metabolite M4Details
Valdecoxib metabolite M1
Not Available
Valdecoxib metabolite M3Details
Valdecoxib metabolite M3
Valdecoxib metabolite M3 glucuronideDetails
Valdecoxib
Valdecoxib metabolite M9Details
Valdecoxib metabolite M9
Valdecoxib metabolite M3Details
Valdecoxib metabolite M9
Valdecoxib metabolite M9 glucuronideDetails
Route of eliminationValdecoxib is eliminated predominantly via hepatic metabolism with less than 5% of the dose excreted unchanged in the urine and feces. About 70% of the dose is excreted in the urine as metabolites, and about 20% as valdecoxib N-glucuronide.
Half life8-11 hours
Clearance
  • oral cl=6 L/h
  • 6 – 7 L/h [In patients undergoing hemodialysis]
  • 6 – 7 L/h [healthy elderly subjects]
ToxicitySymptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur, but are rare.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Valdecoxib Action PathwayDrug actionSMP00116
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9386
Caco-2 permeable+0.5
P-glycoprotein substrateNon-substrate0.8864
P-glycoprotein inhibitor INon-inhibitor0.8772
P-glycoprotein inhibitor IINon-inhibitor0.9157
Renal organic cation transporterNon-inhibitor0.8576
CYP450 2C9 substrateNon-substrate0.7356
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.6501
CYP450 1A2 substrateNon-inhibitor0.5759
CYP450 2C9 inhibitorInhibitor0.5385
CYP450 2D6 inhibitorNon-inhibitor0.8875
CYP450 2C19 inhibitorInhibitor0.5958
CYP450 3A4 inhibitorNon-inhibitor0.8652
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7649
Ames testNon AMES toxic0.8277
CarcinogenicityNon-carcinogens0.7399
BiodegradationNot ready biodegradable0.9948
Rat acute toxicity2.0680 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9708
hERG inhibition (predictor II)Non-inhibitor0.8652
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Gd searle llc
Packagers
Dosage formsNot Available
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2212836 No2003-08-122016-02-12Canada
US5633272 No1995-02-132015-02-13Us
US7135489 No1997-08-122017-08-12Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP3.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0348 mg/mLALOGPS
logP3.32ALOGPS
logP2.82ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)10.06ChemAxon
pKa (Strongest Basic)0.42ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area86.19 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity84.71 m3·mol-1ChemAxon
Polarizability31.76 Å3ChemAxon
Number of Rings3ChemAxon
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 Reference

Eswaraiah Sajja, Anumula Reddy, Aalla Sampath, Gilla Goverdhan, “Process for preparing crystalline form A of valdecoxib.” U.S. Patent US20050272787, issued December 08, 2005.

US20050272787
General ReferencesNot Available
External Links
ATC CodesM01AH03
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (82.8 KB)
MSDSDownload (70.6 KB)
Interactions
Drug Interactions
Drug
AbciximabValdecoxib may increase the anticoagulant activities of Abciximab.
AbirateroneThe metabolism of Valdecoxib can be decreased when combined with Abiraterone.
AcebutololValdecoxib may decrease the antihypertensive activities of Acebutolol.
AceclofenacThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Aceclofenac.
AcenocoumarolValdecoxib may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Acetylsalicylic acid.
AdapaleneThe risk or severity of adverse effects can be increased when Adapalene is combined with Valdecoxib.
Alendronic acidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Alendronic acid.
AliskirenValdecoxib may decrease the antihypertensive activities of Aliskiren.
AlprenololValdecoxib may decrease the antihypertensive activities of Alprenolol.
AlprostadilThe therapeutic efficacy of Alprostadil can be decreased when used in combination with Valdecoxib.
AmikacinValdecoxib may decrease the excretion rate of Amikacin which could result in a lower serum level and potentially a reduction in efficacy.
AmilorideValdecoxib may decrease the antihypertensive activities of Amiloride.
AmiodaroneThe metabolism of Valdecoxib can be decreased when combined with Amiodarone.
AncrodValdecoxib may increase the anticoagulant activities of Ancrod.
AntipyrineThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Antipyrine.
