Identification

Name
Lobeglitazone
Accession Number
DB09198
Type
Small Molecule
Groups
Approved
Description

Lobeglitazone is an antidiabetic medication from the thiazolidinedione class of drugs. It primarily functions as an insulin sensitizer by binding and activating Peroxisome Proliferator-Activated Receptors (PPAR) gamma within fat cells. By activating PPAR-gamma and promoting the binding of insulin at fat cells, lobeglitazone thereby has been shown to reduce blood sugar levels, lower hemoglobain A1C (HbA1C) levels, and improve lipid and liver profiles [1]. Unlike Pioglitazone, which is a dual PPAR agonist at PPAR-alpha and PPAR-gamma, Lobeglitazone is a pure PPAR-alpha agonist.

Lobeglitazone was approved by the Ministry of Food and Drug Safety (South Korea) in 2013, and is being monitored by postmarketing surveillance until 2019. Lobeglitazone is not approved for use by either the Food and Drug Administration (USA), Health Canada, or by the European Medicines Agency for use in the management of diabetes.

Structure
Thumb
Synonyms
Not Available
External IDs
CKD 501 / CKD-501 / CKD501
Product Ingredients
IngredientUNIICASInChI Key
lobeglitazone sulfate95C712E83PNot AvailableNot applicable
International/Other Brands
Duvie (Chong Kun Dang)
Categories
UNII
MY89F08K5D
CAS number
607723-33-1
Weight
Average: 480.54
Monoisotopic: 480.146741063
Chemical Formula
C24H24N4O5S
InChI Key
CHHXEZSCHQVSRE-UHFFFAOYSA-N
InChI
InChI=1S/C24H24N4O5S/c1-28(21-14-22(26-15-25-21)33-19-9-7-17(31-2)8-10-19)11-12-32-18-5-3-16(4-6-18)13-20-23(29)27-24(30)34-20/h3-10,14-15,20H,11-13H2,1-2H3,(H,27,29,30)
IUPAC Name
5-{[4-(2-{[6-(4-methoxyphenoxy)pyrimidin-4-yl](methyl)amino}ethoxy)phenyl]methyl}-1,3-thiazolidine-2,4-dione
SMILES
COC1=CC=C(OC2=NC=NC(=C2)N(C)CCOC2=CC=C(CC3SC(=O)NC3=O)C=C2)C=C1

Pharmacology

Indication

Lobeglitazone was approved by the Ministry of Food and Drug Safety (South Korea) in 2013, and is being monitored by postmarketing surveillance until 2019. Lobeglitazone is not approved for use by either the Food and Drug Administration (USA), Health Canada, or by the European Medicines Agency for use in the management of diabetes.

Structured Indications
Not Available
Pharmacodynamics
Not Available
Mechanism of action

Lobeglitazone acts as an insulin sensitizer by binding and activating Peroxisome Proliferator-Activated Receptors (PPAR) gamma within fat cells. By promoting the binding of insulin at fat cells, lobeglitazone has been shown to reduce blood sugar levels, lower hemoglobain A1C (HbA1C) levels, and improve lipid and liver profiles [1]. Unlike Pioglitazone, which is a dual PPAR agonist at PPAR-alpha and PPAR-gamma, Lobeglitazone is a pure PPAR-alpha agonist.

TargetActionsOrganism
APeroxisome proliferator-activated receptor gamma
activator
Human
Absorption

In rat studies, the AUC for the doses 0.5, 1, and 2 mg/kg, AUC values were determined to be 459, 514, and 481 ug min/mL respectively. Absoprtion occurs rapidly after administration, with Tmax of 67.5 and 48.8 min and a Cmax of 0.962 and 0.4.94 ug/mL following doses of 0.5 and 2 mg/kg, respectively. Absolute bioavailability after oral administration was nearly complete and apparently not affected by the dosage; 92.1% following a 0.5 mg/kg dose and 99.0% following a 2 mg/kg dose. Furthermore, the extent of LB remaining in the GI tract at 24 h was found to be negligible, with values less than 0.2% of the oral dose, suggesting that the intestinal absorption is complete in rats at the dose range studied [2].

