Identification

Name
Rofecoxib
Accession Number
DB00533  (APRD00151)
Type
Small Molecule
Groups
Investigational, Withdrawn
Description

Rofecoxib is used for the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras. Rofecoxib is a solid. This compound belongs to the stilbenes. These are organic compounds containing a 1,2-diphenylethylene moiety. Stilbenes (C6-C2-C6 ) are derived from the common phenylpropene (C6-C3) skeleton building block. The introduction of one or more hydroxyl groups to a phenyl ring lead to stilbenoids. Rofecoxib has a half-life of 17 hours and its mean oral bioavailability at therapeutically recommended doses of 125, 25, and 50 mg is approximately 93%. The proteins that rofecoxib target include elastin and prostaglandin G/H synthase 2. Cytochrome P450 1A2, Cytochrome P450 3A4, Cytochrome P450 2C9, Cytochrome P450 2C8, and Prostaglandin G/H synthase 1 are known to metabolize rofecoxib. On September 30, 2004, Merck voluntarily withdrew rofecoxib from the market because of concerns about increased risk of heart attack and stroke associated with long-term, high-dosage use.

Structure
Thumb
Synonyms
Not Available
External IDs
M01AH02 / MK 966 / MK 996 / MK-0966 / MK0966
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Vioxx Suspension 12.5mg/5mlSuspension12.5 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.2000-05-082004-09-30Canada
Vioxx Tab 12.5mgTablet12.5 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1999-11-082004-09-30Canada
Vioxx Tab 25mgTablet25 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1999-11-082004-09-30Canada
International/Other Brands
Vioxx
Categories
UNII
0QTW8Z7MCR
CAS number
162011-90-7
Weight
Average: 314.356
Monoisotopic: 314.061279626
Chemical Formula
C17H14O4S
InChI Key
RZJQGNCSTQAWON-UHFFFAOYSA-N
InChI
InChI=1S/C17H14O4S/c1-22(19,20)14-9-7-12(8-10-14)15-11-21-17(18)16(15)13-5-3-2-4-6-13/h2-10H,11H2,1H3
IUPAC Name
4-(4-methanesulfonylphenyl)-3-phenyl-2,5-dihydrofuran-2-one
SMILES
CS(=O)(=O)C1=CC=C(C=C1)C1=C(C(=O)OC1)C1=CC=CC=C1

Pharmacology

Indication

For the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras.

Structured Indications
Not Available
Pharmacodynamics

Rofecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Unlike celecoxib, rofecoxib lacks a sulfonamide chain and does not require CYP450 enzymes for metabolism. Like other NSAIDs, rofecoxib exhibits anti-inflammatory, analgesic, and antipyretic activity. NSAIDs appear to inhibit prostaglandin synthesis via the inhibition of cyclooxygenase (COX), which are responsible for catalyzing the formation of prostaglandins in the arachidonic acid pathyway. There are at least two isoenzymes, COX-1 and COX-2, that have been identified. Although the exact mechanisms have not been clearly established, NSAIDs exert their anti-inflammatory, analgesic, and antipyretic primarily through the inhibition of COX-2. The inhibition of COX-1 is principally responsible for the negative effects on the GI mucosa. As rofecoxib is selective for COX-2, it may be potentially associated with a decreased risk of certain adverse events, but more data is needed to fully evaulate the drug.

Mechanism of action

The anti-inflammatory, analgesic, and antipyretic effects of NSAIDs appear to result from the inhibition of prostaglandin synthesis. Although the exact mechanism of action has not been determined, these effects appear to be mediated through the inhibition of the COX-2 isoenzyme at the sites of inflammation with subsequent reduction in the synthesis of certain prostaglandins from their arachidonic acid precursors. Rofecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, which is important for the mediation of inflammation and pain. Unlike non-selective NSAIDs, rofecoxib does not inhibit platelet aggregation. It also has little to no affinity for COX-1.

TargetActionsOrganism
AProstaglandin G/H synthase 2
inhibitor
Human
UElastin
other/unknown
Human
Absorption

The mean oral bioavailability of rofecoxib at therapeutically recommended doses of 12.5, 25, and 50 mg is approximately 93%.

Volume of distribution
Not Available
Protein binding

87%

Metabolism

Hepatic. Metabolism of rofecoxib is primarily mediated through reduction by cytosolic enzymes. The principal metabolic products are the cis-dihydro and trans-dihydro derivatives of rofecoxib, which account for nearly 56% of recovered radioactivity in the urine. An additional 8.8% of the dose was recovered as the glucuronide of the hydroxy derivative, a product of oxidative metabolism. The biotransformation of rofecoxib and this metabolite is reversible in humans to a limited extent (< 5%). These metabolites are inactive as COX-1 or COX-2 inhibitors. Cytochrome P450 plays a minor role in metabolism of rofecoxib.