Antithrombin III humanValdecoxib may increase the anticoagulant activities of Antithrombin III human.
ApixabanValdecoxib may increase the anticoagulant activities of Apixaban.
ApremilastThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Apremilast.
AprepitantThe serum concentration of Valdecoxib can be increased when it is combined with Aprepitant.
ArdeparinValdecoxib may increase the anticoagulant activities of Ardeparin.
ArgatrobanValdecoxib may increase the anticoagulant activities of Argatroban.
ArotinololValdecoxib may decrease the antihypertensive activities of Arotinolol.
AtazanavirThe metabolism of Valdecoxib can be decreased when combined with Atazanavir.
AtenololValdecoxib may decrease the antihypertensive activities of Atenolol.
AtomoxetineThe metabolism of Valdecoxib can be decreased when combined with Atomoxetine.
AzapropazoneThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Azapropazone.
AzelastineThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Azelastine.
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Valdecoxib.
BalsalazideValdecoxib may increase the nephrotoxic activities of Balsalazide.
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Valdecoxib.
BecaplerminValdecoxib may increase the anticoagulant activities of Becaplermin.
BefunololValdecoxib may decrease the antihypertensive activities of Befunolol.
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Valdecoxib.
BendroflumethiazideThe therapeutic efficacy of Bendroflumethiazide can be decreased when used in combination with Valdecoxib.
BenoxaprofenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Benoxaprofen.
BetaxololValdecoxib may decrease the antihypertensive activities of Betaxolol.
BevantololValdecoxib may decrease the antihypertensive activities of Bevantolol.
BexaroteneThe serum concentration of Valdecoxib can be decreased when it is combined with Bexarotene.
BimatoprostThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Valdecoxib.
BisoprololValdecoxib may decrease the antihypertensive activities of Bisoprolol.
BivalirudinValdecoxib may increase the anticoagulant activities of Bivalirudin.
BoceprevirThe metabolism of Valdecoxib can be decreased when combined with Boceprevir.
BopindololValdecoxib may decrease the antihypertensive activities of Bopindolol.
BortezomibThe metabolism of Valdecoxib can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Valdecoxib can be decreased when it is combined with Bosentan.
BromfenacThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Bromfenac.
BufuralolValdecoxib may decrease the antihypertensive activities of Bufuralol.
BumetanideValdecoxib may decrease the diuretic activities of Bumetanide.
BupranololValdecoxib may decrease the antihypertensive activities of Bupranolol.
CandesartanThe risk or severity of adverse effects can be increased when Candesartan is combined with Valdecoxib.
CandoxatrilThe risk or severity of adverse effects can be increased when Candoxatril is combined with Valdecoxib.
CapecitabineThe metabolism of Valdecoxib can be decreased when combined with Capecitabine.
CaptoprilThe risk or severity of adverse effects can be increased when Captopril is combined with Valdecoxib.
CarbamazepineThe metabolism of Valdecoxib can be increased when combined with Carbamazepine.
Carboprost TromethamineThe therapeutic efficacy of Carboprost Tromethamine can be decreased when used in combination with Valdecoxib.
CarprofenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Carprofen.
CarteololValdecoxib may decrease the antihypertensive activities of Carteolol.
CarvedilolValdecoxib may decrease the antihypertensive activities of Carvedilol.
CastanospermineThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Castanospermine.
CelecoxibThe risk or severity of adverse effects can be increased when Celecoxib is combined with Valdecoxib.
CeliprololValdecoxib may decrease the antihypertensive activities of Celiprolol.
CeritinibThe serum concentration of Valdecoxib can be increased when it is combined with Ceritinib.
CertoparinValdecoxib may increase the anticoagulant activities of Certoparin.
ChloroquineThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Chloroquine.
ChlorothiazideThe therapeutic efficacy of Chlorothiazide can be decreased when used in combination with Valdecoxib.
ChlorthalidoneThe therapeutic efficacy of Chlorthalidone can be decreased when used in combination with Valdecoxib.
CholecalciferolThe metabolism of Valdecoxib can be decreased when combined with Cholecalciferol.