Volume of distribution

The steady state volume of distribution (Vss) of lobeglitazone was found to be 189–276 mL/kg. Vss was not found to vary statistically with the dose, suggesting that lobeglitazone follows linear kinetics [2].

Protein binding

Lobeglitazone was found to bind extensively to plasma proteins (i.e., up to 99.9%) with no appreciable concentration dependency on the unbound fraction [2].

Metabolism

Rat studies with lobeglitazone have suggested that it is primarily metabolized by cytochrome P450 (CYP) isozymes [2], however the exact enzymes involved in its metabolism have yet to be elucidated. The structure of Lobeglitazone's five major metabolites have been characterized along with their pharmacokinetic parameters, and can be seen in the metabolism section below. In rat studies, demethylation and hydroxylation appear to be the primary metabolic pathways. The most abundant metabolite found in these studies was confirmed in vivo as M1, a demethylated derivative of lobeglitazone; its rate of formation was found to be approximately 0.216 ∼ 0.252 mL/min/kg, representing approximately 9.76% of the total lobeglitazone elimination in vivo in rats [5].

Route of elimination

It has been reported that the combined extent of the excretion of lobeglitazone to the bile, urine and intestine is low (less than 10% of total dose), suggesting that the major route of elimination for the drug involves its metabolism [2].

Half life

Following an intravenous dosage of 1 mg/kg, the half life was found to be 110 min [2].

Clearance

In rat studies, systemic clearance was found to be between 1.95 and 2.19 mL/min/kg regardless of dosage [2].

Toxicity

Lobeglitazone showed a similar adverse effect profile to pioglitazone, another thiazolidinedione medication from the same class. The most concerning side effects found were edema and weight gain, with no severe adverse effects. Notably, there were no observable changes to patients with heart failure, which is a concern associated with other medications of the same class [3].