Route of elimination
Not Available
Half life

17 hours

Clearance
Not Available
Toxicity

No overdoses of rofecoxib were reported during clinical trials. Administration of single doses of rofecoxib 1000 mg to 6 healthy volunteers and multiple doses of 250 mg/day for 14 days to 75 healthy volunteers did not result in serious toxicity.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Rofecoxib Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
16-BromoepiandrosteroneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with 16-Bromoepiandrosterone.Investigational
19-norandrostenedioneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with 19-norandrostenedione.Experimental, Illicit
5-androstenedioneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with 5-androstenedione.Experimental, Illicit
AbciximabRofecoxib may increase the anticoagulant activities of Abciximab.Approved
AbirateroneThe serum concentration of Rofecoxib can be increased when it is combined with Abiraterone.Approved
AcebutololRofecoxib may decrease the antihypertensive activities of Acebutolol.Approved
AcenocoumarolRofecoxib may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Rofecoxib.Approved, Vet Approved
AclarubicinRofecoxib may decrease the excretion rate of Aclarubicin which could result in a higher serum level.Investigational
AlaproclateAlaproclate may increase the antiplatelet activities of Rofecoxib.Experimental
AlclometasoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Alclometasone.Approved
AldosteroneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Aldosterone.Experimental, Investigational
Alendronic acidThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Alendronic acid.Approved
AliskirenRofecoxib may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
AlprenololRofecoxib may decrease the antihypertensive activities of Alprenolol.Approved, Withdrawn
AlprostadilThe therapeutic efficacy of Alprostadil can be decreased when used in combination with Rofecoxib.Approved, Investigational
AmcinonideThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Amcinonide.Approved
AmikacinRofecoxib may decrease the excretion rate of Amikacin which could result in a higher serum level.Approved, Vet Approved
AmilorideRofecoxib may decrease the antihypertensive activities of Amiloride.Approved
AmiodaroneThe metabolism of Rofecoxib can be decreased when combined with Amiodarone.Approved, Investigational
AmrubicinRofecoxib may decrease the excretion rate of Amrubicin which could result in a higher serum level.Approved, Investigational
AncrodRofecoxib may increase the anticoagulant activities of Ancrod.Investigational
AndrostenedioneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Androstenedione.Experimental, Illicit
AnecortaveThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Anecortave.Investigational
anecortave acetateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with anecortave acetate.Investigational
annamycinRofecoxib may decrease the excretion rate of annamycin which could result in a higher serum level.Investigational
Antithrombin III humanRofecoxib may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanRofecoxib may increase the anticoagulant activities of Apixaban.Approved
ApramycinRofecoxib may decrease the excretion rate of Apramycin which could result in a higher serum level.Experimental, Vet Approved
AprepitantThe serum concentration of Rofecoxib can be increased when it is combined with Aprepitant.Approved, Investigational
ArbekacinRofecoxib may decrease the excretion rate of Arbekacin which could result in a higher serum level.Approved, Investigational
ArdeparinRofecoxib may increase the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
ArgatrobanRofecoxib may increase the anticoagulant activities of Argatroban.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Rofecoxib.Approved, Investigational
ArotinololRofecoxib may decrease the antihypertensive activities of Arotinolol.Approved, Investigational
AtamestaneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Atamestane.Investigational
AtazanavirThe metabolism of Rofecoxib can be decreased when combined with Atazanavir.Approved, Investigational
AtenololRofecoxib may decrease the antihypertensive activities of Atenolol.Approved
AtomoxetineThe metabolism of Rofecoxib can be decreased when combined with Atomoxetine.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Rofecoxib.Approved
AzithromycinThe metabolism of Rofecoxib can be decreased when combined with Azithromycin.Approved
BalsalazideRofecoxib may increase the nephrotoxic activities of Balsalazide.Approved, Investigational
BecaplerminRofecoxib may increase the anticoagulant activities of Becaplermin.Approved, Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Beclomethasone dipropionate.Approved, Investigational
BefunololRofecoxib may decrease the antihypertensive activities of Befunolol.Experimental
BekanamycinRofecoxib may decrease the excretion rate of Bekanamycin which could result in a higher serum level.Experimental
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Rofecoxib.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Bendroflumethiazide can be decreased when used in combination with Rofecoxib.Approved
BeraprostThe therapeutic efficacy of Beraprost can be decreased when used in combination with Rofecoxib.Investigational
BetamethasoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Betamethasone.Approved, Vet Approved
BetaxololRofecoxib may decrease the antihypertensive activities of Betaxolol.Approved
BevantololRofecoxib may decrease the antihypertensive activities of Bevantolol.Approved
BimatoprostThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Rofecoxib.Approved, Investigational
BisoprololRofecoxib may decrease the antihypertensive activities of Bisoprolol.Approved
BivalirudinRofecoxib may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BoceprevirThe metabolism of Rofecoxib can be decreased when combined with Boceprevir.Approved, Withdrawn
BopindololRofecoxib may decrease the antihypertensive activities of Bopindolol.Approved
BortezomibThe metabolism of Rofecoxib can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Rofecoxib can be decreased when it is combined with Bosentan.Approved, Investigational
BucindololRofecoxib may decrease the antihypertensive activities of Bucindolol.Investigational
BudesonideThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Budesonide.Approved
BufuralolRofecoxib may decrease the antihypertensive activities of Bufuralol.Experimental, Investigational
BumetanideRofecoxib may decrease the diuretic activities of Bumetanide.Approved
BupranololRofecoxib may decrease the antihypertensive activities of Bupranolol.Approved
CaffeineThe metabolism of Rofecoxib can be decreased when combined with Caffeine.Approved
Candesartan cilexetilThe risk or severity of adverse effects can be increased when Candesartan is combined with Rofecoxib.Approved
CandoxatrilThe risk or severity of adverse effects can be increased when Candoxatril is combined with Rofecoxib.Experimental
CapecitabineThe metabolism of Rofecoxib can be decreased when combined with Capecitabine.Approved, Investigational
CaptoprilThe risk or severity of adverse effects can be increased when Captopril is combined with Rofecoxib.Approved
CarbamazepineThe metabolism of Rofecoxib can be increased when combined with Carbamazepine.Approved, Investigational
Carboprost TromethamineThe therapeutic efficacy of Carboprost Tromethamine can be decreased when used in combination with Rofecoxib.Approved
CarteololRofecoxib may decrease the antihypertensive activities of Carteolol.Approved
CarvedilolRofecoxib may decrease the antihypertensive activities of Carvedilol.Approved, Investigational
CelecoxibThe metabolism of Rofecoxib can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololRofecoxib may decrease the antihypertensive activities of Celiprolol.Approved, Investigational
CeritinibThe serum concentration of Rofecoxib can be increased when it is combined with Ceritinib.Approved
CertoparinRofecoxib may increase the anticoagulant activities of Certoparin.Approved, Investigational
ChlorothiazideThe therapeutic efficacy of Chlorothiazide can be decreased when used in combination with Rofecoxib.Approved, Vet Approved
ChlorotrianiseneRofecoxib may increase the thrombogenic activities of Chlorotrianisene.Investigational, Withdrawn
ChlorthalidoneThe therapeutic efficacy of Chlorthalidone can be decreased when used in combination with Rofecoxib.Approved
CholecalciferolThe metabolism of Rofecoxib can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholestyramineCholestyramine can cause a decrease in the absorption of Rofecoxib resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CiclesonideThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Ciclesonide.Approved, Investigational
CilazaprilThe risk or severity of adverse effects can be increased when Cilazapril is combined with Rofecoxib.Approved
CinoxacinRofecoxib may increase the neuroexcitatory activities of Cinoxacin.Approved, Investigational, Withdrawn
CitalopramCitalopram may increase the antiplatelet activities of Rofecoxib.Approved
Citric AcidRofecoxib may increase the anticoagulant activities of Citric Acid.Approved, Nutraceutical, Vet Approved
ClarithromycinThe metabolism of Rofecoxib can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Rofecoxib can be decreased when combined with Clemastine.Approved
ClobetasolThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Clobetasol.Investigational
Clobetasol propionateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Clobetasol propionate.Approved
ClobetasoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Clobetasone.Approved
ClocortoloneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Clocortolone.Approved
Clodronic AcidThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Clodronic Acid.Approved, Investigational, Vet Approved
CloprostenolThe therapeutic efficacy of Cloprostenol can be decreased when used in combination with Rofecoxib.Vet Approved