CholestyramineCholestyramine can cause a decrease in the absorption of Valdecoxib 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 Valdecoxib.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Valdecoxib.
Citric AcidValdecoxib may increase the anticoagulant activities of Citric Acid.
ClarithromycinThe metabolism of Valdecoxib can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Valdecoxib can be decreased when combined with Clemastine.
ClodronateThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Clodronate.
ClonixinThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Clonixin.
CloprostenolThe therapeutic efficacy of Cloprostenol can be decreased when used in combination with Valdecoxib.
ClotrimazoleThe metabolism of Valdecoxib can be decreased when combined with Clotrimazole.
CobicistatThe metabolism of Valdecoxib can be decreased when combined with Cobicistat.
ColesevelamColesevelam can cause a decrease in the absorption of Valdecoxib resulting in a reduced serum concentration and potentially a decrease in efficacy.
ColestipolColestipol can cause a decrease in the absorption of Valdecoxib resulting in a reduced serum concentration and potentially a decrease in efficacy.
ConivaptanThe serum concentration of Valdecoxib can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Valdecoxib can be decreased when combined with Crizotinib.
CyclosporineValdecoxib may increase the nephrotoxic activities of Cyclosporine.
CyclosporineThe metabolism of Valdecoxib can be decreased when combined with Cyclosporine.
D-LimoneneThe risk or severity of adverse effects can be increased when Valdecoxib is combined with D-Limonene.
Dabigatran etexilateValdecoxib may increase the anticoagulant activities of Dabigatran etexilate.
DabrafenibThe serum concentration of Valdecoxib can be decreased when it is combined with Dabrafenib.
DalteparinValdecoxib may increase the anticoagulant activities of Dalteparin.
DanaparoidValdecoxib may increase the anticoagulant activities of Danaparoid.
DarunavirThe metabolism of Valdecoxib can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Valdecoxib can be increased when it is combined with Dasatinib.
DaunorubicinValdecoxib 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 Valdecoxib can be decreased when it is combined with Deferasirox.
DeferasiroxThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Deferasirox.
DelavirdineThe metabolism of Valdecoxib can be decreased when combined with Delavirdine.
DesirudinValdecoxib may increase the anticoagulant activities of Desirudin.
DesmopressinThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Desmopressin.
DexamethasoneThe serum concentration of Valdecoxib can be decreased when it is combined with Dexamethasone.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Valdecoxib.
DextranValdecoxib may increase the anticoagulant activities of Dextran.
Dextran 40Valdecoxib may increase the anticoagulant activities of Dextran 40.
Dextran 70Valdecoxib may increase the anticoagulant activities of Dextran 70.
Dextran 75Valdecoxib may increase the anticoagulant activities of Dextran 75.
DiclofenacThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Diclofenac.
DicoumarolValdecoxib may increase the anticoagulant activities of Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Diflunisal.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Valdecoxib.
DihydroergotamineThe metabolism of Valdecoxib can be decreased when combined with Dihydroergotamine.
DihydrostreptomycinValdecoxib may decrease the excretion rate of Dihydrostreptomycin which could result in a lower serum level and potentially a reduction in efficacy.
DiltiazemThe metabolism of Valdecoxib can be decreased when combined with Diltiazem.
DinoprostoneThe therapeutic efficacy of Dinoprostone can be decreased when used in combination with Valdecoxib.
DoxorubicinValdecoxib may decrease the excretion rate of Doxorubicin which could result in a lower serum level and potentially a reduction in efficacy.
DoxycyclineThe metabolism of Valdecoxib can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Valdecoxib can be decreased when combined with Dronedarone.
DrospirenoneValdecoxib may increase the hyperkalemic activities of Drospirenone.
DroxicamThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Droxicam.
Edetic AcidValdecoxib may increase the anticoagulant activities of Edetic Acid.
EdoxabanValdecoxib may increase the anticoagulant activities of Edoxaban.
EfavirenzThe serum concentration of Valdecoxib can be decreased when it is combined with Efavirenz.
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Valdecoxib.
EnalaprilatThe risk or severity of adverse effects can be increased when Enalaprilat is combined with Valdecoxib.