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AceclofenacThe metabolism of Aceclofenac can be decreased when combined with Lobeglitazone.Approved
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Lobeglitazone.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Lobeglitazone.Approved
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be decreased when combined with Lobeglitazone.Approved, Vet Approved
AdinazolamThe metabolism of Adinazolam can be decreased when combined with Lobeglitazone.Approved
AgomelatineThe serum concentration of Agomelatine can be increased when it is combined with Lobeglitazone.Approved, Investigational
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Lobeglitazone.Approved, Vet Approved
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Lobeglitazone.Approved, Investigational
AlosetronThe metabolism of Alosetron can be decreased when combined with Lobeglitazone.Approved, Withdrawn
AlprazolamThe metabolism of Alprazolam can be decreased when combined with Lobeglitazone.Approved, Illicit, Investigational
AmbrisentanThe metabolism of Ambrisentan can be decreased when combined with Lobeglitazone.Approved, Investigational
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Lobeglitazone.Approved, Withdrawn
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Lobeglitazone.Approved
AmiodaroneThe metabolism of Amiodarone can be decreased when combined with Lobeglitazone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Lobeglitazone.Approved
AmoxicillinThe metabolism of Amoxicillin can be decreased when combined with Lobeglitazone.Approved, Vet Approved
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Lobeglitazone.Approved
AnagrelideThe metabolism of Anagrelide can be decreased when combined with Lobeglitazone.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Lobeglitazone.Approved
ApixabanThe metabolism of Apixaban can be decreased when combined with Lobeglitazone.Approved
AprepitantThe metabolism of Aprepitant can be decreased when combined with Lobeglitazone.Approved, Investigational
Arachidonic AcidThe metabolism of Arachidonic Acid can be decreased when combined with Lobeglitazone.Experimental
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Lobeglitazone.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Lobeglitazone.Approved
AsenapineThe metabolism of Asenapine can be decreased when combined with Lobeglitazone.Approved
AtazanavirThe metabolism of Atazanavir can be decreased when combined with Lobeglitazone.Approved, Investigational
AtomoxetineThe metabolism of Atomoxetine can be decreased when combined with Lobeglitazone.Approved
AV650The metabolism of AV650 can be decreased when combined with Lobeglitazone.Approved, Investigational
AxitinibThe metabolism of Axitinib can be decreased when combined with Lobeglitazone.Approved, Investigational
AzelastineThe metabolism of Azelastine can be decreased when combined with Lobeglitazone.Approved
BendamustineThe metabolism of Bendamustine can be decreased when combined with Lobeglitazone.Approved, Investigational
BenzatropineThe metabolism of Benzatropine can be decreased when combined with Lobeglitazone.Approved
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Lobeglitazone.Approved
BetaxololThe metabolism of Betaxolol can be decreased when combined with Lobeglitazone.Approved
BexaroteneThe metabolism of Bexarotene can be decreased when combined with Lobeglitazone.Approved, Investigational
BortezomibThe metabolism of Bortezomib can be decreased when combined with Lobeglitazone.Approved, Investigational
BosentanThe serum concentration of Bosentan can be increased when it is combined with Lobeglitazone.Approved, Investigational
BrivaracetamThe metabolism of Brivaracetam can be decreased when combined with Lobeglitazone.Approved, Investigational
BromazepamThe metabolism of Bromazepam can be decreased when combined with Lobeglitazone.Approved, Illicit
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Lobeglitazone.Approved
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Lobeglitazone.Approved, Investigational
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Lobeglitazone.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Bupropion can be decreased when combined with Lobeglitazone.Approved
CabozantinibThe metabolism of Cabozantinib can be decreased when combined with Lobeglitazone.Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Lobeglitazone.Approved
CandesartanThe metabolism of Candesartan can be decreased when combined with Lobeglitazone.Approved
CarbamazepineThe metabolism of Carbamazepine can be decreased when combined with Lobeglitazone.Approved, Investigational
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Lobeglitazone.Approved
CarisoprodolThe metabolism of Carisoprodol can be decreased when combined with Lobeglitazone.Approved
