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Identification
NameSulindac
Accession NumberDB00605  (APRD01243)
TypeSmall Molecule
GroupsApproved
DescriptionSulindac is a nonsteroidal anti-inflammatory agent (NSAIA) of the arylalkanoic acid class that is marketed in the U.S. by Merck as Clinoril. Like other NSAIAs, it may be used in the treatment of acute or chronic inflammatory conditions. Sulindac is a prodrug, derived from sulfinylindene, that is converted in vivo to an active sulfide compound by liver enzymes. The sulfide metabolite then undergoes enterohepatic circulation; it is excreted in the bile and then reabsorbed from the intestine. This is thought to help maintain constant blood levels with reduced gastrointestinal side effects. Some studies have shown sulindac to be relatively less irritating to the stomach than other NSAIA's except for drugs of the cyclooxygenase-2 (COX-2) inhibitor class. The exact mechanism of its NSAIA properties is unknown, but it is thought to act on enzymes COX-1 and COX-2, inhibiting prostaglandin synthesis.
Structure
Thumb
Synonyms
(Z)-5-Fluoro-2-methyl-1-((P-(methylsulfinyl)phenyl)methylene)-1H-indene-3-acetic acid
cis-5-Fluoro-2-methyl-1-((4-(methylsulfinyl)phenyl)methylene)-1H-indene-3-acetic acid
cis-5-Fluoro-2-methyl-1-((P-methylsulfinyl)benzylidene)indene-3-acetic acid
Clinoril
Sulindac
Sulindaco
Sulindacum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Clinoril Tab 150mgtablet150 mgoralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1979-12-311998-08-14Canada
Clinoril Tab 200mgtablet200 mgoralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1979-12-311998-08-14Canada
Nu-sulindac Tab 150mgtablet150 mgoralNu Pharm Inc1994-12-312012-09-04Canada
Nu-sulindac Tab 200mgtablet200 mgoralNu Pharm Inc1994-12-312012-09-04Canada
Penta-sulindactablet150 mgoralPentapharm Ltd.Not applicableNot applicableCanada
Penta-sulindactablet200 mgoralPentapharm Ltd.Not applicableNot applicableCanada
Sulindac-150 Tab 150mgtablet150 mgoralPro Doc Limitee1989-12-312009-07-23Canada
Sulindac-200 Tab 200mgtablet200 mgoralPro Doc Limitee1989-12-312009-07-23Canada
Teva-sulindactablet150 mgoralTeva Canada Limited1988-12-31Not applicableCanada
Teva-sulindactablet200 mgoralTeva Canada Limited1988-12-31Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-sulin Tab 150mgtablet150 mgoralApotex Inc1988-12-31Not applicableCanada
Apo-sulin Tab 200mgtablet200 mgoralApotex Inc1988-12-31Not applicableCanada
Sulindactablet200 mg/1oralSTAT Rx USA LLC2010-01-25Not applicableUs
Sulindactablet150 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Sulindactablet200 mg/1oralA S Medication Solutions2009-09-04Not applicableUs
Sulindactablet150 mg/1oralMylan Pharmaceuticals Inc.1993-06-22Not applicableUs
Sulindactablet200 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-06-23Not applicableUs
Sulindactablet200 mg/1oralGolden State Medical Supply, Inc.2010-01-25Not applicableUs
Sulindactablet200 mg/1oralEpic Pharma, LLC2010-01-25Not applicableUs
Sulindactablet150 mg/1oralPhysicians Total Care, Inc.2007-07-04Not applicableUs
Sulindactablet200 mg/1oralMajor Pharmaceuticals2009-09-04Not applicableUs
Sulindactablet200 mg/1oralMutual Pharmaceutical Company, Inc.2009-09-04Not applicableUs
Sulindactablet200 mg/1oralCarilion Materials Management1990-04-03Not applicableUs
Sulindactablet150 mg/1oralHeritage Pharmaceuticals Inc.2007-07-16Not applicableUs
Sulindactablet200 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Sulindactablet200 mg/1oralMylan Pharmaceuticals Inc.1993-06-22Not applicableUs
Sulindactablet200 mg/1oralMylan Institutional Inc.1997-01-31Not applicableUs
Sulindactablet200 mg/1oralbryant ranch prepack1990-04-03Not applicableUs
Sulindactablet150 mg/1oralEpic Pharma, LLC2010-01-25Not applicableUs
Sulindactablet200 mg/1oralPhysicians Total Care, Inc.2007-07-05Not applicableUs
Sulindactablet150 mg/1oralMajor Pharmaceuticals2010-11-30Not applicableUs
Sulindactablet200 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Sulindactablet200 mg/1oralHeritage Pharmaceuticals Inc.2007-07-16Not applicableUs
Sulindactablet150 mg/1oralRichmond Pharmaceuticals2009-09-04Not applicableUs
Sulindactablet200 mg/1oralH.J. Harkins Company, Inc.1990-04-03Not applicableUs
Sulindactablet150 mg/1oralbryant ranch prepack1990-04-03Not applicableUs
Sulindactablet200 mg/1oralWatson Laboratories, Inc.1990-04-03Not applicableUs
Sulindactablet150 mg/1oralEpic Pharma, LLC2015-07-28Not applicableUs
Sulindactablet200 mg/1oralPd Rx Pharmaceuticals, Inc.1990-04-03Not applicableUs
Sulindactablet200 mg/1oralMajor Pharmaceuticals2010-11-30Not applicableUs
Sulindactablet200 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Sulindactablet200 mg/1oralAidarex Pharmaceuticals LLC2010-01-25Not applicableUs
Sulindactablet200 mg/1oralRichmond Pharmaceuticals2009-09-04Not applicableUs
Sulindactablet150 mg/1oralWatson Laboratories, Inc.1990-04-03Not applicableUs
Sulindactablet150 mg/1oralMutual Pharmaceutical Company, Inc.2009-09-04Not applicableUs
Sulindactablet200 mg/1oralCarilion Materials Management1990-04-03Not applicableUs
Sulindactablet200 mg/1oralEpic Pharma, LLC2015-07-28Not applicableUs
Sulindactablet150 mg/1oralGolden State Medical Supply, Inc.2010-01-25Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ClinorilMerck
Brand mixturesNot Available
SaltsNot Available
Categories
UNII184SNS8VUH
CAS number38194-50-2
WeightAverage: 356.411
Monoisotopic: 356.088243305
Chemical FormulaC20H17FO3S
InChI KeyInChIKey=MLKXDPUZXIRXEP-MFOYZWKCSA-N
InChI
InChI=1S/C20H17FO3S/c1-12-17(9-13-3-6-15(7-4-13)25(2)24)16-8-5-14(21)10-19(16)18(12)11-20(22)23/h3-10H,11H2,1-2H3,(H,22,23)/b17-9-
IUPAC Name
2-[(1Z)-5-fluoro-1-[(4-methanesulfinylphenyl)methylidene]-2-methyl-1H-inden-3-yl]acetic acid
SMILES
CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(C=C1)S(C)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as indenes and isoindenes. These are compounds containing an indene moiety(which consists of a cyclopentadiene fused to a benzene ring), or a isoindene moiety (which consists of a cyclopentadiene fused to cyclohexadiene ring).