CloranololRofecoxib may decrease the antihypertensive activities of Cloranolol.Experimental
ClorindioneRofecoxib may increase the anticoagulant activities of Clorindione.Experimental
ClotrimazoleThe metabolism of Rofecoxib can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Rofecoxib can be decreased when combined with Cobicistat.Approved
ColesevelamColesevelam can cause a decrease in the absorption of Rofecoxib resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ColestipolColestipol can cause a decrease in the absorption of Rofecoxib resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ConivaptanThe serum concentration of Rofecoxib can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated estrogensRofecoxib may increase the thrombogenic activities of Conjugated estrogens.Approved
Cortexolone 17α-propionateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Cortexolone 17α-propionate.Investigational
CorticosteroneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Corticosterone.Experimental
Cortisone acetateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Cortisone acetate.Approved
CrisaboroleThe metabolism of Rofecoxib can be decreased when combined with Crisaborole.Approved
CrizotinibThe metabolism of Rofecoxib can be decreased when combined with Crizotinib.Approved
CyclopenthiazideThe therapeutic efficacy of Cyclopenthiazide can be decreased when used in combination with Rofecoxib.Experimental
CyclosporineRofecoxib may increase the nephrotoxic activities of Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Rofecoxib can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateRofecoxib may increase the anticoagulant activities of Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Rofecoxib can be decreased when it is combined with Dabrafenib.Approved
DaidzeinRofecoxib may increase the thrombogenic activities of Daidzein.Experimental
DalteparinRofecoxib may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidRofecoxib may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DapoxetineDapoxetine may increase the antiplatelet activities of Rofecoxib.Investigational
DarexabanRofecoxib may increase the anticoagulant activities of Darexaban.Investigational
DarunavirThe metabolism of Rofecoxib can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Rofecoxib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinRofecoxib may decrease the excretion rate of Daunorubicin which could result in a higher serum level.Approved
DeferasiroxThe serum concentration of Rofecoxib can be decreased when it is combined with Deferasirox.Approved, Investigational
DelaprilThe risk or severity of adverse effects can be increased when Delapril is combined with Rofecoxib.Experimental
DelavirdineThe metabolism of Rofecoxib can be decreased when combined with Delavirdine.Approved
DesirudinRofecoxib may increase the anticoagulant activities of Desirudin.Approved
DesmopressinThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Desmopressin.Approved
DesoximetasoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Desoximetasone.Approved
Desoxycorticosterone acetateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Desoxycorticosterone acetate.Approved
Desoxycorticosterone PivalateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Desoxycorticosterone Pivalate.Experimental, Vet Approved
DesvenlafaxineDesvenlafaxine may increase the antiplatelet activities of Rofecoxib.Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Dexamethasone.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Dexamethasone isonicotinate.Vet Approved
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Rofecoxib.Approved, Investigational
DextranRofecoxib may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Rofecoxib may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Rofecoxib may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Rofecoxib may increase the anticoagulant activities of Dextran 75.Approved
DibekacinRofecoxib may decrease the excretion rate of Dibekacin which could result in a higher serum level.Experimental
DicoumarolRofecoxib may increase the anticoagulant activities of Dicoumarol.Approved
DienestrolRofecoxib may increase the thrombogenic activities of Dienestrol.Approved, Investigational
DiethylstilbestrolRofecoxib may increase the thrombogenic activities of Diethylstilbestrol.Approved, Investigational
DiflorasoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Diflorasone.Approved
DifluocortoloneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Difluocortolone.Approved, Investigational
DifluprednateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Difluprednate.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Rofecoxib.Approved
DihydroergotamineThe metabolism of Rofecoxib can be decreased when combined with Dihydroergotamine.Approved
DihydrostreptomycinRofecoxib may decrease the excretion rate of Dihydrostreptomycin which could result in a higher serum level.Investigational, Vet Approved
DiltiazemThe metabolism of Rofecoxib can be decreased when combined with Diltiazem.Approved
DinoprostThe therapeutic efficacy of Dinoprost can be decreased when used in combination with Rofecoxib.Investigational
Dinoprost TromethamineThe therapeutic efficacy of Dinoprost Tromethamine can be decreased when used in combination with Rofecoxib.Approved, Vet Approved
DinoprostoneThe therapeutic efficacy of Dinoprostone can be decreased when used in combination with Rofecoxib.Approved
DiphenadioneRofecoxib may increase the anticoagulant activities of Diphenadione.Experimental
DosulepinThe metabolism of Rofecoxib can be decreased when combined with Dosulepin.Approved
DoxorubicinRofecoxib may decrease the excretion rate of Doxorubicin which could result in a higher serum level.Approved, Investigational
DoxycyclineThe metabolism of Rofecoxib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Rofecoxib can be decreased when combined with Dronedarone.Approved
DrospirenoneRofecoxib may increase the hyperkalemic activities of Drospirenone.Approved
DuloxetineDuloxetine may increase the antiplatelet activities of Rofecoxib.Approved
Edetic AcidRofecoxib may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanRofecoxib may increase the anticoagulant activities of Edoxaban.Approved
EfavirenzThe metabolism of Rofecoxib can be decreased when combined with Efavirenz.Approved, Investigational
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Rofecoxib.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Enalaprilat is combined with Rofecoxib.Approved
EnoxacinRofecoxib may increase the neuroexcitatory activities of Enoxacin.Approved, Investigational
EnoxaparinRofecoxib may increase the anticoagulant activities of Enoxaparin.Approved
EnprostilThe therapeutic efficacy of Enprostil can be decreased when used in combination with Rofecoxib.Experimental
EnzalutamideThe serum concentration of Rofecoxib can be decreased when it is combined with Enzalutamide.Approved
EpanololRofecoxib may decrease the antihypertensive activities of Epanolol.Experimental
EpimestrolRofecoxib may increase the thrombogenic activities of Epimestrol.Experimental
EpirubicinRofecoxib may decrease the excretion rate of Epirubicin which could result in a higher serum level.Approved
EplerenoneRofecoxib may decrease the antihypertensive activities of Eplerenone.Approved
EpoprostenolThe therapeutic efficacy of Epoprostenol can be decreased when used in combination with Rofecoxib.Approved
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Rofecoxib.Approved
EquileninThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Equilenin.Experimental
EquilinThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Equilin.Approved
EquolRofecoxib may increase the thrombogenic activities of Equol.Investigational
ErythromycinThe metabolism of Rofecoxib can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramEscitalopram may increase the antiplatelet activities of Rofecoxib.Approved, Investigational
EsmololRofecoxib may decrease the antihypertensive activities of Esmolol.Approved
EstradiolRofecoxib may increase the thrombogenic activities of Estradiol.Approved, Investigational, Vet Approved
EstriolRofecoxib may increase the thrombogenic activities of Estriol.Approved, Investigational, Vet Approved
EstroneRofecoxib may increase the thrombogenic activities of Estrone.Approved
Estrone sulfateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Estrone sulfate.Approved
Etacrynic acidRofecoxib may decrease the diuretic activities of Etacrynic acid.Approved
Ethinyl EstradiolRofecoxib may increase the thrombogenic activities of Ethinyl Estradiol.Approved
Ethyl biscoumacetateRofecoxib may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Etidronic acidThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Etidronic acid.Approved
EtoperidoneEtoperidone may increase the antiplatelet activities of Rofecoxib.Withdrawn
EtravirineThe metabolism of Rofecoxib can be decreased when combined with Etravirine.Approved
FelodipineThe metabolism of Rofecoxib can be decreased when combined with Felodipine.Approved, Investigational
FenprostaleneThe therapeutic efficacy of Fenprostalene can be decreased when used in combination with Rofecoxib.Vet Approved
Ferulic acidRofecoxib may increase the anticoagulant activities of Ferulic acid.Experimental
FimasartanThe risk or severity of adverse effects can be increased when Fimasartan is combined with Rofecoxib.Approved, Investigational
FleroxacinRofecoxib may increase the neuroexcitatory activities of Fleroxacin.Approved
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Rofecoxib.Approved, Withdrawn
FloxuridineThe metabolism of Rofecoxib can be decreased when combined with Floxuridine.Approved
fluasteroneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with fluasterone.Investigational
FluconazoleThe metabolism of Rofecoxib can be decreased when combined with Fluconazole.Approved
FludrocortisoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Fludrocortisone.Approved
FluindioneRofecoxib may increase the anticoagulant activities of Fluindione.Investigational
FlumequineRofecoxib may increase the neuroexcitatory activities of Flumequine.Withdrawn
FlumethasoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Flumethasone.Approved, Vet Approved
Fluocinolone AcetonideThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Fluocinolone Acetonide.Approved, Investigational, Vet Approved
FluocinonideThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Fluocinonide.Approved, Investigational
FluocortoloneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Fluocortolone.Approved, Withdrawn
FluorometholoneThe risk or severity of adverse effects can be increased when Fluorometholone is combined with Rofecoxib.Approved
FluorouracilThe metabolism of Rofecoxib can be decreased when combined with Fluorouracil.Approved
FluoxetineFluoxetine may increase the antiplatelet activities of Rofecoxib.Approved, Vet Approved
FluprednideneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Fluprednidene.Approved, Withdrawn
FluprednisoloneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Fluprednisolone.Approved
FluprostenolThe therapeutic efficacy of Fluprostenol can be decreased when used in combination with Rofecoxib.Vet Approved
FlurandrenolideThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Flurandrenolide.Approved
FluvastatinThe metabolism of Rofecoxib can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Rofecoxib can be decreased when combined with Fluvoxamine.Approved, Investigational
Folic AcidThe therapeutic efficacy of Folic Acid can be decreased when used in combination with Rofecoxib.Approved, Nutraceutical, Vet Approved
FondaparinuxRofecoxib may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumRofecoxib may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
ForasartanThe risk or severity of adverse effects can be increased when Forasartan is combined with Rofecoxib.Experimental
FormestaneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Formestane.Approved, Investigational, Withdrawn
FosamprenavirThe metabolism of Rofecoxib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Rofecoxib can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Rofecoxib.Approved
FosphenytoinThe metabolism of Rofecoxib can be increased when combined with Fosphenytoin.Approved
FramycetinRofecoxib may decrease the excretion rate of Framycetin which could result in a higher serum level.Approved
FurosemideRofecoxib may decrease the diuretic activities of Furosemide.Approved, Vet Approved
Fusidic AcidThe serum concentration of Rofecoxib can be increased when it is combined with Fusidic Acid.Approved
GabexateRofecoxib may increase the anticoagulant activities of Gabexate.Investigational
GarenoxacinRofecoxib may increase the neuroexcitatory activities of Garenoxacin.Investigational
GatifloxacinRofecoxib may increase the neuroexcitatory activities of Gatifloxacin.Approved, Investigational
GemeprostThe therapeutic efficacy of Gemeprost can be decreased when used in combination with Rofecoxib.Approved, Withdrawn
GemfibrozilThe metabolism of Rofecoxib can be decreased when combined with Gemfibrozil.Approved
GemifloxacinRofecoxib may increase the neuroexcitatory activities of Gemifloxacin.Approved, Investigational
GeneticinRofecoxib may decrease the excretion rate of Geneticin which could result in a higher serum level.Experimental
GenisteinRofecoxib may increase the thrombogenic activities of Genistein.Investigational
GentamicinRofecoxib may decrease the excretion rate of Gentamicin which could result in a higher serum level.Approved, Vet Approved
GENTAMICIN C1ARofecoxib may decrease the excretion rate of GENTAMICIN C1A which could result in a higher serum level.Experimental
GPX-150Rofecoxib may decrease the excretion rate of GPX-150 which could result in a higher serum level.Investigational
GrepafloxacinRofecoxib may increase the neuroexcitatory activities of Grepafloxacin.Investigational, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Haloperidol.Approved
HE3286The risk or severity of adverse effects can be increased when Rofecoxib is combined with HE3286.Investigational
HeparinRofecoxib may increase the anticoagulant activities of Heparin.Approved, Investigational
HexestrolRofecoxib may increase the thrombogenic activities of Hexestrol.Withdrawn
HydralazineRofecoxib may decrease the antihypertensive activities of Hydralazine.Approved
HydrochlorothiazideThe therapeutic efficacy of Hydrochlorothiazide can be decreased when used in combination with Rofecoxib.Approved, Vet Approved
HydrocortisoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Hydroflumethiazide can be decreased when used in combination with Rofecoxib.Approved, Investigational
Hygromycin BRofecoxib may decrease the excretion rate of Hygromycin B which could result in a higher serum level.Vet Approved
IbandronateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Ibandronate.Approved, Investigational
IdarubicinRofecoxib may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
IdelalisibThe serum concentration of Rofecoxib can be increased when it is combined with Idelalisib.Approved
IdraparinuxRofecoxib may increase the anticoagulant activities of Idraparinux.Investigational
IloprostThe therapeutic efficacy of Iloprost can be decreased when used in combination with Rofecoxib.Approved, Investigational
ImatinibThe metabolism of Rofecoxib can be decreased when combined with Imatinib.Approved
ImidaprilThe risk or severity of adverse effects can be increased when Imidapril is combined with Rofecoxib.Investigational
IndalpineIndalpine may increase the antiplatelet activities of Rofecoxib.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Indapamide can be decreased when used in combination with Rofecoxib.Approved
IndenololRofecoxib may decrease the antihypertensive activities of Indenolol.Withdrawn
IndinavirThe metabolism of Rofecoxib can be decreased when combined with Indinavir.Approved
INNO-206Rofecoxib may decrease the excretion rate of INNO-206 which could result in a higher serum level.Investigational
IrbesartanThe metabolism of Rofecoxib can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Rofecoxib can be decreased when combined with Isavuconazonium.Approved, Investigational
IsepamicinRofecoxib may decrease the excretion rate of Isepamicin which could result in a higher serum level.Experimental
IsradipineThe metabolism of Rofecoxib can be decreased when combined with Isradipine.Approved
IstaroximeThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Istaroxime.Investigational
ItraconazoleThe metabolism of Rofecoxib can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Rofecoxib can be increased when it is combined with Ivacaftor.Approved
KanamycinRofecoxib may decrease the excretion rate of Kanamycin which could result in a higher serum level.Approved, Investigational, Vet Approved
KetoconazoleThe metabolism of Rofecoxib can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolRofecoxib may decrease the antihypertensive activities of Labetalol.Approved
LandiololRofecoxib may decrease the antihypertensive activities of Landiolol.Investigational
LapatinibThe metabolism of Rofecoxib can be decreased when combined with Lapatinib.Approved, Investigational
LatanoprostThe therapeutic efficacy of Latanoprost can be decreased when used in combination with Rofecoxib.Approved, Investigational
Latanoprostene BunodThe therapeutic efficacy of Latanoprostene Bunod can be decreased when used in combination with Rofecoxib.Investigational
LeflunomideThe metabolism of Rofecoxib can be decreased when combined with Leflunomide.Approved, Investigational
LepirudinRofecoxib may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanRofecoxib may increase the anticoagulant activities of Letaxaban.Investigational
LevobunololRofecoxib may decrease the antihypertensive activities of Levobunolol.Approved
LevofloxacinRofecoxib may increase the neuroexcitatory activities of Levofloxacin.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the antiplatelet activities of Rofecoxib.Approved
LidocaineThe metabolism of Rofecoxib can be decreased when combined with Lidocaine.Approved, Vet Approved
LimaprostThe therapeutic efficacy of Limaprost can be decreased when used in combination with Rofecoxib.Approved, Investigational
LisinoprilThe risk or severity of adverse effects can be increased when Lisinopril is combined with Rofecoxib.Approved, Investigational
LithiumThe serum concentration of Lithium can be increased when it is combined with Rofecoxib.Approved
LobeglitazoneThe metabolism of Rofecoxib can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe metabolism of Rofecoxib can be decreased when combined with Lopinavir.Approved
LosartanThe metabolism of Rofecoxib can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Rofecoxib can be decreased when combined with Lovastatin.Approved, Investigational
LubiprostoneThe therapeutic efficacy of Lubiprostone can be decreased when used in combination with Rofecoxib.Approved, Investigational
LuliconazoleThe serum concentration of Rofecoxib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Rofecoxib can be increased when it is combined with Lumacaftor.Approved
LuprostiolThe therapeutic efficacy of Luprostiol can be decreased when used in combination with Rofecoxib.Vet Approved
ManidipineThe metabolism of Rofecoxib can be decreased when combined with Manidipine.Approved, Investigational
ME-609The risk or severity of adverse effects can be increased when Rofecoxib is combined with ME-609.Investigational
MedrysoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Medrysone.Approved
MelagatranRofecoxib may increase the anticoagulant activities of Melagatran.Experimental
MelengestrolThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Melengestrol.Vet Approved
MepindololRofecoxib may decrease the antihypertensive activities of Mepindolol.Experimental
MesalazineRofecoxib may increase the nephrotoxic activities of Mesalazine.Approved
MestranolRofecoxib may increase the thrombogenic activities of Mestranol.Approved
MethallenestrilRofecoxib may increase the thrombogenic activities of Methallenestril.Experimental
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Rofecoxib.Approved