CarmustineThe metabolism of Carmustine can be decreased when combined with Lobeglitazone.Approved
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Lobeglitazone.Approved, Investigational
CelecoxibThe metabolism of Celecoxib can be decreased when combined with Lobeglitazone.Approved, Investigational
ChloramphenicolThe metabolism of Chloramphenicol can be decreased when combined with Lobeglitazone.Approved, Vet Approved
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Lobeglitazone.Approved, Vet Approved
ChlorpropamideThe metabolism of Chlorpropamide can be decreased when combined with Lobeglitazone.Approved
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Lobeglitazone.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Lobeglitazone.Approved
CinacalcetThe metabolism of Cinacalcet can be decreased when combined with Lobeglitazone.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Lobeglitazone.Approved
CisaprideThe metabolism of Cisapride can be decreased when combined with Lobeglitazone.Approved, Investigational, Withdrawn
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Lobeglitazone.Approved
ClarithromycinThe metabolism of Clarithromycin can be decreased when combined with Lobeglitazone.Approved
ClenbuterolThe metabolism of Clenbuterol can be decreased when combined with Lobeglitazone.Approved, Vet Approved
ClevidipineThe metabolism of Clevidipine can be decreased when combined with Lobeglitazone.Approved
ClobazamThe metabolism of Clobazam can be decreased when combined with Lobeglitazone.Approved, Illicit
clomethiazoleThe metabolism of clomethiazole can be decreased when combined with Lobeglitazone.Investigational
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Lobeglitazone.Approved, Vet Approved
ClonidineThe metabolism of Clonidine can be decreased when combined with Lobeglitazone.Approved
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Lobeglitazone resulting in a loss in efficacy.Approved, Nutraceutical
ClotiazepamThe metabolism of Clotiazepam can be decreased when combined with Lobeglitazone.Approved, Illicit
ClozapineThe metabolism of Clozapine can be decreased when combined with Lobeglitazone.Approved
Conjugated estrogensThe metabolism of Conjugated estrogens can be decreased when combined with Lobeglitazone.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Lobeglitazone.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Lobeglitazone.Approved, Investigational
DacarbazineThe metabolism of Dacarbazine can be decreased when combined with Lobeglitazone.Approved, Investigational
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Lobeglitazone.Approved
DapsoneThe metabolism of Dapsone can be decreased when combined with Lobeglitazone.Approved, Investigational
DasatinibThe metabolism of Dasatinib can be decreased when combined with Lobeglitazone.Approved, Investigational
DaunorubicinThe metabolism of Daunorubicin can be decreased when combined with Lobeglitazone.Approved
DesipramineThe metabolism of Desipramine can be decreased when combined with Lobeglitazone.Approved
DeutetrabenazineThe metabolism of Deutetrabenazine can be decreased when combined with Lobeglitazone.Approved, Investigational
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Lobeglitazone.Approved, Illicit, Withdrawn
DexlansoprazoleThe metabolism of Dexlansoprazole can be decreased when combined with Lobeglitazone.Approved
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Lobeglitazone.Approved
DiazepamThe metabolism of Diazepam can be decreased when combined with Lobeglitazone.Approved, Illicit, Vet Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Lobeglitazone.Approved, Vet Approved
DicoumarolThe metabolism of Dicoumarol can be decreased when combined with Lobeglitazone.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Lobeglitazone.Approved
DinoprostoneThe metabolism of Dinoprostone can be decreased when combined with Lobeglitazone.Approved
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Lobeglitazone.Approved
DoconexentThe metabolism of Doconexent can be decreased when combined with Lobeglitazone.Investigational
DolasetronThe metabolism of Dolasetron can be decreased when combined with Lobeglitazone.Approved
DomperidoneThe metabolism of Domperidone can be decreased when combined with Lobeglitazone.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Lobeglitazone.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Lobeglitazone.Approved
DorzolamideThe metabolism of Dorzolamide can be decreased when combined with Lobeglitazone.Approved
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Lobeglitazone.Approved
DoxepinThe metabolism of Doxepin can be decreased when combined with Lobeglitazone.Approved
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Lobeglitazone.Approved, Illicit
DuloxetineThe metabolism of Duloxetine can be decreased when combined with Lobeglitazone.Approved
