Identification

Name
Rosiglitazone
Accession Number
DB00412  (APRD00403)
Type
Small Molecule
Groups
Approved, Investigational
Description

Rosiglitazone is an anti-diabetic drug in the thiazolidinedione class of drugs. It is marketed by the pharmaceutical company GlaxoSmithKline as a stand-alone drug (Avandia) and in combination with metformin (Avandamet) or with glimepiride (Avandaryl). Like other thiazolidinediones, the mechanism of action of rosiglitazone is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPARγ. Rosiglitazone is a selective ligand of PPARγ, and has no PPARα-binding action. Apart from its effect on insulin resistance, it appears to have an anti-inflammatory effect: nuclear factor kappa-B (NFκB) levels fall and inhibitor (IκB) levels increase in patients on rosiglitazone. Recent research has suggested that rosiglitazone may also be of benefit to a subset of patients with Alzheimer's disease not expressing the ApoE4 allele. This is the subject of a clinical trial currently underway.

Structure
Thumb
Synonyms
  • (±)-5-[p-[2-(methyl-2-pyridylamino)ethoxy]benzyl]-2,4-thiazolidinedione
  • (RS)-5-{4-[2-(Methyl-2-pyridylamino)ethoxy]benzyl}-2,4-thiazolidinedion
  • Rosiglitazon
  • Rosiglitazona
  • Rosiglitazone
  • Rosiglitazonum
External IDs
BRL-49653 / TDZ-01
Product Ingredients
IngredientUNIICASInChI Key
Rosiglitazone MaleateKX2339DP44155141-29-0SUFUKZSWUHZXAV-BTJKTKAUSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AvandiaTablet, film coated2 mg/1OralGlaxosmithkline Inc2011-05-252016-06-18Us
AvandiaTablet, film coated4 mg/1OralCardinal Health1999-05-292018-04-13Us
AvandiaTablet, film coated4 mg/1OralPhysicians Total Care, Inc.2006-02-07Not applicableUs00029 3159 13 nlmimage10 e418f247
AvandiaTablet2 mgOralGlaxosmithkline Inc2000-03-21Not applicableCanada
AvandiaTablet, film coated2 mg/1OralPhysicians Total Care, Inc.2005-05-13Not applicableUs00029 3158 18 nlmimage10 c118e0a7
AvandiaTablet8 mgOralGlaxosmithkline Inc2000-03-21Not applicableCanada
AvandiaTablet, film coated8 mg/1OralGlaxosmithkline Inc2011-05-252016-04-03Us
AvandiaTablet, film coated8 mg/1OralCardinal Health1999-05-282018-04-13Us
AvandiaTablet, film coated8 mg/1OralPhysicians Total Care, Inc.2001-05-09Not applicableUs00029 3160 13 nlmimage10 9a18cd26
AvandiaTablet4 mgOralGlaxosmithkline Inc2000-03-21Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-rosiglitazoneTablet8 mgOralApotex Corporation2017-02-21Not applicableCanada
Apo-rosiglitazoneTablet4 mgOralApotex Corporation2017-02-21Not applicableCanada
Apo-rosiglitazoneTablet2 mgOralApotex Corporation2017-02-21Not applicableCanada
Dom-rosiglitazoneTablet4 mgOralDominion PharmacalNot applicableNot applicableCanada
Dom-rosiglitazoneTablet2 mgOralDominion PharmacalNot applicableNot applicableCanada
Dom-rosiglitazoneTablet8 mgOralDominion PharmacalNot applicableNot applicableCanada
Mylan-rosiglitazoneTablet8 mgOralMylan PharmaceuticalsNot applicableNot applicableCanada
Mylan-rosiglitazoneTablet4 mgOralMylan PharmaceuticalsNot applicableNot applicableCanada
Mylan-rosiglitazoneTablet2 mgOralMylan PharmaceuticalsNot applicableNot applicableCanada
PHL-rosiglitazoneTablet2 mgOralPharmel IncNot applicableNot applicableCanada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AvandametRosiglitazone Maleate (2 mg/1) + Metformin Hydrochloride (500 mg/1)Tablet, film coatedOralGlaxosmithkline Inc2011-05-242016-05-07Us
AvandametRosiglitazone Maleate (4 mg/1) + Metformin Hydrochloride (500 mg/1)Tablet, film coatedOralPhysicians Total Care, Inc.2006-08-25Not applicableUs
AvandametRosiglitazone (4.00 mg) + Metformin Hydrochloride (1000 mg)TabletOralGlaxosmithkline Inc2004-01-192016-03-24Canada
AvandametRosiglitazone Maleate (4 mg/1) + Metformin Hydrochloride (500 mg/1)Tablet, film coatedOralGlaxosmithkline Inc2011-05-242016-10-13Us
AvandametRosiglitazone Maleate (2 mg/1) + Metformin Hydrochloride (500 mg/1)Tablet, film coatedOralPhysicians Total Care, Inc.2003-12-04Not applicableUs
AvandametRosiglitazone (1 mg) + Metformin Hydrochloride (500 mg)TabletOralGlaxosmithkline Inc2003-02-182013-04-05Canada
AvandametRosiglitazone (2.00 mg) + Metformin Hydrochloride (1000 mg)TabletOralGlaxosmithkline Inc2004-01-192016-07-13Canada
AvandametRosiglitazone Maleate (2 mg/1) + Metformin Hydrochloride (1000 mg/1)Tablet, film coatedOralGlaxosmithkline Inc2011-05-242016-10-13Us
AvandametRosiglitazone Maleate (2 mg/1) + Metformin Hydrochloride (1000 mg/1)Tablet, film coatedOralPhysicians Total Care, Inc.2005-08-03Not applicableUs00007 3163 18 nlmimage10 dd12ee87
AvandametRosiglitazone (4 mg) + Metformin Hydrochloride (500 mg)TabletOralGlaxosmithkline Inc2003-02-182017-04-25Canada
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AvaglimRosiglitazone (8 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
AvaglimRosiglitazone (8 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
AvaglimRosiglitazone (4 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
AvaglimRosiglitazone (8 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
AvaglimRosiglitazone (4 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
AvaglimRosiglitazone (4 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
AvaglimRosiglitazone (4 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
AvaglimRosiglitazone (8 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
AvaglimRosiglitazone (4 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
AvaglimRosiglitazone (8 mg) + Glimepiride (4 mg)Tablet, film coatedOralSmith Kline Beecham2006-06-272011-08-12Eu
International/Other Brands
Blutab (Werrick) / DH-Rosidia (Hasan) / Diaben (Elea) / Diaglinex (Farmindustria) / Gaudil (Craveri) / Gliximina (Denver) / Naidi (Hisun) / Rogelin (Torrent) / Roglit (Gedeon Richter) / Romerol (Drug International) / Rosit (Delta) / Rosix (Garmisch) / Rossini (Trima) / Sensulin (Square) / Sheng Ao (Hengrui) / Sheng Min (ShengJiTang Pharmaceutical)
Categories
UNII
05V02F2KDG
CAS number
122320-73-4
Weight
Average: 357.427
Monoisotopic: 357.114712179
Chemical Formula
C18H19N3O3S
InChI Key
YASAKCUCGLMORW-UHFFFAOYSA-N
InChI
InChI=1S/C18H19N3O3S/c1-21(16-4-2-3-9-19-16)10-11-24-14-7-5-13(6-8-14)12-15-17(22)20-18(23)25-15/h2-9,15H,10-12H2,1H3,(H,20,22,23)
IUPAC Name
5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)methyl]-1,3-thiazolidine-2,4-dione
SMILES
CN(CCOC1=CC=C(CC2SC(=O)NC2=O)C=C1)C1=CC=CC=N1

Pharmacology

Indication

Rosiglitazone is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Associated Conditions
Pharmacodynamics

When rosiglitazone is used as monotherapy, it is associated with increases in total cholesterol, LDL, and HDL. It is also associated with decreases in free fatty acids. Increases in LDL occurred primarily during the first 1 to 2 months of therapy with AVANDIA and LDL levels remained elevated above baseline throughout the trials. In contrast, HDL continued to rise over time. As a result, the LDL/HDL ratio peaked after 2 months of therapy and then appeared to decrease over time.