MethyclothiazideThe therapeutic efficacy of Methyclothiazide can be decreased when used in combination with Rofecoxib.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Methylprednisolone.Approved, Vet Approved
MetipranololRofecoxib may decrease the antihypertensive activities of Metipranolol.Approved
MetolazoneThe therapeutic efficacy of Metolazone can be decreased when used in combination with Rofecoxib.Approved
MetoprololRofecoxib may decrease the antihypertensive activities of Metoprolol.Approved, Investigational
MetrizamideRofecoxib may decrease the excretion rate of Metrizamide which could result in a higher serum level.Approved
MexiletineThe metabolism of Rofecoxib can be decreased when combined with Mexiletine.Approved
MicronomicinRofecoxib may decrease the excretion rate of Micronomicin which could result in a higher serum level.Experimental
MidostaurinThe metabolism of Rofecoxib can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Rofecoxib can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the antiplatelet activities of Rofecoxib.Approved
MisoprostolThe therapeutic efficacy of Misoprostol can be decreased when used in combination with Rofecoxib.Approved
MitotaneThe serum concentration of Rofecoxib can be decreased when it is combined with Mitotane.Approved
MoexiprilThe risk or severity of adverse effects can be increased when Moexipril is combined with Rofecoxib.Approved
MorniflumateThe risk or severity of adverse effects can be increased when Morniflumate is combined with Rofecoxib.Approved
MoxestrolRofecoxib may increase the thrombogenic activities of Moxestrol.Experimental
NadololRofecoxib may decrease the antihypertensive activities of Nadolol.Approved
NadroparinRofecoxib may increase the anticoagulant activities of Nadroparin.Approved
NafamostatRofecoxib may increase the anticoagulant activities of Nafamostat.Approved, Investigational
Nalidixic AcidRofecoxib may increase the neuroexcitatory activities of Nalidixic Acid.Approved, Investigational
NCX 1022The risk or severity of adverse effects can be increased when Rofecoxib is combined with NCX 1022.Investigational
NeamineRofecoxib may decrease the excretion rate of Neamine which could result in a higher serum level.Experimental
NefazodoneThe metabolism of Rofecoxib can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Rofecoxib can be decreased when combined with Nelfinavir.Approved
NemonoxacinRofecoxib may increase the neuroexcitatory activities of Nemonoxacin.Investigational
NeomycinRofecoxib may decrease the excretion rate of Neomycin which could result in a higher serum level.Approved, Vet Approved
NetilmicinRofecoxib may decrease the excretion rate of Netilmicin which could result in a higher serum level.Approved, Investigational
NetupitantThe serum concentration of Rofecoxib can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Rofecoxib can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Rofecoxib can be decreased when combined with Nicardipine.Approved
NilotinibThe metabolism of Rofecoxib can be decreased when combined with Nilotinib.Approved, Investigational
NorfloxacinRofecoxib may increase the neuroexcitatory activities of Norfloxacin.Approved
OlaparibThe metabolism of Rofecoxib can be decreased when combined with Olaparib.Approved
Oleoyl-estroneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Oleoyl-estrone.Investigational
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Rofecoxib.Approved, Investigational
OlsalazineRofecoxib may increase the nephrotoxic activities of Olsalazine.Approved
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Omacetaxine mepesuccinate.Approved
OmapatrilatThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Rofecoxib.Investigational
OmeprazoleThe metabolism of Rofecoxib can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Rofecoxib can be increased when it is combined with Osimertinib.Approved
OtamixabanRofecoxib may increase the anticoagulant activities of Otamixaban.Investigational
Oxolinic acidRofecoxib may increase the neuroexcitatory activities of Oxolinic acid.Experimental
OxprenololRofecoxib may decrease the antihypertensive activities of Oxprenolol.Approved
PalbociclibThe serum concentration of Rofecoxib can be increased when it is combined with Palbociclib.Approved
PamidronateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Pamidronate.Approved
ParamethasoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Paramethasone.Approved
ParomomycinRofecoxib may decrease the excretion rate of Paromomycin which could result in a higher serum level.Approved, Investigational
ParoxetineParoxetine may increase the antiplatelet activities of Rofecoxib.Approved, Investigational
PazufloxacinRofecoxib may increase the neuroexcitatory activities of Pazufloxacin.Investigational
PefloxacinRofecoxib may increase the neuroexcitatory activities of Pefloxacin.Approved
Peginterferon alfa-2bThe serum concentration of Rofecoxib can be increased when it is combined with Peginterferon alfa-2b.Approved
PenbutololRofecoxib may decrease the antihypertensive activities of Penbutolol.Approved, Investigational
PentobarbitalThe metabolism of Rofecoxib can be increased when combined with Pentobarbital.Approved, Vet Approved
Pentosan PolysulfateRofecoxib may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Rofecoxib.Approved
PhenindioneRofecoxib may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenobarbitalThe metabolism of Rofecoxib can be increased when combined with Phenobarbital.Approved
PhenprocoumonRofecoxib may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenytoinThe metabolism of Rofecoxib can be increased when combined with Phenytoin.Approved, Vet Approved
PindololRofecoxib may decrease the antihypertensive activities of Pindolol.Approved
PioglitazoneThe metabolism of Rofecoxib can be decreased when combined with Pioglitazone.Approved, Investigational
Pipemidic acidRofecoxib may increase the neuroexcitatory activities of Pipemidic acid.Experimental
PirarubicinRofecoxib may decrease the excretion rate of Pirarubicin which could result in a higher serum level.Investigational
PiretanideRofecoxib may decrease the diuretic activities of Piretanide.Experimental
Piromidic acidRofecoxib may increase the neuroexcitatory activities of Piromidic acid.Experimental
PlazomicinRofecoxib may decrease the excretion rate of Plazomicin which could result in a higher serum level.Investigational
PlicamycinRofecoxib may decrease the excretion rate of Plicamycin which could result in a higher serum level.Approved, Investigational, Withdrawn
Polyestradiol phosphateRofecoxib may increase the thrombogenic activities of Polyestradiol phosphate.Approved
PolythiazideThe therapeutic efficacy of Polythiazide can be decreased when used in combination with Rofecoxib.Approved
PosaconazoleThe metabolism of Rofecoxib can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PractololRofecoxib may decrease the antihypertensive activities of Practolol.Approved
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Rofecoxib.Approved
PrasteroneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Prasterone.Approved, Nutraceutical
Prasterone sulfateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Prasterone sulfate.Investigational
PrednicarbateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Prednicarbate.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Prednisone.Approved, Vet Approved
PregnenoloneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Pregnenolone.Experimental, Investigational
PrimidoneThe metabolism of Rofecoxib can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Rofecoxib can be increased when it is combined with Probenecid.Approved
PromestrieneRofecoxib may increase the thrombogenic activities of Promestriene.Investigational
PropranololRofecoxib may decrease the antihypertensive activities of Propranolol.Approved, Investigational
Prostaglandin B2The therapeutic efficacy of Prostaglandin B2 can be decreased when used in combination with Rofecoxib.Experimental
Prostaglandin G2The therapeutic efficacy of Prostaglandin G2 can be decreased when used in combination with Rofecoxib.Experimental
ProstaleneThe therapeutic efficacy of Prostalene can be decreased when used in combination with Rofecoxib.Vet Approved
Protein CRofecoxib may increase the anticoagulant activities of Protein C.Approved
Protein S humanRofecoxib may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeRofecoxib may increase the anticoagulant activities of Protocatechualdehyde.Approved
PrulifloxacinRofecoxib may increase the neuroexcitatory activities of Prulifloxacin.Investigational
PuromycinRofecoxib may decrease the excretion rate of Puromycin which could result in a higher serum level.Experimental
PyrimethamineThe metabolism of Rofecoxib can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuinaprilThe risk or severity of adverse effects can be increased when Quinapril is combined with Rofecoxib.Approved, Investigational
QuinestrolRofecoxib may increase the thrombogenic activities of Quinestrol.Approved
QuinethazoneThe therapeutic efficacy of Quinethazone can be decreased when used in combination with Rofecoxib.Approved
QuinineThe metabolism of Rofecoxib can be decreased when combined with Quinine.Approved
RabeprazoleThe metabolism of Rofecoxib can be decreased when combined with Rabeprazole.Approved, Investigational
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Rofecoxib.Approved
RanolazineThe metabolism of Rofecoxib can be decreased when combined with Ranolazine.Approved, Investigational
RescinnamineThe risk or severity of adverse effects can be increased when Rescinnamine is combined with Rofecoxib.Approved
ReviparinRofecoxib may increase the anticoagulant activities of Reviparin.Approved, Investigational
RibostamycinRofecoxib may decrease the excretion rate of Ribostamycin which could result in a higher serum level.Approved, Investigational
RifabutinThe metabolism of Rofecoxib can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Rofecoxib can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Rofecoxib can be increased when combined with Rifapentine.Approved
RimexoloneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Rimexolone.Approved
RisedronateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Risedronate.Approved, Investigational
RitonavirThe metabolism of Rofecoxib can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanRofecoxib may increase the anticoagulant activities of Rivaroxaban.Approved
RopiniroleThe metabolism of Rofecoxib can be decreased when combined with Ropinirole.Approved, Investigational
RosiglitazoneThe metabolism of Rofecoxib can be decreased when combined with Rosiglitazone.Approved, Investigational
RosoxacinRofecoxib may increase the neuroexcitatory activities of Rosoxacin.Approved, Investigational
RufloxacinRofecoxib may increase the neuroexcitatory activities of Rufloxacin.Experimental
SabarubicinRofecoxib may decrease the excretion rate of Sabarubicin which could result in a higher serum level.Investigational
SacubitrilThe risk or severity of adverse effects can be increased when Sacubitril is combined with Rofecoxib.Approved
SaprisartanThe risk or severity of adverse effects can be increased when Saprisartan is combined with Rofecoxib.Experimental
SaquinavirThe metabolism of Rofecoxib can be decreased when combined with Saquinavir.Approved, Investigational
SaralasinThe risk or severity of adverse effects can be increased when Saralasin is combined with Rofecoxib.Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Rofecoxib.Approved
SecobarbitalThe metabolism of Rofecoxib can be increased when combined with Secobarbital.Approved, Vet Approved
SecoisolariciresinolRofecoxib may increase the thrombogenic activities of Secoisolariciresinol.Investigational
SertralineSertraline may increase the antiplatelet activities of Rofecoxib.Approved
SildenafilThe metabolism of Rofecoxib can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Rofecoxib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Rofecoxib can be increased when it is combined with Simeprevir.Approved
SisomicinRofecoxib may decrease the excretion rate of Sisomicin which could result in a higher serum level.Investigational
SitafloxacinRofecoxib may increase the neuroexcitatory activities of Sitafloxacin.Experimental, Investigational
Sodium phosphateSodium phosphate may increase the nephrotoxic activities of Rofecoxib.Approved
SorafenibThe metabolism of Rofecoxib can be decreased when combined with Sorafenib.Approved, Investigational
SotalolRofecoxib may decrease the antihypertensive activities of Sotalol.Approved
SP1049CRofecoxib may decrease the excretion rate of SP1049C which could result in a higher serum level.Investigational
SparfloxacinRofecoxib may increase the neuroexcitatory activities of Sparfloxacin.Approved, Investigational
SpectinomycinRofecoxib may decrease the excretion rate of Spectinomycin which could result in a higher serum level.Approved, Investigational, Vet Approved
SpiraprilThe risk or severity of adverse effects can be increased when Spirapril is combined with Rofecoxib.Approved
SpironolactoneRofecoxib may decrease the antihypertensive activities of Spironolactone.Approved
St. John's WortThe serum concentration of Rofecoxib can be decreased when it is combined with St. John&#39;s Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Rofecoxib can be increased when it is combined with Stiripentol.Approved
StreptomycinRofecoxib may decrease the excretion rate of Streptomycin which could result in a higher serum level.Approved, Vet Approved
StreptozocinRofecoxib may decrease the excretion rate of Streptozocin which could result in a higher serum level.Approved
SulfadiazineThe metabolism of Rofecoxib can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Rofecoxib can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Rofecoxib can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideRofecoxib may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SulprostoneThe therapeutic efficacy of Sulprostone can be decreased when used in combination with Rofecoxib.Investigational
Synthetic Conjugated Estrogens, ARofecoxib may increase the thrombogenic activities of Synthetic Conjugated Estrogens, A.Approved
Synthetic Conjugated Estrogens, BRofecoxib may increase the thrombogenic activities of Synthetic Conjugated Estrogens, B.Approved
TacrolimusRofecoxib may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
TafluprostThe therapeutic efficacy of Tafluprost can be decreased when used in combination with Rofecoxib.Approved
TalinololRofecoxib may decrease the antihypertensive activities of Talinolol.Investigational
TalniflumateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Rofecoxib.Approved
TamoxifenThe metabolism of Rofecoxib can be decreased when combined with Tamoxifen.Approved
TasosartanThe risk or severity of adverse effects can be increased when Tasosartan is combined with Rofecoxib.Approved
Technetium Tc-99m etidronateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Technetium Tc-99m etidronate.Approved
Technetium Tc-99m medronateThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Technetium Tc-99m medronate.Approved
TelaprevirThe metabolism of Rofecoxib can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Rofecoxib can be decreased when combined with Telithromycin.Approved
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Rofecoxib.Approved, Investigational
TemafloxacinRofecoxib may increase the neuroexcitatory activities of Temafloxacin.Withdrawn
TemocaprilThe risk or severity of adverse effects can be increased when Temocapril is combined with Rofecoxib.Experimental, Investigational
Tenofovir disoproxilThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Tenofovir disoproxil.Approved, Investigational
TeriflunomideThe serum concentration of Rofecoxib can be decreased when it is combined with Teriflunomide.Approved
TertatololRofecoxib may decrease the antihypertensive activities of Tertatolol.Experimental
TheophyllineThe metabolism of Rofecoxib can be decreased when combined with Theophylline.Approved
TiboloneRofecoxib may increase the thrombogenic activities of Tibolone.Approved, Investigational
TicagrelorThe metabolism of Rofecoxib can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Rofecoxib can be decreased when combined with Ticlopidine.Approved
Tiludronic acidThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Tiludronic acid.Approved, Investigational, Vet Approved
TimololRofecoxib may decrease the antihypertensive activities of Timolol.Approved
TioclomarolRofecoxib may increase the anticoagulant activities of Tioclomarol.Experimental
TixocortolThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Tixocortol.Approved
TobramycinRofecoxib may decrease the excretion rate of Tobramycin which could result in a higher serum level.Approved, Investigational
TocilizumabThe serum concentration of Rofecoxib can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Rofecoxib can be decreased when combined with Tolbutamide.Approved
TopiroxostatThe metabolism of Rofecoxib can be decreased when combined with Topiroxostat.Approved, Investigational
TorasemideRofecoxib may decrease the diuretic activities of Torasemide.Approved
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Rofecoxib.Approved
TravoprostThe therapeutic efficacy of Travoprost can be decreased when used in combination with Rofecoxib.Approved
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Rofecoxib.Approved, Investigational
TriamcinoloneThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Triamcinolone.Approved, Vet Approved
TriamtereneRofecoxib may decrease the antihypertensive activities of Triamterene.Approved
TrichlormethiazideThe therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Rofecoxib.Approved, Vet Approved
TrimethoprimThe metabolism of Rofecoxib can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrovafloxacinRofecoxib may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational, Withdrawn
TroxerutinRofecoxib may increase the anticoagulant activities of Troxerutin.Investigational
UnoprostoneThe therapeutic efficacy of Unoprostone can be decreased when used in combination with Rofecoxib.Approved
Valproic AcidThe metabolism of Rofecoxib can be decreased when combined with Valproic Acid.Approved, Investigational
ValrubicinRofecoxib may decrease the excretion rate of Valrubicin which could result in a higher serum level.Approved
ValsartanThe metabolism of Rofecoxib can be decreased when combined with Valsartan.Approved, Investigational
VancomycinThe serum concentration of Vancomycin can be increased when it is combined with Rofecoxib.Approved
VemurafenibThe serum concentration of Rofecoxib can be increased when it is combined with Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the antiplatelet activities of Rofecoxib.Approved
VerapamilThe metabolism of Rofecoxib can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Rofecoxib can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinRofecoxib may increase the anticoagulant activities of Warfarin.Approved
XimelagatranRofecoxib may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
ZafirlukastThe metabolism of Rofecoxib can be decreased when combined with Zafirlukast.Approved, Investigational
ZeranolRofecoxib may increase the thrombogenic activities of Zeranol.Vet Approved
ZimelidineZimelidine may increase the antiplatelet activities of Rofecoxib.Withdrawn
ZiprasidoneThe metabolism of Rofecoxib can be decreased when combined with Ziprasidone.Approved
ZofenoprilThe risk or severity of adverse effects can be increased when Zofenopril is combined with Rofecoxib.Experimental
Zoledronic acidThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Zoledronic acid.Approved
Zoptarelin doxorubicinRofecoxib may decrease the excretion rate of Zoptarelin doxorubicin which could result in a higher serum level.Investigational
ZorubicinRofecoxib may decrease the excretion rate of Zorubicin which could result in a higher serum level.Experimental
ZucapsaicinThe metabolism of Rofecoxib can be decreased when combined with Zucapsaicin.Approved
Food Interactions
Not Available