KingdomOrganic compounds
Super ClassBenzenoids
ClassIndenes and isoindenes
Sub ClassNot Available
Direct ParentIndenes and isoindenes
Alternative Parents
Substituents
  • Indene
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Sulfoxide
  • Sulfinyl compound
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Aromatic homopolycyclic compound
Molecular FrameworkAromatic homopolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor acute or long-term use in the relief of signs and symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute painful shoulder (acute subacromial bursitis/supraspinatus tendinitis), and acute gouty arthritis.
PharmacodynamicsSulindac is a non-steroidal anti-inflammatory indene derivative, also possessing analgesic and antipyretic activities.
Mechanism of actionSulindac's exact mechanism of action is unknown. Its antiinflammatory effects are believed to be due to inhibition of both COX-1 and COX-2 which leads to the inhibition of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.
Related Articles
AbsorptionApproximately 90% absorbed in humans following oral administration.
Volume of distributionNot Available
Protein bindingAt 1 mcg/ml concentrations, approximately 93% sulindac and 98% of its sulfide metabolite are bound to human serum albumin.
Metabolism

Undergoes two major biotransformations: reversible reduction to the sulfide metabolite, and irreversible oxidation to the sulfone metabolite. Sulindac and its sulfide and sulfone metabolites undergo extensive enterohepatic circulation. Available evidence indicates that the biological activity resides with the sulfide metabolite. Side chain hydroxylation and hydration of the double bond also occur.

SubstrateEnzymesProduct
Sulindac
Not Available
Sulindac sulfideDetails
Sulindac
Not Available
Sulindac sulfoneDetails
Route of eliminationSulindac is excreted in rat milk; concentrations in milk were 10 to 20% of those levels in plasma. It is not known if sulindac is excreted in human milk. Approximately 50% of the administered dose of sulindac is excreted in the urine with the conjugated sulfone metabolite accounting for the major portion. Hepatic metabolism is an important elimination pathway.
Half lifeThe mean half-life of sulindac is 7.8 hours while the mean half-life of the sulfide metabolite is 16.4 hours.
Clearance
  • Renal cl=68.12 +/- 27.56 mL/min [NORMAL (19-41 yrs)]
ToxicityAcute oral toxicity (LD50) in rats is 264 mg/kg. Cases of overdose have been reported and rarely, deaths have occurred. The following signs and symptoms may be observed following overdose: stupor, coma, diminished urine output and hypotension.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Sulindac Action PathwayDrug actionSMP00094
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9937
Blood Brain Barrier+0.8325
Caco-2 permeable-0.8957
P-glycoprotein substrateNon-substrate0.5904
P-glycoprotein inhibitor INon-inhibitor0.5847
P-glycoprotein inhibitor IINon-inhibitor0.9949
Renal organic cation transporterNon-inhibitor0.8753
CYP450 2C9 substrateNon-substrate0.7715
CYP450 2D6 substrateNon-substrate0.8961
CYP450 3A4 substrateNon-substrate0.5629
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5789
Ames testNon AMES toxic0.5451
CarcinogenicityNon-carcinogens0.6516
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.0989 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9768
hERG inhibition (predictor II)Non-inhibitor0.8671
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Merck research laboratories div merck co inc
  • Epic pharma llc
  • Heritage pharmaceuticals inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral150 mg
Tabletoral200 mg
Tabletoral150 mg/1
Tabletoral200 mg/1
Prices
Unit descriptionCostUnit
Sulindac powder17.36USD g
Clinoril 200 mg tablet1.58USD tablet
Sulindac 200 mg tablet1.23USD tablet
Sulindac 150 mg tablet1.0USD tablet
Apo-Sulin 200 mg Tablet0.51USD tablet
Novo-Sundac 200 mg Tablet0.51USD tablet
Nu-Sulindac 200 mg Tablet0.51USD tablet
Apo-Sulin 150 mg Tablet0.4USD tablet
Novo-Sundac 150 mg Tablet0.4USD tablet
Nu-Sulindac 150 mg Tablet0.4USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point183 °CPhysProp
water solubility3000 mg/LMERCK INDEX (1996); pH 7
logP3.42SANGSTER (1993)
pKa4.7MERCK INDEX (1996)
Predicted Properties
PropertyValueSource
Water Solubility0.0251 mg/mLALOGPS
logP2.96ALOGPS
logP2.93ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)4.09ChemAxon
pKa (Strongest Basic)-6.7ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area54.37 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity99.56 m3·mol-1ChemAxon
Polarizability37.2 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

Gary Piazza, Robert Reynolds, “Derivatives of sulindac, use thereof and preparation thereof.” U.S. Patent US20070244122, issued October 18, 2007.