EnoxaparinValdecoxib may increase the anticoagulant activities of Enoxaparin.
EnzalutamideThe serum concentration of Valdecoxib can be decreased when it is combined with Enzalutamide.
EpirizoleThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Epirizole.
EpirubicinValdecoxib may decrease the excretion rate of Epirubicin which could result in a lower serum level and potentially a reduction in efficacy.
EplerenoneValdecoxib may decrease the antihypertensive activities of Eplerenone.
EpoprostenolThe therapeutic efficacy of Epoprostenol can be decreased when used in combination with Valdecoxib.
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Valdecoxib.
ErythromycinThe metabolism of Valdecoxib can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Valdecoxib can be decreased when it is combined with Eslicarbazepine acetate.
EsmololValdecoxib may decrease the antihypertensive activities of Esmolol.
Etacrynic acidValdecoxib may decrease the diuretic activities of Etacrynic acid.
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Valdecoxib.
Ethyl biscoumacetateValdecoxib may increase the anticoagulant activities of Ethyl biscoumacetate.
Etidronic acidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Etidronic acid.
EtodolacThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Etodolac.
EtofenamateThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Etofenamate.
EtoricoxibThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Etoricoxib.
EtravirineThe serum concentration of Valdecoxib can be decreased when it is combined with Etravirine.
Evening primrose oilThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Evening primrose oil.
exisulindThe risk or severity of adverse effects can be increased when Valdecoxib is combined with exisulind.
FenbufenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Fenbufen.
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Valdecoxib.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Valdecoxib.
FloxuridineThe metabolism of Valdecoxib can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Valdecoxib can be decreased when combined with Fluconazole.
FlunixinThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Flunixin.
FluorouracilThe metabolism of Valdecoxib can be decreased when combined with Fluorouracil.
FlurbiprofenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Flurbiprofen.
FluvastatinThe metabolism of Valdecoxib can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Valdecoxib can be decreased when combined with Fluvoxamine.
Folic AcidThe therapeutic efficacy of Folic Acid can be decreased when used in combination with Valdecoxib.
Fondaparinux sodiumValdecoxib may increase the anticoagulant activities of Fondaparinux sodium.
ForasartanThe risk or severity of adverse effects can be increased when Forasartan is combined with Valdecoxib.
FosamprenavirThe metabolism of Valdecoxib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Valdecoxib can be increased when it is combined with Fosaprepitant.
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Valdecoxib.
FosphenytoinThe metabolism of Valdecoxib can be increased when combined with Fosphenytoin.
FramycetinValdecoxib may decrease the excretion rate of Framycetin which could result in a lower serum level and potentially a reduction in efficacy.
FurosemideValdecoxib may decrease the diuretic activities of Furosemide.
Fusidic AcidThe serum concentration of Valdecoxib can be increased when it is combined with Fusidic Acid.
GemeprostThe therapeutic efficacy of Gemeprost can be decreased when used in combination with Valdecoxib.
GemfibrozilThe metabolism of Valdecoxib can be decreased when combined with Gemfibrozil.
GentamicinValdecoxib 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 Valdecoxib is combined with Haloperidol.
HeparinValdecoxib may increase the anticoagulant activities of Heparin.
HirulogValdecoxib may increase the anticoagulant activities of Hirulog.
HMPL-004The risk or severity of adverse effects can be increased when Valdecoxib is combined with HMPL-004.
HydralazineValdecoxib may decrease the antihypertensive activities of Hydralazine.
HydrochlorothiazideThe therapeutic efficacy of Hydrochlorothiazide can be decreased when used in combination with Valdecoxib.
HydroflumethiazideThe therapeutic efficacy of Hydroflumethiazide can be decreased when used in combination with Valdecoxib.
Hygromycin BValdecoxib 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 Valdecoxib is combined with Ibandronate.
IbuprofenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Ibuprofen.
IbuproxamThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Ibuproxam.
IcatibantThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Icatibant.
IdarubicinValdecoxib may decrease the excretion rate of Idarubicin which could result in a lower serum level and potentially a reduction in efficacy.