EletriptanThe metabolism of Eletriptan can be decreased when combined with Lobeglitazone.Approved, Investigational
EltrombopagThe metabolism of Eltrombopag can be decreased when combined with Lobeglitazone.Approved
EnasidenibThe metabolism of Enasidenib can be decreased when combined with Lobeglitazone.Approved
EnfuvirtideThe metabolism of Enfuvirtide can be decreased when combined with Lobeglitazone.Approved, Investigational
EpoprostenolThe metabolism of Epoprostenol can be decreased when combined with Lobeglitazone.Approved
ErgotamineThe metabolism of Ergotamine can be decreased when combined with Lobeglitazone.Approved
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Lobeglitazone.Approved, Investigational
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Lobeglitazone.Approved, Investigational
EsomeprazoleThe metabolism of Esomeprazole can be decreased when combined with Lobeglitazone.Approved, Investigational
EstradiolThe metabolism of Estradiol can be decreased when combined with Lobeglitazone.Approved, Investigational, Vet Approved
EstroneThe metabolism of Estrone can be decreased when combined with Lobeglitazone.Approved
Estrone sulfateThe metabolism of Estrone sulfate can be decreased when combined with Lobeglitazone.Approved
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Lobeglitazone.Approved
EthanolThe metabolism of Ethanol can be decreased when combined with Lobeglitazone.Approved
EtizolamThe metabolism of Etizolam can be decreased when combined with Lobeglitazone.Approved
EtodolacThe metabolism of Etodolac can be decreased when combined with Lobeglitazone.Approved, Investigational, Vet Approved
EtoposideThe metabolism of Etoposide can be decreased when combined with Lobeglitazone.Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Lobeglitazone.Approved, Investigational
EtravirineThe metabolism of Etravirine can be decreased when combined with Lobeglitazone.Approved
FamotidineThe metabolism of Famotidine can be decreased when combined with Lobeglitazone.Approved
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Lobeglitazone.Approved
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Lobeglitazone.Approved, Illicit
FluorouracilThe metabolism of Fluorouracil can be decreased when combined with Lobeglitazone.Approved
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Lobeglitazone.Approved, Vet Approved
FlurbiprofenThe metabolism of Flurbiprofen can be decreased when combined with Lobeglitazone.Approved, Investigational
FlutamideThe metabolism of Flutamide can be decreased when combined with Lobeglitazone.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Lobeglitazone.Approved
FluvoxamineThe metabolism of Fluvoxamine can be decreased when combined with Lobeglitazone.Approved, Investigational
FormoterolThe metabolism of Formoterol can be decreased when combined with Lobeglitazone.Approved, Investigational
FosphenytoinThe metabolism of Fosphenytoin can be decreased when combined with Lobeglitazone.Approved
FrovatriptanThe metabolism of Frovatriptan can be decreased when combined with Lobeglitazone.Approved, Investigational
GavestinelThe metabolism of Gavestinel can be decreased when combined with Lobeglitazone.Investigational
GenisteinThe metabolism of Genistein can be decreased when combined with Lobeglitazone.Investigational
GliclazideThe metabolism of Gliclazide can be decreased when combined with Lobeglitazone.Approved
GlimepirideThe metabolism of Glimepiride can be decreased when combined with Lobeglitazone.Approved
GlipizideThe metabolism of Glipizide can be decreased when combined with Lobeglitazone.Approved
GlucosamineThe metabolism of Glucosamine can be decreased when combined with Lobeglitazone.Approved
GlyburideThe metabolism of Glyburide can be decreased when combined with Lobeglitazone.Approved
GrepafloxacinThe metabolism of Grepafloxacin can be decreased when combined with Lobeglitazone.Withdrawn
GuanabenzThe metabolism of Guanabenz can be decreased when combined with Lobeglitazone.Approved
GuanfacineThe metabolism of Guanfacine can be decreased when combined with Lobeglitazone.Approved, Investigational
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Lobeglitazone.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Lobeglitazone.Approved, Vet Approved
HesperetinThe metabolism of Hesperetin can be decreased when combined with Lobeglitazone.Approved
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Lobeglitazone.Approved
HistamineThe metabolism of Histamine can be decreased when combined with Lobeglitazone.Approved, Investigational
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Lobeglitazone.Approved, Illicit
IbuprofenThe metabolism of Ibuprofen can be decreased when combined with Lobeglitazone.Approved
IcotinibThe metabolism of Icotinib can be decreased when combined with Lobeglitazone.Approved, Investigational
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Lobeglitazone.Approved