US20070244122
General ReferencesNot Available
External Links
ATC CodesM01AB02
AHFS Codes
  • 28:08.04.92
PDB EntriesNot Available
FDA labelDownload (106 KB)
MSDSDownload (73.2 KB)
Interactions
Drug Interactions
Drug
AbciximabSulindac may increase the anticoagulant activities of Abciximab.
AcebutololSulindac may decrease the antihypertensive activities of Acebutolol.
AceclofenacThe risk or severity of adverse effects can be increased when Sulindac is combined with Aceclofenac.
AcenocoumarolSulindac may increase the anticoagulant activities of Acenocoumarol.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Sulindac.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Sulindac is combined with Acetylsalicylic acid.
AdapaleneThe risk or severity of adverse effects can be increased when Adapalene is combined with Sulindac.
Alendronic acidThe risk or severity of adverse effects can be increased when Sulindac is combined with Alendronic acid.
AliskirenSulindac may decrease the antihypertensive activities of Aliskiren.
AlprenololSulindac may decrease the antihypertensive activities of Alprenolol.
AlprostadilThe therapeutic efficacy of Alprostadil can be decreased when used in combination with Sulindac.
AmikacinSulindac may decrease the excretion rate of Amikacin which could result in a lower serum level and potentially a reduction in efficacy.
AmilorideSulindac may decrease the antihypertensive activities of Amiloride.
AncrodSulindac may increase the anticoagulant activities of Ancrod.
AntipyrineThe risk or severity of adverse effects can be increased when Sulindac is combined with Antipyrine.
Antithrombin III humanSulindac may increase the anticoagulant activities of Antithrombin III human.
ApixabanSulindac may increase the anticoagulant activities of Apixaban.
ApremilastThe risk or severity of adverse effects can be increased when Sulindac is combined with Apremilast.
ArdeparinSulindac may increase the anticoagulant activities of Ardeparin.
ArgatrobanSulindac may increase the anticoagulant activities of Argatroban.
ArotinololSulindac may decrease the antihypertensive activities of Arotinolol.
AtenololSulindac may decrease the antihypertensive activities of Atenolol.
AzapropazoneThe risk or severity of adverse effects can be increased when Sulindac is combined with Azapropazone.
AzelastineThe risk or severity of adverse effects can be increased when Sulindac is combined with Azelastine.
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Sulindac.
BalsalazideSulindac may increase the nephrotoxic activities of Balsalazide.
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Sulindac.
BecaplerminSulindac may increase the anticoagulant activities of Becaplermin.
BefunololSulindac may decrease the antihypertensive activities of Befunolol.
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Sulindac.
BendroflumethiazideThe therapeutic efficacy of Bendroflumethiazide can be decreased when used in combination with Sulindac.
BenoxaprofenThe risk or severity of adverse effects can be increased when Sulindac is combined with Benoxaprofen.
BetaxololSulindac may decrease the antihypertensive activities of Betaxolol.
BevacizumabBevacizumab may increase the cardiotoxic activities of Sulindac.
BevantololSulindac may decrease the antihypertensive activities of Bevantolol.
BimatoprostThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Sulindac.
BisoprololSulindac may decrease the antihypertensive activities of Bisoprolol.
BivalirudinSulindac may increase the anticoagulant activities of Bivalirudin.
BopindololSulindac may decrease the antihypertensive activities of Bopindolol.
BromfenacThe risk or severity of adverse effects can be increased when Sulindac is combined with Bromfenac.
BufuralolSulindac may decrease the antihypertensive activities of Bufuralol.
BumetanideSulindac may decrease the diuretic activities of Bumetanide.
BupranololSulindac may decrease the antihypertensive activities of Bupranolol.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Sulindac.
CandesartanThe risk or severity of adverse effects can be increased when Candesartan is combined with Sulindac.
CandoxatrilThe risk or severity of adverse effects can be increased when Candoxatril is combined with Sulindac.
CaptoprilThe risk or severity of adverse effects can be increased when Captopril is combined with Sulindac.
Carboprost TromethamineThe therapeutic efficacy of Carboprost Tromethamine can be decreased when used in combination with Sulindac.
CarprofenThe risk or severity of adverse effects can be increased when Sulindac is combined with Carprofen.
CarteololSulindac may decrease the antihypertensive activities of Carteolol.
CarvedilolSulindac may decrease the antihypertensive activities of Carvedilol.
CastanospermineThe risk or severity of adverse effects can be increased when Sulindac is combined with Castanospermine.
CelecoxibThe risk or severity of adverse effects can be increased when Celecoxib is combined with Sulindac.
CeliprololSulindac may decrease the antihypertensive activities of Celiprolol.
CertoparinSulindac may increase the anticoagulant activities of Certoparin.
ChloroquineThe risk or severity of adverse effects can be increased when Sulindac is combined with Chloroquine.
ChlorothiazideThe therapeutic efficacy of Chlorothiazide can be decreased when used in combination with Sulindac.
ChlorthalidoneThe therapeutic efficacy of Chlorthalidone can be decreased when used in combination with Sulindac.
CholestyramineCholestyramine can cause a decrease in the absorption of Sulindac 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 Sulindac.
Citric AcidSulindac may increase the anticoagulant activities of Citric Acid.
ClodronateThe risk or severity of adverse effects can be increased when Sulindac is combined with Clodronate.
ClonixinThe risk or severity of adverse effects can be increased when Sulindac is combined with Clonixin.