References

General References
  1. Bombardier C, Laine L, Reicin A, Shapiro D, Burgos-Vargas R, Davis B, Day R, Ferraz MB, Hawkey CJ, Hochberg MC, Kvien TK, Schnitzer TJ: Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. VIGOR Study Group. N Engl J Med. 2000 Nov 23;343(21):1520-8, 2 p following 1528. [PubMed:11087881]
  2. Bresalier RS, Sandler RS, Quan H, Bolognese JA, Oxenius B, Horgan K, Lines C, Riddell R, Morton D, Lanas A, Konstam MA, Baron JA: Cardiovascular events associated with rofecoxib in a colorectal adenoma chemoprevention trial. N Engl J Med. 2005 Mar 17;352(11):1092-102. Epub 2005 Feb 15. [PubMed:15713943]
  3. Curfman GD, Morrissey S, Drazen JM: Expression of concern reaffirmed. N Engl J Med. 2006 Mar 16;354(11):1193. Epub 2006 Feb 22. [PubMed:16495386]
  4. Fitzgerald GA: Coxibs and cardiovascular disease. N Engl J Med. 2004 Oct 21;351(17):1709-11. Epub 2004 Oct 6. [PubMed:15470192]
  5. Karha J, Topol EJ: The sad story of Vioxx, and what we should learn from it. Cleve Clin J Med. 2004 Dec;71(12):933-4, 936, 938-9. [PubMed:15641522]
  6. Baron JA, Sandler RS, Bresalier RS, Lanas A, Morton DG, Riddell R, Iverson ER, Demets DL: Cardiovascular events associated with rofecoxib: final analysis of the APPROVe trial. Lancet. 2008 Nov 15;372(9651):1756-64. doi: 10.1016/S0140-6736(08)61490-7. Epub 2008 Oct 14. [PubMed:18922570]
  7. Matheson AJ, Figgitt DP: Rofecoxib: a review of its use in the management of osteoarthritis, acute pain and rheumatoid arthritis. Drugs. 2001;61(6):833-65. [PubMed:11398914]
  8. Hillson JL, Furst DE: Rofecoxib. Expert Opin Pharmacother. 2000 Jul;1(5):1053-66. [PubMed:11249495]
External Links
KEGG Drug
D00568
KEGG Compound
C07590
PubChem Compound
5090
PubChem Substance
46504787
ChemSpider
4911
BindingDB
22369
ChEBI
8887
ChEMBL
CHEMBL122
Therapeutic Targets Database
DAP001338
PharmGKB
PA451268
HET
RCX
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Rofecoxib
ATC Codes
M01AH02 — Rofecoxib
PDB Entries
5kir
FDA label
Download (291 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1TerminatedTreatmentGliomas / Neoplasms, Brain1
2CompletedTreatmentPain1
2CompletedTreatmentPain / Tooth Extractions1
2, 3CompletedTreatmentAdvanced Non-Small Cell Lung Cancer1
2, 3CompletedTreatmentAlzheimer's Disease (AD)1
2, 3TerminatedTreatmentDuodenal Polyposis1
3CompletedPreventionProstate Cancer1
3CompletedTreatmentColorectal Cancers1
3CompletedTreatmentOsteoarthritis of the Knees1
3CompletedTreatmentPostoperative pain5
3CompletedTreatmentSynovitis of osteoarthritis3
3TerminatedTreatmentPain1
3Unknown StatusTreatmentCancer of Stomach2
4CompletedTreatmentAnalgesics1
4CompletedTreatmentEsophagus, Barrett1
4CompletedTreatmentRheumatoid Arthritis1
4TerminatedTreatmentPain1
4TerminatedTreatmentPain, Acute1
Not AvailableCompletedPreventionHeadaches1
Not AvailableCompletedTreatmentAntiphospholipid Antibody Syndrome1