IdelalisibThe serum concentration of Valdecoxib can be increased when it is combined with Idelalisib.
IloprostThe therapeutic efficacy of Iloprost can be decreased when used in combination with Valdecoxib.
ImatinibThe metabolism of Valdecoxib can be decreased when combined with Imatinib.
IndapamideThe therapeutic efficacy of Indapamide can be decreased when used in combination with Valdecoxib.
IndenololValdecoxib may decrease the antihypertensive activities of Indenolol.
IndinavirThe metabolism of Valdecoxib can be decreased when combined with Indinavir.
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Valdecoxib.
IndoprofenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Indoprofen.
IrbesartanThe risk or severity of adverse effects can be increased when Irbesartan is combined with Valdecoxib.
IsavuconazoniumThe metabolism of Valdecoxib can be decreased when combined with Isavuconazonium.
IsoxicamThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Isoxicam.
IsradipineThe metabolism of Valdecoxib can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Valdecoxib can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Valdecoxib can be increased when it is combined with Ivacaftor.
KanamycinValdecoxib 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 Valdecoxib is combined with Kebuzone.
KetoconazoleThe metabolism of Valdecoxib can be decreased when combined with Ketoconazole.
KetoprofenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Ketoprofen.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Valdecoxib.
LabetalolValdecoxib may decrease the antihypertensive activities of Labetalol.
LeflunomideThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Leflunomide.
LepirudinValdecoxib may increase the anticoagulant activities of Lepirudin.
LevobunololValdecoxib may decrease the antihypertensive activities of Levobunolol.
LisinoprilThe risk or severity of adverse effects can be increased when Lisinopril is combined with Valdecoxib.
LithiumThe serum concentration of Lithium can be increased when it is combined with Valdecoxib.
LopinavirThe metabolism of Valdecoxib can be decreased when combined with Lopinavir.
LornoxicamThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Lornoxicam.
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Valdecoxib.
LovastatinThe metabolism of Valdecoxib can be decreased when combined with Lovastatin.
LoxoprofenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Loxoprofen.
LubiprostoneThe therapeutic efficacy of Lubiprostone can be decreased when used in combination with Valdecoxib.
LuliconazoleThe serum concentration of Valdecoxib can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Valdecoxib can be decreased when it is combined with Lumacaftor.
LumiracoxibThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Lumiracoxib.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Magnesium salicylate.
MasoprocolThe risk or severity of adverse effects can be increased when Masoprocol is combined with Valdecoxib.
Meclofenamic acidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Meclofenamic acid.
Mefenamic acidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Mefenamic acid.
MeloxicamThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Meloxicam.
MesalazineValdecoxib may increase the nephrotoxic activities of Mesalazine.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Valdecoxib.
MetamizoleThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Metamizole.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Valdecoxib.
MethyclothiazideThe therapeutic efficacy of Methyclothiazide can be decreased when used in combination with Valdecoxib.
MetipranololValdecoxib may decrease the antihypertensive activities of Metipranolol.
MetolazoneThe therapeutic efficacy of Metolazone can be decreased when used in combination with Valdecoxib.
MetoprololValdecoxib may decrease the antihypertensive activities of Metoprolol.
MetrizamideValdecoxib may decrease the excretion rate of Metrizamide which could result in a lower serum level and potentially a reduction in efficacy.
MifepristoneThe metabolism of Valdecoxib can be decreased when combined with Mifepristone.
MisoprostolThe therapeutic efficacy of Misoprostol can be decreased when used in combination with Valdecoxib.
MitotaneThe serum concentration of Valdecoxib can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Valdecoxib can be decreased when it is combined with Modafinil.
MoexiprilThe risk or severity of adverse effects can be increased when Moexipril is combined with Valdecoxib.
MorniflumateThe risk or severity of adverse effects can be increased when Morniflumate is combined with Valdecoxib.
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Mycophenolate mofetil.
Mycophenolic acidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Mycophenolic acid.
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Valdecoxib.
NadololValdecoxib may decrease the antihypertensive activities of Nadolol.