CloprostenolThe therapeutic efficacy of Cloprostenol can be decreased when used in combination with Sulindac.
ColesevelamColesevelam can cause a decrease in the absorption of Sulindac resulting in a reduced serum concentration and potentially a decrease in efficacy.
ColestipolColestipol can cause a decrease in the absorption of Sulindac resulting in a reduced serum concentration and potentially a decrease in efficacy.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Sulindac.
CyclosporineSulindac may increase the nephrotoxic activities of Cyclosporine.
D-LimoneneThe risk or severity of adverse effects can be increased when Sulindac is combined with D-Limonene.
Dabigatran etexilateSulindac may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinSulindac may increase the anticoagulant activities of Dalteparin.
DanaparoidSulindac may increase the anticoagulant activities of Danaparoid.
DaunorubicinSulindac may decrease the excretion rate of Daunorubicin which could result in a lower serum level and potentially a reduction in efficacy.
DeferasiroxThe risk or severity of adverse effects can be increased when Sulindac is combined with Deferasirox.
DesirudinSulindac may increase the anticoagulant activities of Desirudin.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Sulindac.
DesmopressinThe risk or severity of adverse effects can be increased when Sulindac is combined with Desmopressin.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Sulindac.
DextranSulindac may increase the anticoagulant activities of Dextran.
Dextran 40Sulindac may increase the anticoagulant activities of Dextran 40.
Dextran 70Sulindac may increase the anticoagulant activities of Dextran 70.
Dextran 75Sulindac may increase the anticoagulant activities of Dextran 75.
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Sulindac.
DicoumarolSulindac may increase the anticoagulant activities of Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Sulindac is combined with Diflunisal.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Sulindac.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Sulindac.
DigoxinDigoxin may decrease the cardiotoxic activities of Sulindac.
DihydrostreptomycinSulindac may decrease the excretion rate of Dihydrostreptomycin which could result in a lower serum level and potentially a reduction in efficacy.
Dimethyl sulfoxideThe metabolism of Sulindac can be decreased when combined with Dimethyl sulfoxide.
DinoprostoneThe therapeutic efficacy of Dinoprostone can be decreased when used in combination with Sulindac.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Sulindac.
DoxorubicinSulindac may decrease the excretion rate of Doxorubicin which could result in a lower serum level and potentially a reduction in efficacy.
DrospirenoneSulindac may increase the hyperkalemic activities of Drospirenone.
DroxicamThe risk or severity of adverse effects can be increased when Sulindac is combined with Droxicam.
Edetic AcidSulindac may increase the anticoagulant activities of Edetic Acid.
EdoxabanSulindac may increase the anticoagulant activities of Edoxaban.
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Sulindac.
EnalaprilatThe risk or severity of adverse effects can be increased when Enalaprilat is combined with Sulindac.
EnoxaparinSulindac may increase the anticoagulant activities of Enoxaparin.
EpirizoleThe risk or severity of adverse effects can be increased when Sulindac is combined with Epirizole.
EpirubicinSulindac may decrease the excretion rate of Epirubicin which could result in a lower serum level and potentially a reduction in efficacy.
EplerenoneSulindac may decrease the antihypertensive activities of Eplerenone.
EpoprostenolThe therapeutic efficacy of Epoprostenol can be decreased when used in combination with Sulindac.
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Sulindac.
EsmololSulindac may decrease the antihypertensive activities of Esmolol.
Etacrynic acidSulindac may decrease the diuretic activities of Etacrynic acid.
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Sulindac.
Ethyl biscoumacetateSulindac may increase the anticoagulant activities of Ethyl biscoumacetate.
Etidronic acidThe risk or severity of adverse effects can be increased when Sulindac is combined with Etidronic acid.
EtodolacThe risk or severity of adverse effects can be increased when Sulindac is combined with Etodolac.
EtofenamateThe risk or severity of adverse effects can be increased when Sulindac is combined with Etofenamate.
EtoricoxibThe risk or severity of adverse effects can be increased when Sulindac is combined with Etoricoxib.
Evening primrose oilThe risk or severity of adverse effects can be increased when Sulindac is combined with Evening primrose oil.
exisulindThe risk or severity of adverse effects can be increased when Sulindac is combined with exisulind.
FenbufenThe risk or severity of adverse effects can be increased when Sulindac is combined with Fenbufen.
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Sulindac.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Sulindac.
FlunixinThe risk or severity of adverse effects can be increased when Sulindac is combined with Flunixin.
FlurbiprofenThe risk or severity of adverse effects can be increased when Sulindac is combined with Flurbiprofen.
Folic AcidThe therapeutic efficacy of Folic Acid can be decreased when used in combination with Sulindac.
Fondaparinux sodiumSulindac may increase the anticoagulant activities of Fondaparinux sodium.
ForasartanThe risk or severity of adverse effects can be increased when Forasartan is combined with Sulindac.
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Sulindac.
FramycetinSulindac may decrease the excretion rate of Framycetin which could result in a lower serum level and potentially a reduction in efficacy.
FurosemideSulindac may decrease the diuretic activities of Furosemide.
GemeprostThe therapeutic efficacy of Gemeprost can be decreased when used in combination with Sulindac.
GentamicinSulindac 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 Sulindac is combined with Haloperidol.
HeparinSulindac may increase the anticoagulant activities of Heparin.
HirulogSulindac may increase the anticoagulant activities of Hirulog.
HMPL-004The risk or severity of adverse effects can be increased when Sulindac is combined with HMPL-004.
HydralazineSulindac may decrease the antihypertensive activities of Hydralazine.
HydrochlorothiazideThe therapeutic efficacy of Hydrochlorothiazide can be decreased when used in combination with Sulindac.
HydroflumethiazideThe therapeutic efficacy of Hydroflumethiazide can be decreased when used in combination with Sulindac.