Mechanism of action

Rosiglitazone acts as a highly selective and potent agonist at peroxisome proliferator activated receptors (PPAR) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, rosiglitazone enhances tissue sensitivity to insulin.

TargetActionsOrganism
APeroxisome proliferator-activated receptor gamma
agonist
Human
ULong-chain-fatty-acid--CoA ligase 4
inhibitor
Human
UPeroxisome proliferator-activated receptor alphaNot AvailableHuman
UPeroxisome proliferator-activated receptor deltaNot AvailableHuman
URetinoic acid receptor RXR-alphaNot AvailableHuman
URetinoic acid receptor RXR-betaNot AvailableHuman
URetinoic acid receptor RXR-gammaNot AvailableHuman
Absorption

The absolute bioavailability of rosiglitazone is 99%. Peak plasma concentrations are observed about 1 hour after dosing. Administration of rosiglitazone with food resulted in no change in overall exposure (AUC), but there was an approximately 28% decrease in Cmax and a delay in Tmax (1.75 hours). These changes are not likely to be clinically significant; therefore, rosiglitazone may be administered with or without food. Maximum plasma concentration (Cmax) and the area under the curve (AUC) of rosiglitazone increase in a dose-proportional manner over the therapeutic dose range.

Volume of distribution
  • 17.6 L [oral volume of distribution Vss/F]
  • 13.5 L [population mean, pediatric patients]
Protein binding

99.8% bound to plasma proteins, primarily albumin.

Metabolism

Hepatic. Rosiglitazone is extensively metabolized in the liver to inactive metabolites via N-demethylation, hydroxylation, and conjugation with sulfate and glucuronic acid. In vitro data have shown that Cytochrome (CYP) P450 isoenzyme 2C8 (CYP2C8) and to a minor extent CYP2C9 are involved in the hepatic metabolism of rosiglitazone.

Route of elimination

Following oral or intravenous administration of [14C]rosiglitazone maleate, approximately 64% and 23% of the dose was eliminated in the urine and in the feces, respectively.

Half life

3-4 hours (single oral dose, independent of dose)

Clearance
  • Oral clearance (CL) = 3.03 ± 0.87 L/hr [1 mg Fasting]
  • Oral CL = 2.89 ± 0.71 L/hr [2 mg Fasting]
  • Oral CL = 2.85 ± 0.69 L/hr [8 mg Fasting]
  • Oral CL = 2.97 ± 0.81 L/hr [8 mg Fed]
  • 3.15 L/hr [Population mean, Pediatric patients]
Toxicity

Side effects include fluid retention, congestive heart failure (CHF), liver disease