NadroparinValdecoxib may increase the anticoagulant activities of Nadroparin.
NafcillinThe serum concentration of Valdecoxib can be decreased when it is combined with Nafcillin.
NaftifineThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Naftifine.
NaproxenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Naproxen.
NCX 4016The risk or severity of adverse effects can be increased when Valdecoxib is combined with NCX 4016.
NefazodoneThe metabolism of Valdecoxib can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Valdecoxib can be decreased when combined with Nelfinavir.
NeomycinValdecoxib 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 Valdecoxib is combined with Nepafenac.
NetilmicinValdecoxib may decrease the excretion rate of Netilmicin which could result in a lower serum level and potentially a reduction in efficacy.
NetupitantThe serum concentration of Valdecoxib can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Valdecoxib can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Valdecoxib can be decreased when combined with Nicardipine.
Niflumic AcidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Niflumic Acid.
NilotinibThe metabolism of Valdecoxib can be decreased when combined with Nilotinib.
NimesulideThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Nimesulide.
OlaparibThe metabolism of Valdecoxib can be decreased when combined with Olaparib.
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Valdecoxib.
OlopatadineThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Olopatadine.
OlsalazineValdecoxib may increase the nephrotoxic activities of Olsalazine.
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Valdecoxib.
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Omacetaxine mepesuccinate.
OmapatrilatThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Valdecoxib.
OmeprazoleThe metabolism of Valdecoxib can be decreased when combined with Omeprazole.
OrgoteinThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Orgotein.
OsimertinibThe serum concentration of Valdecoxib can be increased when it is combined with Osimertinib.
OtamixabanValdecoxib may increase the anticoagulant activities of Otamixaban.
OxaprozinThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Oxaprozin.
OxprenololValdecoxib may decrease the antihypertensive activities of Oxprenolol.
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Oxyphenbutazone.
PalbociclibThe serum concentration of Valdecoxib can be increased when it is combined with Palbociclib.
PamidronateThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Pamidronate.
ParecoxibThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Parecoxib.
ParomomycinValdecoxib may decrease the excretion rate of Paromomycin which could result in a lower serum level and potentially a reduction in efficacy.
PenbutololValdecoxib may decrease the antihypertensive activities of Penbutolol.
PentobarbitalThe metabolism of Valdecoxib can be increased when combined with Pentobarbital.
Pentosan PolysulfateValdecoxib may increase the anticoagulant activities of Pentosan Polysulfate.
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Valdecoxib.
PhenindioneValdecoxib may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe metabolism of Valdecoxib can be increased when combined with Phenobarbital.
PhenprocoumonValdecoxib may increase the anticoagulant activities of Phenprocoumon.
PhenylbutazoneThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Phenylbutazone.
PhenytoinThe metabolism of Valdecoxib can be increased when combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Valdecoxib.
PindololValdecoxib may decrease the antihypertensive activities of Pindolol.
PiretanideValdecoxib may decrease the diuretic activities of Piretanide.
PirfenidoneThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Pirfenidone.
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Valdecoxib.
PlicamycinValdecoxib 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 Valdecoxib.
PosaconazoleThe metabolism of Valdecoxib can be decreased when combined with Posaconazole.
PractololValdecoxib may decrease the antihypertensive activities of Practolol.
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Valdecoxib.
PrimidoneThe metabolism of Valdecoxib can be increased when combined with Primidone.
ProbenecidThe serum concentration of Valdecoxib can be increased when it is combined with Probenecid.
PropacetamolThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Propacetamol.
PropranololValdecoxib may decrease the antihypertensive activities of Propranolol.
Prostaglandin D2The therapeutic efficacy of Prostaglandin D2 can be decreased when used in combination with Valdecoxib.
Protein CValdecoxib may increase the anticoagulant activities of Protein C.
ProtocatechualdehydeValdecoxib may increase the anticoagulant activities of Protocatechualdehyde.
PTC299The risk or severity of adverse effects can be increased when Valdecoxib is combined with PTC299.
PuromycinValdecoxib may decrease the excretion rate of Puromycin which could result in a lower serum level and potentially a reduction in efficacy.