Hygromycin BSulindac 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 Sulindac is combined with Ibandronate.
IbuprofenThe risk or severity of adverse effects can be increased when Sulindac is combined with Ibuprofen.
IbuproxamThe risk or severity of adverse effects can be increased when Sulindac is combined with Ibuproxam.
IcatibantThe risk or severity of adverse effects can be increased when Sulindac is combined with Icatibant.
IdarubicinSulindac may decrease the excretion rate of Idarubicin which could result in a lower serum level and potentially a reduction in efficacy.
IloprostThe therapeutic efficacy of Iloprost can be decreased when used in combination with Sulindac.
IndapamideThe therapeutic efficacy of Indapamide can be decreased when used in combination with Sulindac.
IndenololSulindac may decrease the antihypertensive activities of Indenolol.
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Sulindac.
IndoprofenThe risk or severity of adverse effects can be increased when Sulindac is combined with Indoprofen.
IrbesartanThe risk or severity of adverse effects can be increased when Irbesartan is combined with Sulindac.
IsoxicamThe risk or severity of adverse effects can be increased when Sulindac is combined with Isoxicam.
KanamycinSulindac 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 Sulindac is combined with Kebuzone.
KetoprofenThe risk or severity of adverse effects can be increased when Sulindac is combined with Ketoprofen.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Sulindac.
LabetalolSulindac may decrease the antihypertensive activities of Labetalol.
LeflunomideThe risk or severity of adverse effects can be increased when Sulindac is combined with Leflunomide.
LepirudinSulindac may increase the anticoagulant activities of Lepirudin.
LevobunololSulindac may decrease the antihypertensive activities of Levobunolol.
LisinoprilThe risk or severity of adverse effects can be increased when Lisinopril is combined with Sulindac.
LithiumThe serum concentration of Lithium can be increased when it is combined with Sulindac.
LornoxicamThe risk or severity of adverse effects can be increased when Sulindac is combined with Lornoxicam.
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Sulindac.
LoxoprofenThe risk or severity of adverse effects can be increased when Sulindac is combined with Loxoprofen.
LubiprostoneThe therapeutic efficacy of Lubiprostone can be decreased when used in combination with Sulindac.
LumiracoxibThe risk or severity of adverse effects can be increased when Sulindac is combined with Lumiracoxib.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Sulindac is combined with Magnesium salicylate.
MasoprocolThe risk or severity of adverse effects can be increased when Masoprocol is combined with Sulindac.
Meclofenamic acidThe risk or severity of adverse effects can be increased when Sulindac is combined with Meclofenamic acid.
Mefenamic acidThe risk or severity of adverse effects can be increased when Sulindac is combined with Mefenamic acid.
MeloxicamThe risk or severity of adverse effects can be increased when Sulindac is combined with Meloxicam.
MesalazineSulindac may increase the nephrotoxic activities of Mesalazine.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Sulindac.
MetamizoleThe risk or severity of adverse effects can be increased when Sulindac is combined with Metamizole.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Sulindac.
MethyclothiazideThe therapeutic efficacy of Methyclothiazide can be decreased when used in combination with Sulindac.
MetipranololSulindac may decrease the antihypertensive activities of Metipranolol.
MetolazoneThe therapeutic efficacy of Metolazone can be decreased when used in combination with Sulindac.
MetoprololSulindac may decrease the antihypertensive activities of Metoprolol.
MetrizamideSulindac may decrease the excretion rate of Metrizamide which could result in a lower serum level and potentially a reduction in efficacy.
MisoprostolThe therapeutic efficacy of Misoprostol can be decreased when used in combination with Sulindac.
MoexiprilThe risk or severity of adverse effects can be increased when Moexipril is combined with Sulindac.
MorniflumateThe risk or severity of adverse effects can be increased when Morniflumate is combined with Sulindac.
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Sulindac is combined with Mycophenolate mofetil.
Mycophenolic acidThe risk or severity of adverse effects can be increased when Sulindac is combined with Mycophenolic acid.
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Sulindac.
NadololSulindac may decrease the antihypertensive activities of Nadolol.
NadroparinSulindac may increase the anticoagulant activities of Nadroparin.
NaftifineThe risk or severity of adverse effects can be increased when Sulindac is combined with Naftifine.
NaproxenThe risk or severity of adverse effects can be increased when Sulindac is combined with Naproxen.
NCX 4016The risk or severity of adverse effects can be increased when Sulindac is combined with NCX 4016.
NeomycinSulindac 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 Sulindac is combined with Nepafenac.
NetilmicinSulindac may decrease the excretion rate of Netilmicin which could result in a lower serum level and potentially a reduction in efficacy.
Niflumic AcidThe risk or severity of adverse effects can be increased when Sulindac is combined with Niflumic Acid.
NimesulideThe risk or severity of adverse effects can be increased when Sulindac is combined with Nimesulide.
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Sulindac.
OlopatadineThe risk or severity of adverse effects can be increased when Sulindac is combined with Olopatadine.
OlsalazineSulindac may increase the nephrotoxic activities of Olsalazine.
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Sulindac.
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Sulindac is combined with Omacetaxine mepesuccinate.
OmapatrilatThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Sulindac.
OrgoteinThe risk or severity of adverse effects can be increased when Sulindac is combined with Orgotein.
OtamixabanSulindac may increase the anticoagulant activities of Otamixaban.
OuabainOuabain may decrease the cardiotoxic activities of Sulindac.
OxaprozinThe risk or severity of adverse effects can be increased when Sulindac is combined with Oxaprozin.
OxprenololSulindac may decrease the antihypertensive activities of Oxprenolol.
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Sulindac is combined with Oxyphenbutazone.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Sulindac.
PamidronateThe risk or severity of adverse effects can be increased when Sulindac is combined with Pamidronate.