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Rosiglitazone Metabolism PathwayDrug metabolism
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Rosiglitazone.Experimental
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Rosiglitazone.Experimental, Investigational
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.Experimental
AbirateroneThe serum concentration of Rosiglitazone can be increased when it is combined with Abiraterone.Approved
AcetohexamideThe therapeutic efficacy of Acetohexamide can be increased when used in combination with Rosiglitazone.Approved, Investigational, Withdrawn
Acetyl sulfisoxazoleThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Acetyl sulfisoxazole.Approved, Vet Approved
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Rosiglitazone.Approved, Vet Approved
AlaproclateAlaproclate may increase the hypoglycemic activities of Rosiglitazone.Experimental
AloxiprinAloxiprin may increase the hypoglycemic activities of Rosiglitazone.Experimental
AmineptineAmineptine may decrease the hypoglycemic activities of Rosiglitazone.Illicit, Withdrawn
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Rosiglitazone.Approved
AmiodaroneThe metabolism of Rosiglitazone can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may decrease the hypoglycemic activities of Rosiglitazone.Approved
AmitriptylinoxideAmitriptylinoxide may decrease the hypoglycemic activities of Rosiglitazone.Approved, Investigational
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Rosiglitazone.Approved, Investigational
AmoxapineAmoxapine may decrease the hypoglycemic activities of Rosiglitazone.Approved
AmprenavirThe metabolism of Rosiglitazone can be decreased when combined with Amprenavir.Approved, Investigational
ApalutamideThe serum concentration of Rosiglitazone can be decreased when it is combined with Apalutamide.Approved, Investigational
ApixabanThe metabolism of Apixaban can be decreased when combined with Rosiglitazone.Approved
AprepitantThe serum concentration of Rosiglitazone can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Asenapine.Approved
AtazanavirThe serum concentration of Rosiglitazone can be increased when it is combined with Atazanavir.Approved, Investigational
AtorvastatinThe excretion of Atorvastatin can be decreased when combined with Rosiglitazone.Approved
AzosemideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Azosemide.Investigational
BalaglitazoneThe metabolism of Balaglitazone can be decreased when combined with Rosiglitazone.Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
BenzthiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Benzthiazide.Approved
BesifloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Besifloxacin.Approved
BetamethasoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BoceprevirThe metabolism of Rosiglitazone can be decreased when combined with Boceprevir.Approved, Withdrawn
BosentanThe serum concentration of Rosiglitazone can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Brexpiprazole.Approved, Investigational
BumetanideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Bumetanide.Approved
BuserelinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Buserelin.Approved, Investigational
ButriptylineButriptyline may decrease the hypoglycemic activities of Rosiglitazone.Approved
CapecitabineThe metabolism of Rosiglitazone can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Rosiglitazone can be increased when combined with Carbamazepine.Approved, Investigational
Carbaspirin calciumCarbaspirin calcium may increase the hypoglycemic activities of Rosiglitazone.Experimental, Investigational
CarbutamideThe therapeutic efficacy of Carbutamide can be increased when used in combination with Rosiglitazone.Experimental
CaroxazoneCaroxazone may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
CelecoxibThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Rosiglitazone can be increased when it is combined with Ceritinib.Approved
CerivastatinThe metabolism of Cerivastatin can be decreased when combined with Rosiglitazone.Approved, Withdrawn
Chloramine-TThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Chloramine-T.Vet Approved
ChlorothiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be increased when used in combination with Rosiglitazone.Approved, Investigational
ChlorsulfaquinoxalineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Chlorsulfaquinoxaline.Investigational
ChlorthalidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Chlorthalidone.Approved
CholestyramineThe serum concentration of Rosiglitazone can be decreased when it is combined with Cholestyramine.Approved, Investigational
CiglitazoneThe metabolism of Ciglitazone can be decreased when combined with Rosiglitazone.Experimental
CinoxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Cinoxacin.Approved, Investigational, Withdrawn
CiprofloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Ciprofloxacin.Approved, Investigational
CitalopramCitalopram may increase the hypoglycemic activities of Rosiglitazone.Approved
ClarithromycinThe metabolism of Rosiglitazone can be decreased when combined with Clarithromycin.Approved
ClofenamideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Clofenamide.Experimental
ClomipramineClomipramine may decrease the hypoglycemic activities of Rosiglitazone.Approved, Investigational, Vet Approved
ClopamideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Clopamide.Experimental
ClopidogrelThe metabolism of Rosiglitazone can be decreased when combined with Clopidogrel.Approved
ClorexoloneThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Clorexolone.Experimental
ClorsulonThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Clorsulon.Vet Approved
ClotrimazoleThe metabolism of Rosiglitazone can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Clozapine.Approved
CobicistatThe metabolism of Rosiglitazone can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Rosiglitazone.Approved, Investigational
CorticotropinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Corticotropin.Approved, Investigational, Vet Approved
Cortisone acetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Cortisone acetate.Approved, Investigational
CrisaboroleThe metabolism of Rosiglitazone can be decreased when combined with Crisaborole.Approved, Investigational
CrizotinibThe metabolism of Rosiglitazone can be decreased when combined with Crizotinib.Approved
CurcuminThe metabolism of Rosiglitazone can be decreased when combined with Curcumin.Approved, Investigational
CyclobenzaprineCyclobenzaprine may decrease the hypoglycemic activities of Rosiglitazone.Approved
CyclopenthiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Cyclopenthiazide.Experimental
CyclosporineThe metabolism of Rosiglitazone can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclothiazideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Cyclothiazide.Approved
Cyproterone acetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Rosiglitazone can be decreased when it is combined with Dabrafenib.Approved, Investigational
DanazolThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Rosiglitazone.Investigational
DarunavirThe metabolism of Rosiglitazone can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Rosiglitazone can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Rosiglitazone can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Rosiglitazone can be decreased when combined with Delavirdine.Approved
DersalazineDersalazine may increase the hypoglycemic activities of Rosiglitazone.Investigational
DesipramineDesipramine may decrease the hypoglycemic activities of Rosiglitazone.Approved, Investigational
DesogestrelThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
DexamethasoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Diazoxide.Approved
DibenzepinDibenzepin may decrease the hypoglycemic activities of Rosiglitazone.Experimental
DiclofenamideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Diclofenamide.Approved, Investigational
DienogestThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Dienogest.Approved
DifloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Difloxacin.Vet Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
DiltiazemThe metabolism of Rosiglitazone can be decreased when combined with Diltiazem.Approved, Investigational
DimetacrineDimetacrine may decrease the hypoglycemic activities of Rosiglitazone.Approved, Withdrawn
DisopyramideRosiglitazone may increase the hypoglycemic activities of Disopyramide.Approved
DosulepinDosulepin may decrease the hypoglycemic activities of Rosiglitazone.Approved
DoxepinDoxepin may decrease the hypoglycemic activities of Rosiglitazone.Approved, Investigational
DoxycyclineThe metabolism of Rosiglitazone can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Rosiglitazone can be decreased when combined with Dronedarone.Approved
DrospirenoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Drospirenone.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Rosiglitazone.Approved
EfavirenzThe metabolism of Rosiglitazone can be decreased when combined with Efavirenz.Approved, Investigational
ElagolixThe metabolism of Elagolix can be decreased when combined with Rosiglitazone.Approved, Investigational
EnoxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Enoxacin.Approved, Investigational
EnzalutamideThe serum concentration of Rosiglitazone can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Epinephrine.Approved, Vet Approved
EpitizideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Epitizide.Experimental
Erythrityl TetranitrateThe risk or severity of adverse effects can be increased when Erythrityl Tetranitrate is combined with Rosiglitazone.Approved, Investigational
ErythromycinThe metabolism of Rosiglitazone can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
EstradiolThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Estrone sulfate.Approved
Etacrynic acidThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Etacrynic acid.Approved, Investigational
Ethinyl EstradiolThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Ethinyl Estradiol.Approved
EthoxzolamideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Ethoxzolamide.Withdrawn
Ethynodiol diacetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtravirineThe serum concentration of Rosiglitazone can be decreased when it is combined with Etravirine.Approved
EverolimusThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Everolimus.Approved
FelbamateThe metabolism of Rosiglitazone can be decreased when combined with Felbamate.Approved
FelodipineThe metabolism of Rosiglitazone can be decreased when combined with Felodipine.Approved, Investigational
FenquizoneThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Fenquizone.Experimental
FleroxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Fleroxacin.Approved
FloxuridineThe metabolism of Rosiglitazone can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Rosiglitazone can be decreased when combined with Fluconazole.Approved, Investigational
FludrocortisoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Fludrocortisone.Approved, Investigational
FlumequineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Flumequine.Withdrawn
FluorouracilThe metabolism of Rosiglitazone can be decreased when combined with Fluorouracil.Approved
FluoxetineFluoxetine may increase the hypoglycemic activities of Rosiglitazone.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Rosiglitazone.Approved, Illicit
FluvastatinThe excretion of Fluvastatin can be decreased when combined with Rosiglitazone.Approved
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
FosamprenavirThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Rosiglitazone can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Rosiglitazone can be increased when combined with Fosphenytoin.Approved, Investigational
FurazolidoneFurazolidone may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational, Vet Approved
FurosemideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Furosemide.Approved, Vet Approved
Fusidic AcidThe serum concentration of Rosiglitazone can be increased when it is combined with Fusidic Acid.Approved, Investigational
GarenoxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Garenoxacin.Investigational
GatifloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Gatifloxacin.Approved, Investigational
GemfibrozilThe metabolism of Rosiglitazone can be decreased when combined with Gemfibrozil.Approved
GemifloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Gemifloxacin.Approved, Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be increased when used in combination with Rosiglitazone.Investigational, Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be increased when used in combination with Rosiglitazone.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be increased when used in combination with Rosiglitazone.Approved
GlipizideThe therapeutic efficacy of Glipizide can be increased when used in combination with Rosiglitazone.Approved, Investigational
GliquidoneThe therapeutic efficacy of Gliquidone can be increased when used in combination with Rosiglitazone.Approved, Investigational
GlisoxepideThe therapeutic efficacy of Glisoxepide can be increased when used in combination with Rosiglitazone.Investigational
GLPG-0492GLPG-0492 may increase the hypoglycemic activities of Rosiglitazone.Investigational
GlyburideThe therapeutic efficacy of Glyburide can be increased when used in combination with Rosiglitazone.Approved
GlycodiazineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Glycodiazine.Approved, Investigational
GoserelinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Goserelin.Approved
GrepafloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Grepafloxacin.Approved, Investigational, Withdrawn
GuacetisalGuacetisal may increase the hypoglycemic activities of Rosiglitazone.Experimental
HarmalineHarmaline may increase the hypoglycemic activities of Rosiglitazone.Experimental
HistrelinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Rosiglitazone.Experimental
HydrochlorothiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydroflumethiazide.Approved, Investigational
HydroxyfasudilThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Hydroxyfasudil.Experimental
Hydroxyprogesterone caproateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydroxyprogesterone caproate.Approved, Investigational
IdelalisibThe metabolism of Rosiglitazone can be decreased when combined with Idelalisib.Approved
IloperidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Iloperidone.Approved
ImatinibThe metabolism of Rosiglitazone can be decreased when combined with Imatinib.Approved
ImipramineImipramine may decrease the hypoglycemic activities of Rosiglitazone.Approved
Imipramine oxideImipramine oxide may decrease the hypoglycemic activities of Rosiglitazone.Experimental
IndalpineIndalpine may increase the hypoglycemic activities of Rosiglitazone.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Indapamide.Approved
IndinavirThe metabolism of Rosiglitazone can be decreased when combined with Indinavir.Approved
Insulin AspartThe risk or severity of congestive heart failure can be increased when Insulin Aspart is combined with Rosiglitazone.Approved
Insulin AspartRosiglitazone may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DegludecThe risk or severity of congestive heart failure can be increased when Insulin Degludec is combined with Rosiglitazone.Approved
Insulin DetemirThe risk or severity of congestive heart failure can be increased when Insulin Detemir is combined with Rosiglitazone.Approved
Insulin DetemirRosiglitazone may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineThe risk or severity of congestive heart failure can be increased when Insulin Glargine is combined with Rosiglitazone.Approved
Insulin GlargineRosiglitazone may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineThe risk or severity of congestive heart failure can be increased when Insulin Glulisine is combined with Rosiglitazone.Approved
Insulin GlulisineRosiglitazone may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanThe risk or severity of congestive heart failure can be increased when Insulin Human is combined with Rosiglitazone.Approved, Investigational
Insulin HumanRosiglitazone may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproThe risk or severity of congestive heart failure can be increased when Insulin Lispro is combined with Rosiglitazone.Approved
Insulin LisproRosiglitazone may increase the hypoglycemic activities of Insulin Lispro.Approved
Insulin peglisproThe risk or severity of congestive heart failure can be increased when Insulin peglispro is combined with Rosiglitazone.Investigational
Insulin PorkThe risk or severity of congestive heart failure can be increased when Insulin Pork is combined with Rosiglitazone.Approved
IprindoleIprindole may decrease the hypoglycemic activities of Rosiglitazone.Experimental
IproniazidIproniazid may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
IrbesartanThe metabolism of Rosiglitazone can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoleThe serum concentration of Rosiglitazone can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Rosiglitazone can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Rosiglitazone.Approved
IsoniazidThe metabolism of Rosiglitazone can be decreased when combined with Isoniazid.Approved, Investigational
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Rosiglitazone.Approved, Investigational
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Isosorbide Mononitrate is combined with Rosiglitazone.Approved
ItraconazoleThe metabolism of Rosiglitazone can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Rosiglitazone can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Rosiglitazone can be decreased when combined with Ketoconazole.Approved, Investigational
LanreotideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Lanreotide.Approved
LapatinibThe metabolism of Lapatinib can be decreased when combined with Rosiglitazone.Approved, Investigational
LeuprolideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Levofloxacin.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
LevonorgestrelThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LinezolidLinezolid may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational, Nutraceutical
LobeglitazoneThe metabolism of Lobeglitazone can be decreased when combined with Rosiglitazone.Approved, Investigational
LofepramineLofepramine may decrease the hypoglycemic activities of Rosiglitazone.Experimental
LomefloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Lomefloxacin.Approved, Investigational
LopinavirThe metabolism of Rosiglitazone can be decreased when combined with Lopinavir.Approved
LorpiprazoleThe serum concentration of Rosiglitazone can be increased when it is combined with Lorpiprazole.Approved
LosartanThe metabolism of Rosiglitazone can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Rosiglitazone can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Rosiglitazone can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Rosiglitazone can be decreased when it is combined with Lumacaftor.Approved
LurasidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Lurasidone.Approved, Investigational
MafenideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Mafenide.Approved, Vet Approved
MebanazineMebanazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
MebutizideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Mebutizide.Experimental
MecaserminRosiglitazone may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
MedrogestoneThe serum concentration of Rosiglitazone can be decreased when it is combined with Medrogestone.Approved
Medroxyprogesterone acetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
MefrusideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Mefruside.Experimental
Megestrol acetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Megestrol acetate.Approved, Investigational, Vet Approved
MelitracenMelitracen may decrease the hypoglycemic activities of Rosiglitazone.Experimental, Investigational
MesalazineMesalazine may increase the hypoglycemic activities of Rosiglitazone.Approved
MesteroloneMesterolone may increase the hypoglycemic activities of Rosiglitazone.Experimental
MestranolThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Mestranol.Approved
MetahexamideThe therapeutic efficacy of Metahexamide can be increased when used in combination with Rosiglitazone.Experimental
MethotrimeprazineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Methotrimeprazine.Approved, Investigational
MethyclothiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Methyclothiazide.Approved
Methyl salicylateMethyl salicylate may increase the hypoglycemic activities of Rosiglitazone.Approved, Vet Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
MethylprednisoloneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
Methylpropylpropanediol dinitrateThe risk or severity of adverse effects can be increased when Methylpropylpropanediol dinitrate is combined with Rosiglitazone.Experimental
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Rosiglitazone.Approved
MeticraneThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Meticrane.Experimental
MetolazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Metolazone.Approved
MibefradilThe metabolism of Rosiglitazone can be decreased when combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe metabolism of Rosiglitazone can be decreased when combined with Miconazole.Approved, Investigational, Vet Approved
MidostaurinThe metabolism of Rosiglitazone can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Rosiglitazone can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
MinaprineMinaprine may increase the hypoglycemic activities of Rosiglitazone.Approved
MitotaneThe serum concentration of Rosiglitazone can be decreased when it is combined with Mitotane.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
ModafinilThe serum concentration of Rosiglitazone can be decreased when it is combined with Modafinil.Approved, Investigational
MoxifloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Moxifloxacin.Approved, Investigational
NabiloneThe metabolism of Rosiglitazone can be decreased when combined with Nabilone.Approved, Investigational
NafcillinThe serum concentration of Rosiglitazone can be decreased when it is combined with Nafcillin.Approved, Investigational
Nalidixic AcidThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Nalidixic Acid.Approved, Investigational
NaloxoneThe metabolism of Rosiglitazone can be decreased when combined with Naloxone.Approved, Vet Approved
NandroloneNandrolone may increase the hypoglycemic activities of Rosiglitazone.Experimental, Investigational
Nandrolone decanoateNandrolone decanoate may increase the hypoglycemic activities of Rosiglitazone.Approved, Illicit
NateglinideRosiglitazone may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NefazodoneThe metabolism of Rosiglitazone can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Rosiglitazone can be decreased when combined with Nelfinavir.Approved
NemonoxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Nemonoxacin.Investigational
NetoglitazoneThe metabolism of Netoglitazone can be decreased when combined with Rosiglitazone.Experimental
NetupitantThe serum concentration of Rosiglitazone can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Rosiglitazone can be increased when combined with Nevirapine.Approved
NiacinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
NicardipineThe metabolism of Rosiglitazone can be decreased when combined with Nicardipine.Approved, Investigational
NilotinibThe metabolism of Rosiglitazone can be decreased when combined with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Rosiglitazone.Investigational
NitroglycerinThe risk or severity of adverse effects can be increased when Nitroglycerin is combined with Rosiglitazone.Approved, Investigational
NN344The risk or severity of congestive heart failure can be increased when NN344 is combined with Rosiglitazone.Investigational
NorethisteroneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Norethisterone.Approved
NorfloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Norfloxacin.Approved
NorgestimateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Norgestimate.Approved, Investigational
NortriptylineNortriptyline may decrease the hypoglycemic activities of Rosiglitazone.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
OctreotideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Octreotide.Approved, Investigational
OfloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Ofloxacin.Approved
OlanzapineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Rosiglitazone can be decreased when combined with Olaparib.Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Rosiglitazone.Approved
OpipramolOpipramol may decrease the hypoglycemic activities of Rosiglitazone.Investigational
OrbifloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Orbifloxacin.Vet Approved
OsimertinibThe serum concentration of Rosiglitazone can be increased when it is combined with Osimertinib.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
OxaprotilineOxaprotiline may decrease the hypoglycemic activities of Rosiglitazone.Experimental
Oxolinic acidThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Oxolinic acid.Experimental
OxymetholoneOxymetholone may increase the hypoglycemic activities of Rosiglitazone.Approved, Illicit
PaclitaxelThe metabolism of Paclitaxel can be decreased when combined with Rosiglitazone.Approved, Vet Approved
PalbociclibThe serum concentration of Rosiglitazone can be increased when it is combined with Palbociclib.Approved, Investigational
PaliperidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Paliperidone.Approved
PargylinePargyline may increase the hypoglycemic activities of Rosiglitazone.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
PasireotideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pasireotide.Approved
Patent BlueThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Patent Blue.Approved
PazopanibThe metabolism of Pazopanib can be decreased when combined with Rosiglitazone.Approved
PazufloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Pazufloxacin.Investigational
PefloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Pefloxacin.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Rosiglitazone.Approved
Pentaerythritol TetranitrateThe risk or severity of adverse effects can be increased when Pentaerythritol Tetranitrate is combined with Rosiglitazone.Approved
PentamidineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pentamidine.Approved, Investigational
PentobarbitalThe metabolism of Rosiglitazone can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Rosiglitazone.Approved
PheniprazinePheniprazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