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Lobeglitazone.Approved
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Lobeglitazone.Approved
ImatinibThe metabolism of Imatinib can be decreased when combined with Lobeglitazone.Approved
ImipramineThe metabolism of Imipramine can be decreased when combined with Lobeglitazone.Approved
ImiquimodThe metabolism of Imiquimod can be decreased when combined with Lobeglitazone.Approved, Investigational
indisulamThe metabolism of indisulam can be decreased when combined with Lobeglitazone.Investigational
IndomethacinThe metabolism of Indomethacin can be decreased when combined with Lobeglitazone.Approved, Investigational
IrbesartanThe metabolism of Irbesartan can be decreased when combined with Lobeglitazone.Approved, Investigational
IxazomibThe metabolism of Ixazomib can be decreased when combined with Lobeglitazone.Approved
KetamineThe metabolism of Ketamine can be decreased when combined with Lobeglitazone.Approved, Vet Approved
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Lobeglitazone.Approved
KetoprofenThe metabolism of Ketoprofen can be decreased when combined with Lobeglitazone.Approved, Vet Approved
LansoprazoleThe metabolism of Lansoprazole can be decreased when combined with Lobeglitazone.Approved, Investigational
LapatinibThe metabolism of Lapatinib can be decreased when combined with Lobeglitazone.Approved, Investigational
LeflunomideThe metabolism of Leflunomide can be decreased when combined with Lobeglitazone.Approved, Investigational
LesinuradThe metabolism of Lesinurad can be decreased when combined with Lobeglitazone.Approved
LevobupivacaineThe metabolism of Levobupivacaine can be decreased when combined with Lobeglitazone.Approved
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Lobeglitazone.Approved
LicofeloneThe metabolism of Licofelone can be decreased when combined with Lobeglitazone.Investigational
LidocaineThe metabolism of Lidocaine can be decreased when combined with Lobeglitazone.Approved, Vet Approved
LomefloxacinThe metabolism of Lomefloxacin can be decreased when combined with Lobeglitazone.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Lobeglitazone.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Lobeglitazone.Approved
LornoxicamThe metabolism of Lornoxicam can be decreased when combined with Lobeglitazone.Approved
LosartanThe metabolism of Losartan can be decreased when combined with Lobeglitazone.Approved
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Lobeglitazone.Approved, Investigational
MacitentanThe metabolism of Macitentan can be decreased when combined with Lobeglitazone.Approved
MalathionThe metabolism of Malathion can be decreased when combined with Lobeglitazone.Approved, Investigational
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Lobeglitazone.Approved
Mefenamic acidThe metabolism of Mefenamic acid can be decreased when combined with Lobeglitazone.Approved
MelatoninThe metabolism of Melatonin can be decreased when combined with Lobeglitazone.Approved, Nutraceutical, Vet Approved
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Lobeglitazone.Approved, Vet Approved
MenadioneThe metabolism of Menadione can be decreased when combined with Lobeglitazone.Approved, Nutraceutical
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Lobeglitazone.Investigational, Withdrawn
MeprobamateThe metabolism of Meprobamate can be decreased when combined with Lobeglitazone.Approved, Illicit
MestranolThe metabolism of Mestranol can be decreased when combined with Lobeglitazone.Approved
MethadoneThe metabolism of Methadone can be decreased when combined with Lobeglitazone.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Lobeglitazone.Approved, Vet Approved
MethsuximideThe metabolism of Methsuximide can be decreased when combined with Lobeglitazone.Approved
MethylphenobarbitalThe metabolism of Methylphenobarbital can be decreased when combined with Lobeglitazone.Approved
MetoprololThe metabolism of Metoprolol can be decreased when combined with Lobeglitazone.Approved, Investigational
MetronidazoleThe metabolism of Metronidazole can be decreased when combined with Lobeglitazone.Approved
MexiletineThe metabolism of Mexiletine can be decreased when combined with Lobeglitazone.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Lobeglitazone.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Lobeglitazone.Approved
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Lobeglitazone.Approved
MontelukastThe metabolism of Montelukast can be decreased when combined with Lobeglitazone.Approved
muraglitazarThe metabolism of muraglitazar can be decreased when combined with Lobeglitazone.Investigational
NabumetoneThe metabolism of Nabumetone can be decreased when combined with Lobeglitazone.Approved
NaproxenThe metabolism of Naproxen can be decreased when combined with Lobeglitazone.Approved, Vet Approved