ParecoxibThe risk or severity of adverse effects can be increased when Sulindac is combined with Parecoxib.
ParomomycinSulindac may decrease the excretion rate of Paromomycin which could result in a lower serum level and potentially a reduction in efficacy.
PenbutololSulindac may decrease the antihypertensive activities of Penbutolol.
Pentosan PolysulfateSulindac may increase the anticoagulant activities of Pentosan Polysulfate.
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Sulindac.
PhenindioneSulindac may increase the anticoagulant activities of Phenindione.
PhenprocoumonSulindac may increase the anticoagulant activities of Phenprocoumon.
PhenylbutazoneThe risk or severity of adverse effects can be increased when Sulindac is combined with Phenylbutazone.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Sulindac.
PindololSulindac may decrease the antihypertensive activities of Pindolol.
PiretanideSulindac may decrease the diuretic activities of Piretanide.
PirfenidoneThe risk or severity of adverse effects can be increased when Sulindac is combined with Pirfenidone.
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Sulindac.
PlicamycinSulindac 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 Sulindac.
PractololSulindac may decrease the antihypertensive activities of Practolol.
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Sulindac.
ProbenecidThe serum concentration of Sulindac can be increased when it is combined with Probenecid.
PropacetamolThe risk or severity of adverse effects can be increased when Sulindac is combined with Propacetamol.
PropranololSulindac may decrease the antihypertensive activities of Propranolol.
Prostaglandin D2The therapeutic efficacy of Prostaglandin D2 can be decreased when used in combination with Sulindac.
Protein CSulindac may increase the anticoagulant activities of Protein C.
ProtocatechualdehydeSulindac may increase the anticoagulant activities of Protocatechualdehyde.
PTC299The risk or severity of adverse effects can be increased when Sulindac is combined with PTC299.
PuromycinSulindac may decrease the excretion rate of Puromycin which could result in a lower serum level and potentially a reduction in efficacy.
QuinaprilThe risk or severity of adverse effects can be increased when Quinapril is combined with Sulindac.
QuinethazoneThe therapeutic efficacy of Quinethazone can be decreased when used in combination with Sulindac.
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Sulindac.
RescinnamineThe risk or severity of adverse effects can be increased when Rescinnamine is combined with Sulindac.
ResveratrolThe risk or severity of adverse effects can be increased when Sulindac is combined with Resveratrol.
ReviparinSulindac may increase the anticoagulant activities of Reviparin.
RibostamycinSulindac may decrease the excretion rate of Ribostamycin which could result in a lower serum level and potentially a reduction in efficacy.
RisedronateThe risk or severity of adverse effects can be increased when Sulindac is combined with Risedronate.
RivaroxabanSulindac may increase the anticoagulant activities of Rivaroxaban.
RofecoxibThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Sulindac.
SalicylamideThe risk or severity of adverse effects can be increased when Sulindac is combined with Salicylamide.
Salicylic acidThe risk or severity of adverse effects can be increased when Sulindac is combined with Salicylic acid.
SalsalateThe risk or severity of adverse effects can be increased when Sulindac is combined with Salsalate.
SaprisartanThe risk or severity of adverse effects can be increased when Saprisartan is combined with Sulindac.
SaralasinThe risk or severity of adverse effects can be increased when Saralasin is combined with Sulindac.
SeratrodastThe risk or severity of adverse effects can be increased when Sulindac is combined with Seratrodast.
SotalolSulindac may decrease the antihypertensive activities of Sotalol.
SpectinomycinSulindac 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 Sulindac.
SpironolactoneSulindac may decrease the antihypertensive activities of Spironolactone.
SRT501The risk or severity of adverse effects can be increased when Sulindac is combined with SRT501.
StreptomycinSulindac may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
StreptozocinSulindac may decrease the excretion rate of Streptozocin which could result in a lower serum level and potentially a reduction in efficacy.
SulfasalazineSulindac may increase the nephrotoxic activities of Sulfasalazine.
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Sulindac.
SulodexideSulindac may increase the anticoagulant activities of Sulodexide.
SuprofenThe risk or severity of adverse effects can be increased when Sulindac is combined with Suprofen.
TacrolimusSulindac may increase the nephrotoxic activities of Tacrolimus.
TalniflumateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Sulindac.
TasosartanThe risk or severity of adverse effects can be increased when Tasosartan is combined with Sulindac.
Technetium Tc-99m MedronateThe risk or severity of adverse effects can be increased when Sulindac is combined with Technetium Tc-99m Medronate.
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Sulindac.
TemocaprilThe risk or severity of adverse effects can be increased when Temocapril is combined with Sulindac.
TenofovirThe risk or severity of adverse effects can be increased when Sulindac is combined with Tenofovir.
TenoxicamThe risk or severity of adverse effects can be increased when Tenoxicam is combined with Sulindac.
TepoxalinThe risk or severity of adverse effects can be increased when Sulindac is combined with Tepoxalin.
TeriflunomideThe risk or severity of adverse effects can be increased when Sulindac is combined with Teriflunomide.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Sulindac is combined with Tiaprofenic acid.
TiludronateThe risk or severity of adverse effects can be increased when Sulindac is combined with Tiludronate.
TimololSulindac may decrease the antihypertensive activities of Timolol.
TobramycinSulindac may decrease the excretion rate of Tobramycin which could result in a lower serum level and potentially a reduction in efficacy.
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Sulindac is combined with Tolfenamic Acid.
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Sulindac.
TorasemideSulindac may decrease the diuretic activities of Torasemide.
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Sulindac.
TranilastThe risk or severity of adverse effects can be increased when Sulindac is combined with Tranilast.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Sulindac.
TravoprostThe therapeutic efficacy of Travoprost can be decreased when used in combination with Sulindac.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Sulindac.