PhenobarbitalThe metabolism of Rosiglitazone can be increased when combined with Phenobarbital.Approved, Investigational
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
PhenprocoumonThe metabolism of Phenprocoumon can be decreased when combined with Rosiglitazone.Approved, Investigational
Phenyl aminosalicylatePhenyl aminosalicylate may increase the hypoglycemic activities of Rosiglitazone.Approved
PhenytoinThe metabolism of Rosiglitazone can be increased when combined with Phenytoin.Approved, Vet Approved
PhthalylsulfathiazoleThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Phthalylsulfathiazole.Experimental
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Rosiglitazone.Approved, Investigational
Pipemidic acidThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Pipemidic acid.Experimental
PiperazineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Piperazine.Approved, Vet Approved
PiperineThe metabolism of Rosiglitazone can be decreased when combined with Piperine.Investigational
PipotiazineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pipotiazine.Approved, Investigational
PiretanideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Piretanide.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Rosiglitazone.Approved
Piromidic acidThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Piromidic acid.Experimental
PitavastatinThe excretion of Pitavastatin can be decreased when combined with Rosiglitazone.Approved
PitolisantThe serum concentration of Rosiglitazone can be decreased when it is combined with Pitolisant.Approved, Investigational
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
PolythiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Polythiazide.Approved
PosaconazoleThe metabolism of Rosiglitazone can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe excretion of Pravastatin can be decreased when combined with Rosiglitazone.Approved
PrednisoloneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Prednisone.Approved, Vet Approved
PregabalinThe risk or severity of heart failure can be increased when Pregabalin is combined with Rosiglitazone.Approved, Illicit, Investigational
PrimidoneThe metabolism of Rosiglitazone can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Probenecid.Approved, Investigational
ProgesteroneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Progesterone.Approved, Vet Approved
Propatyl nitrateThe risk or severity of adverse effects can be increased when Propatyl nitrate is combined with Rosiglitazone.Experimental, Investigational
ProtriptylineProtriptyline may decrease the hypoglycemic activities of Rosiglitazone.Approved
PrulifloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Prulifloxacin.Investigational
QuetiapineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Quinethazone.Approved
QuinineThe metabolism of Rosiglitazone can be increased when combined with Quinine.Approved
QuinupramineQuinupramine may decrease the hypoglycemic activities of Rosiglitazone.Experimental
RabeprazoleThe metabolism of Rosiglitazone can be decreased when combined with Rabeprazole.Approved, Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Rosiglitazone.Approved
RepaglinideRosiglitazone may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RifampicinThe metabolism of Rosiglitazone can be increased when combined with Rifampicin.Approved
RifamycinThe metabolism of Rosiglitazone can be increased when combined with Rifamycin.Investigational
RifapentineThe metabolism of Rosiglitazone can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe metabolism of Rosiglitazone can be increased when combined with Rifaximin.Approved, Investigational
RimexoloneThe metabolism of Rosiglitazone can be increased when combined with Rimexolone.Approved
RisperidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Risperidone.Approved, Investigational
RitanserinRitanserin may increase the hypoglycemic activities of Rosiglitazone.Investigational
RitonavirThe metabolism of Rosiglitazone can be decreased when combined with Ritonavir.Approved, Investigational
RivoglitazoneThe metabolism of Rivoglitazone can be decreased when combined with Rosiglitazone.Experimental, Investigational
RosoxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Rosoxacin.Approved, Investigational
RosuvastatinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Rosuvastatin.Approved
RufloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Rufloxacin.Experimental
SafinamideSafinamide may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
SafrazineSafrazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational, Vet Approved
SaquinavirThe metabolism of Rosiglitazone can be decreased when combined with Saquinavir.Approved, Investigational
SarafloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sarafloxacin.Vet Approved, Withdrawn
SarilumabThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Sarilumab.Approved, Investigational
SecobarbitalThe metabolism of Rosiglitazone can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational, Vet Approved
SertralineSertraline may increase the hypoglycemic activities of Rosiglitazone.Approved
SetrobuvirThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Setrobuvir.Investigational
SildenafilThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Rosiglitazone can be decreased when it is combined with Siltuximab.Approved, Investigational
Silver sulfadiazineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Silver sulfadiazine.Approved, Vet Approved
SimeprevirThe serum concentration of Rosiglitazone can be increased when it is combined with Simeprevir.Approved
SimvastatinThe excretion of Simvastatin can be decreased when combined with Rosiglitazone.Approved
SirolimusThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Sirolimus.Approved, Investigational
SitafloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sitafloxacin.Experimental, Investigational
SparfloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sparfloxacin.Approved, Investigational
St. John's WortThe serum concentration of Rosiglitazone can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StanoloneStanolone may increase the hypoglycemic activities of Rosiglitazone.Illicit, Investigational
StanozololStanozolol may increase the hypoglycemic activities of Rosiglitazone.Approved, Vet Approved
StiripentolThe serum concentration of Rosiglitazone can be increased when it is combined with Stiripentol.Approved
SuccinylsulfathiazoleThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Succinylsulfathiazole.Experimental
SulfacetamideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfacetamide.Approved
SulfachlorpyridazineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfachlorpyridazine.Vet Approved
SulfacytineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfacytine.Approved
SulfadiazineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfadiazine.Approved, Investigational, Vet Approved
SulfadicramideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfadicramide.Experimental
SulfadimethoxineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfadimethoxine.Approved, Vet Approved
SulfadoxineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfadoxine.Approved, Investigational
SulfaethoxypyridazineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfaethoxypyridazine.Vet Approved
SulfaguanidineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfaguanidine.Experimental
SulfaisodimidineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfaisodimidine.Experimental
SulfamazoneThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfamazone.Experimental
SulfamerazineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfamerazine.Approved, Vet Approved
SulfameterThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfameter.Approved
SulfamethazineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfamethazine.Approved, Investigational, Vet Approved
SulfamethizoleThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfamethizole.Approved, Investigational, Vet Approved
SulfamethoxazoleThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfamethoxazole.Approved
SulfamethoxypyridazineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfamethoxypyridazine.Experimental
SulfametomidineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfametomidine.Experimental
SulfametopyrazineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfametopyrazine.Approved, Withdrawn
SulfamoxoleThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfamoxole.Approved
SulfanilamideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfanilamide.Approved
SulfanitranThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfanitran.Vet Approved
SulfaperinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfaperin.Experimental
SulfaphenazoleThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfaphenazole.Approved
SulfapyridineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfapyridine.Approved
SulfaquinoxalineThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfaquinoxaline.Vet Approved
SulfasalazineSulfasalazine may increase the hypoglycemic activities of Rosiglitazone.Approved
SulfathiazoleThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfathiazole.Approved, Vet Approved
SulfathioureaThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfathiourea.Experimental
SulfatolamideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfatolamide.Experimental
SulfisoxazoleThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sumatriptan.Approved, Investigational
SunitinibRosiglitazone may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Tacrolimus.Approved, Investigational
TamoxifenThe metabolism of Rosiglitazone can be decreased when combined with Tamoxifen.Approved
Technetium Tc-99m ciprofloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Technetium Tc-99m ciprofloxacin.Investigational
TelaprevirThe metabolism of Rosiglitazone can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Rosiglitazone can be decreased when combined with Telithromycin.Approved
TemafloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Temafloxacin.Withdrawn
TemsirolimusThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Temsirolimus.Approved
TenitramineThe risk or severity of adverse effects can be increased when Tenitramine is combined with Rosiglitazone.Experimental
TestosteroneTestosterone may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
Testosterone cypionateTestosterone cypionate may increase the hypoglycemic activities of Rosiglitazone.Approved
Testosterone enanthateTestosterone enanthate may increase the hypoglycemic activities of Rosiglitazone.Approved
Testosterone propionateTestosterone propionate may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational, Vet Approved, Withdrawn
Testosterone undecanoateTestosterone undecanoate may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
TianeptineTianeptine may decrease the hypoglycemic activities of Rosiglitazone.Approved, Investigational
TipranavirThe metabolism of Rosiglitazone can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Rosiglitazone can be decreased when it is combined with Tocilizumab.Approved
TolazamideThe therapeutic efficacy of Tolazamide can be increased when used in combination with Rosiglitazone.Approved, Investigational
TolbutamideThe therapeutic efficacy of Tolbutamide can be increased when used in combination with Rosiglitazone.Approved, Investigational
ToloxatoneToloxatone may increase the hypoglycemic activities of Rosiglitazone.Approved
TorasemideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Torasemide.Approved
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
TrazodoneTrazodone may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
TriamcinoloneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrimethoprimThe metabolism of Rosiglitazone can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimipramineTrimipramine may decrease the hypoglycemic activities of Rosiglitazone.Approved
TriptorelinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Rosiglitazone.Investigational, Withdrawn
Trolamine salicylateTrolamine salicylate may increase the hypoglycemic activities of Rosiglitazone.Approved
TroleandomycinThe metabolism of Rosiglitazone can be decreased when combined with Troleandomycin.Approved
TrolnitrateThe risk or severity of adverse effects can be increased when Trolnitrate is combined with Rosiglitazone.Experimental
TrovafloxacinThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Trovafloxacin.Approved, Investigational, Withdrawn
UbidecarenoneThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Ubidecarenone.Approved, Investigational, Nutraceutical
Valproic AcidThe metabolism of Rosiglitazone can be decreased when combined with Valproic Acid.Approved, Investigational
VemurafenibThe serum concentration of Rosiglitazone can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the hypoglycemic activities of Rosiglitazone.Approved
VerapamilThe metabolism of Rosiglitazone can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Rosiglitazone can be decreased when combined with Voriconazole.Approved, Investigational
VorinostatThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Vorinostat.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Rosiglitazone.Approved, Investigational
XipamideThe therapeutic efficacy of Rosiglitazone can be increased when used in combination with Xipamide.Experimental
ZimelidineZimelidine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
ZiprasidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Ziprasidone.Approved
Food Interactions
Not Available