NateglinideThe metabolism of Nateglinide can be decreased when combined with Lobeglitazone.Approved, Investigational
NelfinavirThe metabolism of Nelfinavir can be decreased when combined with Lobeglitazone.Approved
NetupitantThe metabolism of Netupitant can be decreased when combined with Lobeglitazone.Approved
NevirapineThe metabolism of Nevirapine can be decreased when combined with Lobeglitazone.Approved
NiclosamideThe metabolism of Niclosamide can be decreased when combined with Lobeglitazone.Approved, Vet Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Lobeglitazone.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Lobeglitazone.Approved
NilutamideThe metabolism of Nilutamide can be decreased when combined with Lobeglitazone.Approved
Nitric OxideThe metabolism of Nitric Oxide can be decreased when combined with Lobeglitazone.Approved
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Lobeglitazone.Approved
OlanzapineThe metabolism of Olanzapine can be decreased when combined with Lobeglitazone.Approved, Investigational
OlodaterolThe metabolism of Olodaterol can be decreased when combined with Lobeglitazone.Approved
OmeprazoleThe metabolism of Omeprazole can be decreased when combined with Lobeglitazone.Approved, Investigational, Vet Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Lobeglitazone.Approved
OspemifeneThe metabolism of Ospemifene can be decreased when combined with Lobeglitazone.Approved
OxaliplatinThe metabolism of Oxaliplatin can be decreased when combined with Lobeglitazone.Approved, Investigational
OxaprozinThe metabolism of Oxaprozin can be decreased when combined with Lobeglitazone.Approved
OxiconazoleThe metabolism of Oxiconazole can be decreased when combined with Lobeglitazone.Approved
OxtriphyllineThe metabolism of Oxtriphylline can be decreased when combined with Lobeglitazone.Approved
PaclitaxelThe metabolism of Paclitaxel can be decreased when combined with Lobeglitazone.Approved, Vet Approved
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Lobeglitazone.Approved, Investigational
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Lobeglitazone.Approved
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Lobeglitazone.Approved
ParecoxibThe metabolism of Parecoxib can be decreased when combined with Lobeglitazone.Approved
PazopanibThe metabolism of Pazopanib can be decreased when combined with Lobeglitazone.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Lobeglitazone.Approved
PentobarbitalThe metabolism of Pentobarbital can be decreased when combined with Lobeglitazone.Approved, Vet Approved
PentoxifyllineThe metabolism of Pentoxifylline can be decreased when combined with Lobeglitazone.Approved, Investigational
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Lobeglitazone.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Lobeglitazone.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Lobeglitazone.Withdrawn
PhenobarbitalThe metabolism of Phenobarbital can be decreased when combined with Lobeglitazone.Approved
PhenprocoumonThe metabolism of Phenprocoumon can be decreased when combined with Lobeglitazone.Approved
PhenylbutazoneThe metabolism of Phenylbutazone can be decreased when combined with Lobeglitazone.Approved, Vet Approved
PhenytoinThe metabolism of Phenytoin can be decreased when combined with Lobeglitazone.Approved, Vet Approved
PimozideThe metabolism of Pimozide can be decreased when combined with Lobeglitazone.Approved
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Lobeglitazone.Approved, Investigational
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Lobeglitazone.Approved
PirfenidoneThe serum concentration of Pirfenidone can be increased when it is combined with Lobeglitazone.Investigational
PiroxicamThe metabolism of Piroxicam can be decreased when combined with Lobeglitazone.Approved, Investigational
PitavastatinThe metabolism of Pitavastatin can be decreased when combined with Lobeglitazone.Approved
PodofiloxThe metabolism of Podofilox can be decreased when combined with Lobeglitazone.Approved
PomalidomideThe metabolism of Pomalidomide can be decreased when combined with Lobeglitazone.Approved
PrasugrelThe metabolism of Prasugrel can be decreased when combined with Lobeglitazone.Approved
PravastatinThe metabolism of Pravastatin can be decreased when combined with Lobeglitazone.Approved
PraziquantelThe metabolism of Praziquantel can be decreased when combined with Lobeglitazone.Approved, Vet Approved
PrimaquineThe metabolism of Primaquine can be decreased when combined with Lobeglitazone.Approved
PrimidoneThe metabolism of Primidone can be decreased when combined with Lobeglitazone.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Lobeglitazone.Approved, Vet Approved
ProguanilThe metabolism of Proguanil can be decreased when combined with Lobeglitazone.Approved