Pharmacoeconomics

Manufacturers
  • Merck research laboratories div merck co inc
Packagers
Dosage forms
FormRouteStrength
SuspensionOral12.5 mg
TabletOral12.5 mg
TabletOral25 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5474995No1993-06-242013-06-24Us
US6063811Yes1997-11-062017-11-06Us
US5691374Yes1995-11-182015-11-18Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityInsolubleNot Available
logP3.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0106 mg/mLALOGPS
logP2.32ALOGPS
logP2.56ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)14.84ChemAxon
pKa (Strongest Basic)-7ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area60.44 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity84.08 m3·mol-1ChemAxon
Polarizability31.74 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9938
Blood Brain Barrier+0.6296
Caco-2 permeable-0.5696
P-glycoprotein substrateNon-substrate0.7186
P-glycoprotein inhibitor INon-inhibitor0.5401
P-glycoprotein inhibitor IINon-inhibitor0.922
Renal organic cation transporterNon-inhibitor0.7846
CYP450 2C9 substrateNon-substrate0.5807
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5941
CYP450 1A2 substrateInhibitor0.5426
CYP450 2C9 inhibitorInhibitor0.6668
CYP450 2D6 inhibitorNon-inhibitor0.889
CYP450 2C19 inhibitorInhibitor0.6214
CYP450 3A4 inhibitorNon-inhibitor0.8508
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7596
Ames testNon AMES toxic0.6152
CarcinogenicityNon-carcinogens0.5754
BiodegradationNot ready biodegradable0.7716
Rat acute toxicity2.4527 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9848
hERG inhibition (predictor II)Non-inhibitor0.8932
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014i-0497000000-44320e93d610fb5074f5
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-0300900000-8c21a5272c47622769e7
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0002-0390000000-b69da0c82250f1f81243
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014i-0496000000-06716b4dad8f8d33dee6
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-2920000000-abe97627fbae89daa0db

Taxonomy

Description
This compound belongs to the class of organic compounds known as stilbenes. These are organic compounds containing a 1,2-diphenylethylene moiety. Stilbenes (C6-C2-C6 ) are derived from the common phenylpropene (C6-C3) skeleton building block. The introduction of one or more hydroxyl groups to a phenyl ring lead to stilbenoids.
Kingdom
Organic compounds
Super Class
Phenylpropanoids and polyketides
Class
Stilbenes
Sub Class
Not Available
Direct Parent
Stilbenes
Alternative Parents
Benzenesulfonyl compounds / Butenolides / Sulfones / Enoate esters / Lactones / Oxacyclic compounds / Monocarboxylic acids and derivatives / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Stilbene / Benzenesulfonyl group / Monocyclic benzene moiety / 2-furanone / Benzenoid / Dihydrofuran / Alpha,beta-unsaturated carboxylic ester / Enoate ester / Sulfonyl / Sulfone
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
sulfone, butenolide (CHEBI:8887)

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...
Gene Name
PTGS2
Uniprot ID
P35354
Uniprot Name
Prostaglandin G/H synthase 2
Molecular Weight
68995.625 Da
References
  1. Ehrich EW, Schnitzer TJ, McIlwain H, Levy R, Wolfe F, Weisman M, Zeng Q, Morrison B, Bolognese J, Seidenberg B, Gertz BJ: Effect of specific COX-2 inhibition in osteoarthritis of the knee: a 6 week double blind, placebo controlled pilot study of rofecoxib. Rofecoxib Osteoarthritis Pilot Study Group. J Rheumatol. 1999 Nov;26(11):2438-47. [PubMed:10555907]
  2. Malmstrom K, Daniels S, Kotey P, Seidenberg BC, Desjardins PJ: Comparison of rofecoxib and celecoxib, two cyclooxygenase-2 inhibitors, in postoperative dental pain: a randomized, placebo- and active-comparator-controlled clinical trial. Clin Ther. 1999 Oct;21(10):1653-63. [PubMed:10566562]
  3. Langman MJ, Jensen DM, Watson DJ, Harper SE, Zhao PL, Quan H, Bolognese JA, Simon TJ: Adverse upper gastrointestinal effects of rofecoxib compared with NSAIDs. JAMA. 1999 Nov 24;282(20):1929-33. [PubMed:10580458]
  4. Pascucci RA: COX-2-specific inhibition: implications for clinical practice. J Am Osteopath Assoc. 1999 Nov;99(11 Suppl):S18-22. [PubMed:10643177]
  5. Hawkey C, Laine L, Simon T, Beaulieu A, Maldonado-Cocco J, Acevedo E, Shahane A, Quan H, Bolognese J, Mortensen E: Comparison of the effect of rofecoxib (a cyclooxygenase 2 inhibitor), ibuprofen, and placebo on the gastroduodenal mucosa of patients with osteoarthritis: a randomized, double-blind, placebo-controlled trial. The Rofecoxib Osteoarthritis Endoscopy Multinational Study Group. Arthritis Rheum. 2000 Feb;43(2):370-7. [PubMed:10693877]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  7. Ashok V, Dash C, Rohan TE, Sprafka JM, Terry PD: Selective cyclooxygenase-2 (COX-2) inhibitors and breast cancer risk. Breast. 2011 Feb;20(1):66-70. doi: 10.1016/j.breast.2010.07.004. Epub 2010 Aug 17. [PubMed:20724158]
  8. Baron JA, Sandler RS, Bresalier RS, Lanas A, Morton DG, Riddell R, Iverson ER, Demets DL: Cardiovascular events associated with rofecoxib: final analysis of the APPROVe trial. Lancet. 2008 Nov 15;372(9651):1756-64. doi: 10.1016/S0140-6736(08)61490-7. Epub 2008 Oct 14. [PubMed:18922570]
  9. Chakraborti AK, Garg SK, Kumar R, Motiwala HF, Jadhavar PS: Progress in COX-2 inhibitors: a journey so far. Curr Med Chem. 2010;17(15):1563-93. [PubMed:20166930]
  10. Matheson AJ, Figgitt DP: Rofecoxib: a review of its use in the management of osteoarthritis, acute pain and rheumatoid arthritis. Drugs. 2001;61(6):833-65. [PubMed:11398914]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Extracellular matrix structural constituent
Specific Function
Major structural protein of tissues such as aorta and nuchal ligament, which must expand rapidly and recover completely. Molecular determinant of the late arterial morphogenesis, stabilizing arteri...
Gene Name
ELN
Uniprot ID
P15502
Uniprot Name
Elastin
Molecular Weight
68468.375 Da
References
  1. Oitate M, Hirota T, Koyama K, Inoue S, Kawai K, Ikeda T: Covalent binding of radioactivity from [14C]rofecoxib, but not [14C]celecoxib or [14C]CS-706, to the arterial elastin of rats. Drug Metab Dispos. 2006 Aug;34(8):1417-22. Epub 2006 May 5. [PubMed:16679386]
  2. Oitate M, Hirota T, Takahashi M, Murai T, Miura S, Senoo A, Hosokawa T, Oonishi T, Ikeda T: Mechanism for covalent binding of rofecoxib to elastin of rat aorta. J Pharmacol Exp Ther. 2007 Mar;320(3):1195-203. Epub 2006 Dec 12. [PubMed:17164475]
  3. Oitate M, Hirota T, Murai T, Miura S, Ikeda T: Covalent binding of rofecoxib, but not other cyclooxygenase-2 inhibitors, to allysine aldehyde in elastin of human aorta. Drug Metab Dispos. 2007 Oct;35(10):1846-52. Epub 2007 Jul 9. [PubMed:17620346]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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
Inhibitor
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [PubMed:19754423]
  2. 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]
  3. 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
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 gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
Molecular Weight
68685.82 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
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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 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]
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 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]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Atpase activity, coupled to transmembrane movement of substances
Specific Function
May be an organic anion pump relevant to cellular detoxification.
Gene Name
ABCC4
Uniprot ID
O15439
Uniprot Name
Multidrug resistance-associated protein 4
Molecular Weight
149525.33 Da
References
  1. Reid G, Wielinga P, Zelcer N, van der Heijden I, Kuil A, de Haas M, Wijnholds J, Borst P: The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9. Epub 2003 Jun 30. [PubMed:12835412]

Drug created on June 13, 2005 07:24 / Updated on November 07, 2017 01:39