References

Synthesis Reference

Manne Reddy, "Amorphous form of rosiglitazone maleate and process for preparation thereof." U.S. Patent US20040242658, issued December 02, 2004.

US20040242658
General References
  1. Mohanty P, Aljada A, Ghanim H, Hofmeyer D, Tripathy D, Syed T, Al-Haddad W, Dhindsa S, Dandona P: Evidence for a potent antiinflammatory effect of rosiglitazone. J Clin Endocrinol Metab. 2004 Jun;89(6):2728-35. [PubMed:15181049]
  2. Kahn SE, Haffner SM, Heise MA, Herman WH, Holman RR, Jones NP, Kravitz BG, Lachin JM, O'Neill MC, Zinman B, Viberti G: Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N Engl J Med. 2006 Dec 7;355(23):2427-43. Epub 2006 Dec 4. [PubMed:17145742]
External Links
Human Metabolome Database
HMDB0005031
KEGG Drug
D00596
PubChem Compound
77999
PubChem Substance
46504556
ChemSpider
70383
BindingDB
28681
ChEBI
50122
ChEMBL
CHEMBL121
Therapeutic Targets Database
DAP000271
PharmGKB
PA451283
IUPHAR
1056
Guide to Pharmacology
GtP Drug Page
HET
BRL
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Rosiglitazone
ATC Codes
A10BD03 — Metformin and rosiglitazoneA10BG02 — RosiglitazoneA10BD04 — Glimepiride and rosiglitazone
AHFS Codes
  • 68:20.28 — Thiazolidinediones
FDA label
Download (86.2 KB)
MSDS
Download (30 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentNeoplasms1
1CompletedNot AvailableHuman Immunodeficiency Virus (HIV) Infections1
1CompletedNot AvailableType 2 Diabetes Mellitus1
1CompletedBasic ScienceAlzheimer's Disease (AD) / Metabolism1
1CompletedBasic ScienceDrug Interactions1
1CompletedBasic ScienceHealthy Volunteers3
1CompletedDiagnosticBMI >30 kg/m2 / Healthy Volunteers / Type 2 Diabetes Mellitus1
1CompletedTreatmentAlzheimer's Disease (AD)1
1CompletedTreatmentAnemias / Healthy Volunteers1
1CompletedTreatmentAsthma Bronchial1
1CompletedTreatmentCancer, Breast1
1CompletedTreatmentErectile Dysfunction (ED)1
1CompletedTreatmentFollicular Thyroid Cancer / Huerthle Cell Thyroid Cancer / Renal Cell Adenocarcinoma / Thyroid Papillary Carcinoma1
1CompletedTreatmentGlomerulosclerosis, Focal Segmental1
1CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1CompletedTreatmentProphylaxis against postoperative nausea and vomiting / Prophylaxis of acute chemotherapy induced nausea and vomiting1
1CompletedTreatmentSolid Cancers1
1CompletedTreatmentType 2 Diabetes Mellitus2
1TerminatedTreatmentPlasmodium Infections1
1, 2CompletedTreatmentBody Weight Changes / HIV-Associated Lipodystrophy Syndrome / Human Immunodeficiency Virus (HIV) Infections / Insulin Resistance / Metabolic Syndromes1
1, 2CompletedTreatmentMalaria caused by Plasmodium falciparum1
1, 2Unknown StatusTreatmentUlcerative Colitis (UC)1
2CompletedBasic ScienceChange in Bone Marrow Fat Content / Change in Bone Mineral Density1
2CompletedBasic ScienceInsulin Resistance / Metabolic Syndromes1
2CompletedPreventionIschemia-Reperfusion Injury / The Metabolic Syndrome1
2CompletedPreventionOral Leukoplakia1
2CompletedTreatmentAlzheimer's Disease (AD)3
2CompletedTreatmentAsthma Bronchial1
2CompletedTreatmentBMI >30 kg/m2 / Hyperinsulinemia / Insulin Resistance1
2CompletedTreatmentCongestive Heart Failure (CHF)1
2CompletedTreatmentCutaneous T-Cell Lymphoma (CTCL) / Mycosis Fungoides (MF) / Sezary Syndrome1
2CompletedTreatmentDiabetes Mellitus (DM) / Insulin Resistance1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Hyperlipidemias1
2CompletedTreatmentImpaired Glucose Tolerance (IGT) / Metabolic Syndromes1
2CompletedTreatmentInflammatory Bowel Diseases (IBD) / Ulcerative Colitis (UC)1
2CompletedTreatmentNon Alcoholic Steatohepatitis1
2CompletedTreatmentSarcomas1
2CompletedTreatmentTransplant, Kidney1
2CompletedTreatmentType 2 Diabetes Mellitus1
2CompletedTreatmentType 2 Diabetes Mellitus With Features of Insulin Resistance1
2TerminatedTreatmentBrain and Central Nervous System Tumors1
2TerminatedTreatmentCushing's Disease1
2TerminatedTreatmentEndometriosis1
2Unknown StatusTreatmentHead and Neck Carcinoma1
2Unknown StatusTreatmentMild Cognitive Impairment (MCI)1
2Unknown StatusTreatmentNonalcoholic Fatty Liver Disease / Nonalcoholic Steatohepatitis1
2, 3CompletedNot AvailablePre-Diabetic1
2, 3CompletedTreatmentAsthma Bronchial1
2, 3WithdrawnDiagnosticEndometriosis1
2, 3WithdrawnTreatmentChronic Kidney Disease (CKD) / Inflammatory Reaction1
3CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Blood Cholesterol Level / High Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
3CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Impaired Glucose Tolerance (IGT) / Isolated Impaired Fasting Glucose1
3CompletedPreventionCardiovascular Disease (CVD) / Glucose Metabolism Disorders / Impaired Glucose Tolerance (IGT)1
3CompletedPreventionCoronary Artery Bypass Grafting (CABG) Surgery / Diabetes Mellitus (DM)1
3CompletedPreventionDiabetes Mellitus (DM) / Impaired Glucose Tolerance (IGT)1
3CompletedTreatmentAdenocarcinoma of the Prostate / Prostate Cancer1
3CompletedTreatmentAlzheimer's Disease (AD)2
3CompletedTreatmentAtherosclerosis / Cardiovascular Disease (CVD) / Type 2 Diabetes Mellitus1
3CompletedTreatmentDiabetes Mellitus (DM)1
3CompletedTreatmentDiabetes Mellitus (DM) / Impaired Glucose Tolerance (IGT)1
3CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus3
3CompletedTreatmentDiabetes Mellitus Non Insulin Dependent Oral Agent Therapy1
3CompletedTreatmentDiabetic Neuropathies / Type 2 Diabetes Mellitus1
3CompletedTreatmentHyperlipidemias / Type 2 Diabetes Mellitus1
3CompletedTreatmentInsulin Resistance1
3CompletedTreatmentMicroalbuminuria / Type 2 Diabetes Mellitus1
3CompletedTreatmentType 2 Diabetes Mellitus18
3TerminatedTreatmentChronic Kidney Disease (CKD) / Insulin Resistance1
3TerminatedTreatmentDiabetes Mellitus (DM)1
3TerminatedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus3
3TerminatedTreatmentDyslipidemias / Glucose Metabolism Disorders1
3TerminatedTreatmentMetabolic Syndromes1
3TerminatedTreatmentType 2 Diabetes Mellitus1
3Unknown StatusPreventionGlucose tolerance impaired1
3Unknown StatusTreatmentCritical Illness / Multiple Organ Failure1
3Unknown StatusTreatmentHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus / Vascular Diseases1
4CompletedNot AvailableBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
4CompletedBasic ScienceInflammatory Bowel Diseases (IBD)1
4CompletedPreventionBMI >30 kg/m2 / Menopause / Type 2 Diabetes Mellitus1
4CompletedPreventionSchizophrenic Disorders1
4CompletedPreventionType 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus2
4CompletedTreatmentDiabetes, Diabetes Mellitus Type 1 / Puberty: >Tanner 2 Breast Development or Testis >4ml1
4CompletedTreatmentHepatitis C Viral Infection1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedTreatmentImpaired Glucose Tolerance (IGT)1
4CompletedTreatmentInsulin Resistance / Metabolic Syndromes2
4CompletedTreatmentInsulin Sensitivity1
4CompletedTreatmentInsulin Sensitivity / Type 2 Diabetes Mellitus1
4CompletedTreatmentMetabolic Syndromes1
4CompletedTreatmentPolycystic Ovaries Syndrome1
4CompletedTreatmentType 2 Diabetes Mellitus14
4CompletedTreatmentType 2 Diabetes Mellitus / Vascular Diseases1
4TerminatedPreventionNASH (Non-alcoholic Steato-hepatitis)1
4TerminatedTreatmentAngina Pectoris / Metabolic Syndromes1
4TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection / Fatty Liver1
4TerminatedTreatmentCoronary Artery Disease1
4TerminatedTreatmentFatty Liver / Hepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) / Liver Diseases / Steatosis1
4TerminatedTreatmentHypertriglyceridemia in Type 4 Hyperlipidemia / Non Diabetic Subjects With Normoglycemia1
4TerminatedTreatmentType 2 Diabetes Mellitus1
4Unknown StatusTreatmentImpaired Glucose Tolerance (IGT)1
4WithdrawnTreatmentAngina Pectoris / Type 2 Diabetes Mellitus1
Not AvailableActive Not RecruitingBasic SciencePolycystic Ovaries Syndrome1
Not AvailableCompletedNot AvailableCarotid Atherosclerosis / Metabolic Syndromes / Strokes / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableType 2 Diabetes Mellitus7
Not AvailableCompletedPreventionBMI >30 kg/m2 / Impaired Glucose Tolerance (IGT) / Type 2 Diabetes Mellitus1
Not AvailableCompletedScreeningDiabetes Mellitus (DM)1
Not AvailableCompletedTreatmentAlzheimer's Disease (AD)1
Not AvailableCompletedTreatmentAtherosclerosis / Human Immunodeficiency Virus (HIV) Infections1
Not AvailableCompletedTreatmentBipolar Disorder (BD) / Depression / Insulin Resistance1
Not AvailableCompletedTreatmentHealthy Volunteers2
Not AvailableCompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Hyperinsulinemia / Lipodystrophies1
Not AvailableCompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Insulin Resistance1
Not AvailableCompletedTreatmentHypertriglyceridemias / Insulin Resistance1
Not AvailableCompletedTreatmentInsulin Resistance2
Not AvailableCompletedTreatmentOvert Diabetic Nephropathy / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus3
Not AvailableRecruitingTreatmentPituitary Neoplasms1
Not AvailableRecruitingTreatmentPlasmodium Infections1
Not AvailableSuspendedTreatmentDiabetes Mellitus, Atherosclerosis1
Not AvailableTerminatedNot AvailableCongestive Cardiomyopathy1
Not AvailableTerminatedBasic ScienceFatty Liver / Insulin Resistance1
Not AvailableTerminatedDiagnosticType 2 Diabetes Mellitus1
Not AvailableTerminatedPreventionType 2 Diabetes Mellitus1
Not AvailableUnknown StatusTreatmentCardiovascular Disease (CVD) / Disease, Chronic / Kidney Diseases1
Not AvailableWithdrawnTreatmentBladder Cancers1