TriamtereneSulindac may decrease the antihypertensive activities of Triamterene.
TrichlormethiazideThe therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Sulindac.
Trisalicylate-cholineThe risk or severity of adverse effects can be increased when Sulindac is combined with Trisalicylate-choline.
ValdecoxibThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Sulindac.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Sulindac.
VancomycinThe serum concentration of Vancomycin can be increased when it is combined with Sulindac.
WarfarinSulindac may increase the anticoagulant activities of Warfarin.
XimelagatranSulindac may increase the anticoagulant activities of Ximelagatran.
ZaltoprofenThe risk or severity of adverse effects can be increased when Sulindac is combined with Zaltoprofen.
ZileutonThe risk or severity of adverse effects can be increased when Sulindac is combined with Zileuton.
Zoledronic acidThe risk or severity of adverse effects can be increased when Sulindac is combined with Zoledronic acid.
ZomepiracThe risk or severity of adverse effects can be increased when Sulindac 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. Giuliano F, Warner TD: Ex vivo assay to determine the cyclooxygenase selectivity of non-steroidal anti-inflammatory drugs. Br J Pharmacol. 1999 Apr;126(8):1824-30. [PubMed:10372826 ]
  2. Molina MA, Sitja-Arnau M, Lemoine MG, Frazier ML, Sinicrope FA: Increased cyclooxygenase-2 expression in human pancreatic carcinomas and cell lines: growth inhibition by nonsteroidal anti-inflammatory drugs. Cancer Res. 1999 Sep 1;59(17):4356-62. [PubMed:10485483 ]
  3. Yip-Schneider MT, Barnard DS, Billings SD, Cheng L, Heilman DK, Lin A, Marshall SJ, Crowell PL, Marshall MS, Sweeney CJ: Cyclooxygenase-2 expression in human pancreatic adenocarcinomas. Carcinogenesis. 2000 Feb;21(2):139-46. [PubMed:10657949 ]
  4. Fosslien E: Biochemistry of cyclooxygenase (COX)-2 inhibitors and molecular pathology of COX-2 in neoplasia. Crit Rev Clin Lab Sci. 2000 Oct;37(5):431-502. [PubMed:11078056 ]
  5. Taylor MT, Lawson KR, Ignatenko NA, Marek SE, Stringer DE, Skovan BA, Gerner EW: Sulindac sulfone inhibits K-ras-dependent cyclooxygenase-2 expression in human colon cancer cells. Cancer Res. 2000 Dec 1;60(23):6607-10. [PubMed:11118042 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Giuliano F, Warner TD: Ex vivo assay to determine the cyclooxygenase selectivity of non-steroidal anti-inflammatory drugs. Br J Pharmacol. 1999 Apr;126(8):1824-30. [PubMed:10372826 ]
  2. Lim JT, Piazza GA, Han EK, Delohery TM, Li H, Finn TS, Buttyan R, Yamamoto H, Sperl GJ, Brendel K, Gross PH, Pamukcu R, Weinstein IB: Sulindac derivatives inhibit growth and induce apoptosis in human prostate cancer cell lines. Biochem Pharmacol. 1999 Oct 1;58(7):1097-107. [PubMed:10484067 ]
  3. Soriano AF, Helfrich B, Chan DC, Heasley LE, Bunn PA Jr, Chou TC: Synergistic effects of new chemopreventive agents and conventional cytotoxic agents against human lung cancer cell lines. Cancer Res. 1999 Dec 15;59(24):6178-84. [PubMed:10626810 ]
  4. Cheng ZJ, Tikkanen I, Vapaatalo H, Mervaala EM: Vascular effects of COX inhibition and AT1 receptor blockade in transgenic rats harboring mouse renin-2 gene. J Physiol Pharmacol. 2002 Dec;53(4 Pt 1):597-613. [PubMed:12512695 ]
  5. Cheng ZJ, Finckenberg P, Louhelainen M, Merasto S, Tikkanen I, Vapaatalo H, Mervaala EM: Cardiovascular and renal effects of cyclooxygenase inhibition in transgenic rats harboring mouse renin-2 gene (TGR[mREN2]27). Eur J Pharmacol. 2003 Feb 14;461(2-3):159-69. [PubMed:12586211 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Glyceraldehyde oxidoreductase activity
Specific Function:
Catalyzes the NADPH-dependent reduction of a wide variety of carbonyl-containing compounds to their corresponding alcohols with a broad range of catalytic efficiencies.
Gene Name:
AKR1B1
Uniprot ID:
P15121
Molecular Weight:
35853.125 Da
References
  1. Sharma YR, Vajpayee RB, Bhatnagar R, Mohan M, Azad RV, Kumar M, Nath R: Topical sulindac therapy in diabetic senile cataracts: cataract-IV. Indian J Ophthalmol. 1989 Jul-Sep;37(3):127-33. [PubMed:2632448 ]
  2. Crabbe MJ, Freeman G, Halder AB, Bron AJ: The inhibition of bovine lens aldose reductase by Clinoril, its absorption into the human red cell and its effect on human red cell aldose reductase activity. Ophthalmic Res. 1985;17(2):85-9. [PubMed:3920599 ]
  3. Chaudhry PS, Cabrera J, Juliani HR, Varma SD: Inhibition of human lens aldose reductase by flavonoids, sulindac and indomethacin. Biochem Pharmacol. 1983 Jul 1;32(13):1995-8. [PubMed:6409111 ]
  4. Jacobson M, Sharma YR, Cotlier E, Hollander JD: Diabetic complications in lens and nerve and their prevention by sulindac or sorbinil: two novel aldose reductase inhibitors. Invest Ophthalmol Vis Sci. 1983 Oct;24(10):1426-9. [PubMed:6413448 ]
  5. van der Sloot P, Mizisin A, Zochodne D: Sulindac in established experimental diabetes: a follow-up study. Can J Neurol Sci. 1995 Aug;22(3):198-201. [PubMed:8529171 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Phosphatase binding
Specific Function:
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signaling cascade initiated by activated KIT and KITLG/SCF. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell...