PyrimethamineThe metabolism of Valdecoxib can be decreased when combined with Pyrimethamine.
QuinaprilThe risk or severity of adverse effects can be increased when Quinapril is combined with Valdecoxib.
QuinethazoneThe therapeutic efficacy of Quinethazone can be decreased when used in combination with Valdecoxib.
QuinineThe metabolism of Valdecoxib can be decreased when combined with Quinine.
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Valdecoxib.
RanolazineThe metabolism of Valdecoxib can be decreased when combined with Ranolazine.
RescinnamineThe risk or severity of adverse effects can be increased when Rescinnamine is combined with Valdecoxib.
ResveratrolThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Resveratrol.
ReviparinValdecoxib may increase the anticoagulant activities of Reviparin.
RibostamycinValdecoxib may decrease the excretion rate of Ribostamycin which could result in a lower serum level and potentially a reduction in efficacy.
RifabutinThe metabolism of Valdecoxib can be increased when combined with Rifabutin.
RifampicinThe metabolism of Valdecoxib can be increased when combined with Rifampicin.
RifapentineThe metabolism of Valdecoxib can be increased when combined with Rifapentine.
RisedronateThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Risedronate.
RitonavirThe metabolism of Valdecoxib can be decreased when combined with Ritonavir.
RivaroxabanValdecoxib may increase the anticoagulant activities of Rivaroxaban.
RofecoxibThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Valdecoxib.
SalicylamideThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Salicylamide.
Salicylic acidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Salicylic acid.
SalsalateThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Salsalate.
SaprisartanThe risk or severity of adverse effects can be increased when Saprisartan is combined with Valdecoxib.
SaquinavirThe metabolism of Valdecoxib can be decreased when combined with Saquinavir.
SaralasinThe risk or severity of adverse effects can be increased when Saralasin is combined with Valdecoxib.
SecobarbitalThe metabolism of Valdecoxib can be increased when combined with Secobarbital.
SeratrodastThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Seratrodast.
SildenafilThe metabolism of Valdecoxib can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Valdecoxib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Valdecoxib can be increased when it is combined with Simeprevir.
SorafenibThe metabolism of Valdecoxib can be decreased when combined with Sorafenib.
SotalolValdecoxib may decrease the antihypertensive activities of Sotalol.
SpectinomycinValdecoxib 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 Valdecoxib.
SpironolactoneValdecoxib may decrease the antihypertensive activities of Spironolactone.
SRT501The risk or severity of adverse effects can be increased when Valdecoxib is combined with SRT501.
St. John's WortThe serum concentration of Valdecoxib can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Valdecoxib can be increased when it is combined with Stiripentol.
StreptomycinValdecoxib may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
StreptozocinValdecoxib may decrease the excretion rate of Streptozocin which could result in a lower serum level and potentially a reduction in efficacy.
SulfadiazineThe metabolism of Valdecoxib can be decreased when combined with Sulfadiazine.
SulfamethoxazoleThe metabolism of Valdecoxib can be decreased when combined with Sulfamethoxazole.
SulfasalazineValdecoxib may increase the nephrotoxic activities of Sulfasalazine.
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Valdecoxib.
SulfisoxazoleThe metabolism of Valdecoxib can be decreased when combined with Sulfisoxazole.
SulindacThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Sulindac.
SulodexideValdecoxib may increase the anticoagulant activities of Sulodexide.
SuprofenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Suprofen.
TacrolimusValdecoxib may increase the nephrotoxic activities of Tacrolimus.
TalniflumateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Valdecoxib.
TasosartanThe risk or severity of adverse effects can be increased when Tasosartan is combined with Valdecoxib.
Technetium Tc-99m MedronateThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Technetium Tc-99m Medronate.
TelaprevirThe metabolism of Valdecoxib can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Valdecoxib can be decreased when combined with Telithromycin.
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Valdecoxib.
TemocaprilThe risk or severity of adverse effects can be increased when Temocapril is combined with Valdecoxib.
TenofovirThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Tenofovir.
TenoxicamThe risk or severity of adverse effects can be increased when Tenoxicam is combined with Valdecoxib.
TepoxalinThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Tepoxalin.
TeriflunomideThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Teriflunomide.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Tiaprofenic acid.
TicagrelorThe metabolism of Valdecoxib can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Valdecoxib can be decreased when combined with Ticlopidine.
TiludronateThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Tiludronate.
TimololValdecoxib may decrease the antihypertensive activities of Timolol.
TobramycinValdecoxib may decrease the excretion rate of Tobramycin which could result in a lower serum level and potentially a reduction in efficacy.
TocilizumabThe serum concentration of Valdecoxib can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Valdecoxib can be decreased when combined with Tolbutamide.
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Tolfenamic Acid.
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Valdecoxib.
TorasemideValdecoxib may decrease the diuretic activities of Torasemide.
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Valdecoxib.
TranilastThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Tranilast.
TravoprostThe therapeutic efficacy of Travoprost can be decreased when used in combination with Valdecoxib.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Valdecoxib.
TriamtereneValdecoxib may decrease the antihypertensive activities of Triamterene.
TrichlormethiazideThe therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Valdecoxib.
TrimethoprimThe metabolism of Valdecoxib can be decreased when combined with Trimethoprim.
Trisalicylate-cholineThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Trisalicylate-choline.
Valproic AcidThe metabolism of Valdecoxib can be decreased when combined with Valproic Acid.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Valdecoxib.
VancomycinThe serum concentration of Vancomycin can be increased when it is combined with Valdecoxib.
VenlafaxineThe metabolism of Valdecoxib can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Valdecoxib can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Valdecoxib can be decreased when combined with Voriconazole.
WarfarinValdecoxib may increase the anticoagulant activities of Warfarin.
XimelagatranValdecoxib may increase the anticoagulant activities of Ximelagatran.
ZafirlukastThe metabolism of Valdecoxib can be decreased when combined with Zafirlukast.
ZaltoprofenThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Zaltoprofen.
ZileutonThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Zileuton.
ZiprasidoneThe metabolism of Valdecoxib can be decreased when combined with Ziprasidone.
Zoledronic acidThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Zoledronic acid.
ZomepiracThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Zomepirac.
Food InteractionsNot Available

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. Talley JJ, Brown DL, Carter JS, Graneto MJ, Koboldt CM, Masferrer JL, Perkins WE, Rogers RS, Shaffer AF, Zhang YY, Zweifel BS, Seibert K: 4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. J Med Chem. 2000 Mar 9;43(5):775-7. [PubMed:10715145 ]
  2. Jain KK: Evaluation of intravenous parecoxib for the relief of acute post-surgical pain. Expert Opin Investig Drugs. 2000 Nov;9(11):2717-23. [PubMed:11060833 ]
  3. Yuan JJ, Yang DC, Zhang JY, Bible R Jr, Karim A, Findlay JW: Disposition of a specific cyclooxygenase-2 inhibitor, valdecoxib, in human. Drug Metab Dispos. 2002 Sep;30(9):1013-21. [PubMed:12167567 ]
  4. Tacconelli S, Capone ML, Sciulli MG, Ricciotti E, Patrignani P: The biochemical selectivity of novel COX-2 inhibitors in whole blood assays of COX-isozyme activity. Curr Med Res Opin. 2002;18(8):503-11. [PubMed:12564662 ]
  5. Hood WF, Gierse JK, Isakson PC, Kiefer JR, Kurumbail RG, Seibert K, Monahan JB: Characterization of celecoxib and valdecoxib binding to cyclooxygenase. Mol Pharmacol. 2003 Apr;63(4):870-7. [PubMed:12644588 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. Gierse JK, Zhang Y, Hood WF, Walker MC, Trigg JS, Maziasz TJ, Koboldt CM, Muhammad JL, Zweifel BS, Masferrer JL, Isakson PC, Seibert K: Valdecoxib: assessment of cyclooxygenase-2 potency and selectivity. J Pharmacol Exp Ther. 2005 Mar;312(3):1206-12. Epub 2004 Oct 19. [PubMed:15494548 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. 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
inhibitor
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23