Pharmacoeconomics

Manufacturers
  • Sb pharmco puerto rico inc
  • Glaxosmithkline
Packagers
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Cardinal Health
  • Diversified Healthcare Services Inc.
  • GlaxoSmithKline Inc.
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • PD-Rx Pharmaceuticals Inc.
  • Pharmacy Service Center
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Resource Optimization and Innovation LLC
  • Searle and Co.
  • Southwood Pharmaceuticals
  • Tya Pharmaceuticals
  • Vangard Labs Inc.
  • West-Ward Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral
Tablet, film coatedOral
TabletOral2 mg
TabletOral4 mg
TabletOral8 mg
Tablet, film coatedOral2 mg/1
Tablet, film coatedOral2 mg
Tablet, film coatedOral4 mg
Tablet, film coatedOral8 mg/1
Tablet, film coatedOral8 mg
Tablet, film coatedOral4 mg/1
Prices
Unit descriptionCostUnit
Avandia 8 mg tablet8.69USD tablet
Avandia 4 mg tablet4.72USD tablet
Avandia 2 mg tablet3.22USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5002953No1994-09-172011-09-17Us
CA2143849No2000-04-252013-09-01Canada
CA1328452No1994-04-122011-04-12Canada
US5965584No1996-06-192016-06-19Us
US6166042No1996-06-192016-06-19Us
US6288095Yes1997-08-112017-08-11Us
US7358366Yes2000-10-192020-10-19Us
US8236345No2002-10-072022-10-07Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)122-123 °CNot Available
logP2.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.038 mg/mLALOGPS
logP2.95ALOGPS
logP2.45ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)6.84ChemAxon
pKa (Strongest Basic)6.23ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area71.53 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity97.79 m3·mol-1ChemAxon
Polarizability37.8 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9861
Blood Brain Barrier+0.8994
Caco-2 permeable-0.5451
P-glycoprotein substrateSubstrate0.6535
P-glycoprotein inhibitor INon-inhibitor0.5274
P-glycoprotein inhibitor IINon-inhibitor0.6289
Renal organic cation transporterNon-inhibitor0.5203
CYP450 2C9 substrateNon-substrate0.7418
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5744
CYP450 1A2 substrateInhibitor0.5391
CYP450 2C9 inhibitorInhibitor0.5783
CYP450 2D6 inhibitorNon-inhibitor0.846
CYP450 2C19 inhibitorInhibitor0.5884
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7213
Ames testNon AMES toxic0.687
CarcinogenicityNon-carcinogens0.9465
BiodegradationNot ready biodegradable0.8635
Rat acute toxicity2.4515 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8055
hERG inhibition (predictor II)Non-inhibitor0.7768
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
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0109000000-d527d5c2b5f1de352264
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4r-1609000000-585d240b82e4a1918a29
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0309000000-a9fa2307075b611cffcc