Gene Name:
MAPK3
Uniprot ID:
P27361
Molecular Weight:
43135.16 Da
References
  1. Rice PL, Goldberg RJ, Ray EC, Driggers LJ, Ahnen DJ: Inhibition of extracellular signal-regulated kinase 1/2 phosphorylation and induction of apoptosis by sulindac metabolites. Cancer Res. 2001 Feb 15;61(4):1541-7. [PubMed:11245463 ]
  2. Rice PL, Washington M, Schleman S, Beard KS, Driggers LJ, Ahnen DJ: Sulindac sulfide inhibits epidermal growth factor-induced phosphorylation of extracellular-regulated kinase 1/2 and Bad in human colon cancer cells. Cancer Res. 2003 Feb 1;63(3):616-20. [PubMed:12566304 ]
  3. Rice PL, Beard KS, Driggers LJ, Ahnen DJ: Inhibition of extracellular-signal regulated kinases 1/2 is required for apoptosis of human colon cancer cells in vitro by sulindac metabolites. Cancer Res. 2004 Nov 15;64(22):8148-51. [PubMed:15548677 ]
  4. Pangburn HA, Kraus H, Ahnen DJ, Rice PL: Sulindac metabolites inhibit epidermal growth factor receptor activation and expression. J Carcinog. 2005 Sep 2;4:16. [PubMed:16138927 ]
  5. Rice PL, Peters SL, Beard KS, Ahnen DJ: Sulindac independently modulates extracellular signal-regulated kinase 1/2 and cyclic GMP-dependent protein kinase signaling pathways. Mol Cancer Ther. 2006 Mar;5(3):746-54. [PubMed:16546990 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
negative modulator
General Function:
Zinc ion binding
Specific Function:
Ligand-activated transcription factor. Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Has a preference for poly-unsaturated fatty acids, such as gamma-linoleic acid and eicosapentanoic acid. Once activated by a ligand, the receptor binds to promoter elements of target genes. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as ...
Gene Name:
PPARD
Uniprot ID:
Q03181
Molecular Weight:
49902.99 Da
References
  1. He TC, Chan TA, Vogelstein B, Kinzler KW: PPARdelta is an APC-regulated target of nonsteroidal anti-inflammatory drugs. Cell. 1999 Oct 29;99(3):335-45. [PubMed:10555149 ]
  2. Babbar N, Ignatenko NA, Casero RA Jr, Gerner EW: Cyclooxygenase-independent induction of apoptosis by sulindac sulfone is mediated by polyamines in colon cancer. J Biol Chem. 2003 Nov 28;278(48):47762-75. Epub 2003 Sep 23. [PubMed:14506281 ]
  3. Jarvis MC, Gray TJ, Palmer CN: Both PPARgamma and PPARdelta influence sulindac sulfide-mediated p21WAF1/CIP1 upregulation in a human prostate epithelial cell line. Oncogene. 2005 Dec 8;24(55):8211-5. [PubMed:16091736 ]
  4. Kim DJ, Prabhu KS, Gonzalez FJ, Peters JM: Inhibition of chemically induced skin carcinogenesis by sulindac is independent of peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta). Carcinogenesis. 2006 May;27(5):1105-12. Epub 2006 Jan 16. [PubMed:16418176 ]
  5. Liou JY, Ghelani D, Yeh S, Wu KK: Nonsteroidal anti-inflammatory drugs induce colorectal cancer cell apoptosis by suppressing 14-3-3epsilon. Cancer Res. 2007 Apr 1;67(7):3185-91. [PubMed:17409426 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Prostaglandin j receptor activity
Specific Function:
Receptor for prostaglandin D2 (PGD2). Coupled to the G(i)-protein. Receptor activation may result in pertussis toxin-sensitive decreases in cAMP levels and Ca(2+) mobilization. PI3K signaling is also implicated in mediating PTGDR2 effects. PGD2 induced receptor internalization. CRTH2 internalization can be regulated by diverse kinases such as, PKC, PKA, ADRBK1/GRK2, GPRK5/GRK5 and GRK6. Recepto...
Gene Name:
PTGDR2
Uniprot ID:
Q9Y5Y4
Molecular Weight:
43267.15 Da
References
  1. Hata AN, Lybrand TP, Marnett LJ, Breyer RM: Structural determinants of arylacetic acid nonsteroidal anti-inflammatory drugs necessary for binding and activation of the prostaglandin D2 receptor CRTH2. Mol Pharmacol. 2005 Mar;67(3):640-7. Epub 2004 Nov 24. [PubMed:15563582 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Vitamin d 24-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.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 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
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Russeva VN, Zhivkova ZD: Molecular basis of sulindac competition with specific markers for the major binding sites on human serum albumin. Arzneimittelforschung. 2003;53(3):174-81. [PubMed:12705172 ]
  2. Shams-Eldeen MA, Vallner JJ, Needham TE: Interaction of sulindac and metabolite with human serum albumin. J Pharm Sci. 1978 Aug;67(8):1077-80. [PubMed:671241 ]
  3. Zhivkova ZD, Russeva VN: Thermodynamic characterization of the binding process of sulindac to human serum albumin. Arzneimittelforschung. 2003;53(1):53-6. [PubMed:12608015 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Kuze K, Graves P, Leahy A, Wilson P, Stuhlmann H, You G: Heterologous expression and functional characterization of a mouse renal organic anion transporter in mammalian cells. J Biol Chem. 1999 Jan 15;274(3):1519-24. [PubMed:9880528 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23