Taxonomy

Description
This compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenol ethers
Sub Class
Not Available
Direct Parent
Phenol ethers
Alternative Parents
Phenoxy compounds / Dialkylarylamines / Aminopyridines and derivatives / Alkyl aryl ethers / Imidolactams / Thiazolines / Heteroaromatic compounds / Organic carbonic acids and derivatives / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds
show 4 more
Substituents
Phenoxy compound / Phenol ether / Dialkylarylamine / Alkyl aryl ether / Aminopyridine / Monocyclic benzene moiety / Pyridine / Imidolactam / Heteroaromatic compound / Meta-thiazoline
show 15 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
aminopyridine, thiazolidenediones (CHEBI:50122)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE...
Gene Name
PPARG
Uniprot ID
P37231
Uniprot Name
Peroxisome proliferator-activated receptor gamma
Molecular Weight
57619.58 Da
References
  1. Su JL, Winegar DA, Wisely GB, Sigel CS, Hull-Ryde EA: Use of a PPAR gamma-specific monoclonal antibody to demonstrate thiazolidinediones induce PPAR gamma receptor expression in vitro. Hybridoma. 1999 Jun;18(3):273-80. [PubMed:10475242]
  2. Rieusset J, Auwerx J, Vidal H: Regulation of gene expression by activation of the peroxisome proliferator-activated receptor gamma with rosiglitazone (BRL 49653) in human adipocytes. Biochem Biophys Res Commun. 1999 Nov;265(1):265-71. [PubMed:10548525]
  3. Kameda N, Okuya S, Oka Y: [Rosiglitazone (BRL-49653)]. Nihon Rinsho. 2000 Feb;58(2):401-4. [PubMed:10707565]
  4. Johnson BA, Wilson EM, Li Y, Moller DE, Smith RG, Zhou G: Ligand-induced stabilization of PPARgamma monitored by NMR spectroscopy: implications for nuclear receptor activation. J Mol Biol. 2000 Apr 28;298(2):187-94. [PubMed:10764590]
  5. Camp HS, Li O, Wise SC, Hong YH, Frankowski CL, Shen X, Vanbogelen R, Leff T: Differential activation of peroxisome proliferator-activated receptor-gamma by troglitazone and rosiglitazone. Diabetes. 2000 Apr;49(4):539-47. [PubMed:10871190]
  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
Very long-chain fatty acid-coa ligase activity
Specific Function
Activation of long-chain fatty acids for both synthesis of cellular lipids, and degradation via beta-oxidation. Preferentially uses arachidonate and eicosapentaenoate as substrates.
Gene Name
ACSL4
Uniprot ID
O60488
Uniprot Name
Long-chain-fatty-acid--CoA ligase 4
Molecular Weight
79187.38 Da
References
  1. Askari B, Kanter JE, Sherrid AM, Golej DL, Bender AT, Liu J, Hsueh WA, Beavo JA, Coleman RA, Bornfeldt KE: Rosiglitazone inhibits acyl-CoA synthetase activity and fatty acid partitioning to diacylglycerol and triacylglycerol via a peroxisome proliferator-activated receptor-gamma-independent mechanism in human arterial smooth muscle cells and macrophages. Diabetes. 2007 Apr;56(4):1143-52. Epub 2007 Jan 26. [PubMed:17259370]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleyleth...
Gene Name
PPARA
Uniprot ID
Q07869
Uniprot Name
Peroxisome proliferator-activated receptor alpha
Molecular Weight
52224.595 Da
References
  1. Inoue I, Itoh F, Aoyagi S, Tazawa S, Kusama H, Akahane M, Mastunaga T, Hayashi K, Awata T, Komoda T, Katayama S: Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB. Biochem Biophys Res Commun. 2002 Jan 11;290(1):131-9. [PubMed:11779144]
  2. Drevon CA: Fatty acids and expression of adipokines. Biochim Biophys Acta. 2005 May 30;1740(2):287-92. Epub 2004 Dec 8. [PubMed:15949695]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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-lin...
Gene Name
PPARD
Uniprot ID
Q03181
Uniprot Name
Peroxisome proliferator-activated receptor delta
Molecular Weight
49902.99 Da
References
  1. Inoue I, Itoh F, Aoyagi S, Tazawa S, Kusama H, Akahane M, Mastunaga T, Hayashi K, Awata T, Komoda T, Katayama S: Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB. Biochem Biophys Res Commun. 2002 Jan 11;290(1):131-9. [PubMed:11779144]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expressi...
Gene Name
RXRA
Uniprot ID
P19793
Uniprot Name
Retinoic acid receptor RXR-alpha
Molecular Weight
50810.835 Da
References
  1. Sarath Josh MK, Pradeep S, Vijayalekshmi Amma KS, Balachandran S, Abdul Jaleel UC, Doble M, Spener F, Benjamin S: Phthalates efficiently bind to human peroxisome proliferator activated receptor and retinoid X receptor alpha, beta, gamma subtypes: an in silico approach. J Appl Toxicol. 2014 Jul;34(7):754-65. doi: 10.1002/jat.2902. Epub 2013 Jul 11. [PubMed:23843199]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expressi...
Gene Name
RXRB
Uniprot ID
P28702
Uniprot Name
Retinoic acid receptor RXR-beta
Molecular Weight
56921.38 Da
References
  1. Sarath Josh MK, Pradeep S, Vijayalekshmi Amma KS, Balachandran S, Abdul Jaleel UC, Doble M, Spener F, Benjamin S: Phthalates efficiently bind to human peroxisome proliferator activated receptor and retinoid X receptor alpha, beta, gamma subtypes: an in silico approach. J Appl Toxicol. 2014 Jul;34(7):754-65. doi: 10.1002/jat.2902. Epub 2013 Jul 11. [PubMed:23843199]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expressi...
Gene Name
RXRG
Uniprot ID
P48443
Uniprot Name
Retinoic acid receptor RXR-gamma
Molecular Weight
50870.72 Da
References
  1. Sarath Josh MK, Pradeep S, Vijayalekshmi Amma KS, Balachandran S, Abdul Jaleel UC, Doble M, Spener F, Benjamin S: Phthalates efficiently bind to human peroxisome proliferator activated receptor and retinoid X receptor alpha, beta, gamma subtypes: an in silico approach. J Appl Toxicol. 2014 Jul;34(7):754-65. doi: 10.1002/jat.2902. Epub 2013 Jul 11. [PubMed:23843199]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. 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
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]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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
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. 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
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 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
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 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
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Jaakkola T, Backman JT, Neuvonen M, Neuvonen PJ: Effects of gemfibrozil, itraconazole, and their combination on the pharmacokinetics of pioglitazone. Clin Pharmacol Ther. 2005 May;77(5):404-14. doi: 10.1016/j.clpt.2004.12.266. [PubMed:15900286]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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 colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Nozawa T, Sugiura S, Nakajima M, Goto A, Yokoi T, Nezu J, Tsuji A, Tamai I: Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. Drug Metab Dispos. 2004 Mar;32(3):291-4. [PubMed:14977862]
  2. Karlgren M, Ahlin G, Bergstrom CA, Svensson R, Palm J, Artursson P: In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions. Pharm Res. 2012 Feb;29(2):411-26. doi: 10.1007/s11095-011-0564-9. Epub 2011 Aug 23. [PubMed:21861202]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]

Drug created on June 13, 2005 07:24 / Updated on August 15, 2018 09:39