PromazineThe metabolism of Promazine can be decreased when combined with Lobeglitazone.Approved, Vet Approved
PropafenoneThe metabolism of Propafenone can be decreased when combined with Lobeglitazone.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Lobeglitazone.Approved, Investigational, Vet Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Lobeglitazone.Approved, Investigational
PyrazinamideThe metabolism of Pyrazinamide can be decreased when combined with Lobeglitazone.Approved
QuazepamThe metabolism of Quazepam can be decreased when combined with Lobeglitazone.Approved, Illicit
QuetiapineThe metabolism of Quetiapine can be decreased when combined with Lobeglitazone.Approved
QuinidineThe metabolism of Quinidine can be decreased when combined with Lobeglitazone.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Lobeglitazone.Approved
RabeprazoleThe metabolism of Rabeprazole can be decreased when combined with Lobeglitazone.Approved, Investigational
RamelteonThe metabolism of Ramelteon can be decreased when combined with Lobeglitazone.Approved, Investigational
RanitidineThe metabolism of Ranitidine can be decreased when combined with Lobeglitazone.Approved
RasagilineThe metabolism of Rasagiline can be decreased when combined with Lobeglitazone.Approved
ResveratrolThe metabolism of Resveratrol can be decreased when combined with Lobeglitazone.Experimental, Investigational
RifabutinThe metabolism of Rifabutin can be decreased when combined with Lobeglitazone.Approved
RifampicinThe metabolism of Rifampicin can be decreased when combined with Lobeglitazone.Approved
RiluzoleThe metabolism of Riluzole can be decreased when combined with Lobeglitazone.Approved, Investigational
RitonavirThe metabolism of Ritonavir can be decreased when combined with Lobeglitazone.Approved, Investigational
RizatriptanThe metabolism of Rizatriptan can be decreased when combined with Lobeglitazone.Approved
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Lobeglitazone.Investigational, Withdrawn
RomidepsinThe metabolism of Romidepsin can be decreased when combined with Lobeglitazone.Approved, Investigational
RopiniroleThe metabolism of Ropinirole can be decreased when combined with Lobeglitazone.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Lobeglitazone.Approved
RosiglitazoneThe metabolism of Rosiglitazone can be decreased when combined with Lobeglitazone.Approved, Investigational
RosuvastatinThe metabolism of Rosuvastatin can be decreased when combined with Lobeglitazone.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Lobeglitazone.Approved
RucaparibThe metabolism of Rucaparib can be decreased when combined with Lobeglitazone.Approved, Investigational
RupatadineThe metabolism of Rupatadine can be decreased when combined with Lobeglitazone.Approved
Salicylic acidThe metabolism of Salicylic acid can be decreased when combined with Lobeglitazone.Approved, Vet Approved
SelegilineThe metabolism of Selegiline can be decreased when combined with Lobeglitazone.Approved, Investigational, Vet Approved
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Lobeglitazone.Approved
SertralineThe metabolism of Sertraline can be decreased when combined with Lobeglitazone.Approved
SildenafilThe metabolism of Sildenafil can be decreased when combined with Lobeglitazone.Approved, Investigational
SitaxentanThe metabolism of Sitaxentan can be decreased when combined with Lobeglitazone.Approved, Investigational, Withdrawn
StiripentolThe metabolism of Stiripentol can be decreased when combined with Lobeglitazone.Approved
SulfadiazineThe metabolism of Sulfadiazine can be decreased when combined with Lobeglitazone.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Sulfamethoxazole can be decreased when combined with Lobeglitazone.Approved
SulfamoxoleThe metabolism of Sulfamoxole can be decreased when combined with Lobeglitazone.Approved
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Lobeglitazone.Approved
SulfisoxazoleThe metabolism of Sulfisoxazole can be decreased when combined with Lobeglitazone.Approved, Vet Approved
SuprofenThe metabolism of Suprofen can be decreased when combined with Lobeglitazone.Approved, Withdrawn
TacrineThe metabolism of Tacrine can be decreased when combined with Lobeglitazone.Withdrawn
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Lobeglitazone.Approved
TapentadolThe metabolism of Tapentadol can be decreased when combined with Lobeglitazone.Approved
TelithromycinThe metabolism of Telithromycin can be decreased when combined with Lobeglitazone.Approved
TemafloxacinThe metabolism of Temafloxacin can be decreased when combined with Lobeglitazone.Withdrawn
TemazepamThe metabolism of Temazepam can be decreased when combined with Lobeglitazone.Approved
TeniposideThe metabolism of Teniposide can be decreased when combined with Lobeglitazone.Approved
TenoxicamThe metabolism of Tenoxicam can be decreased when combined with Lobeglitazone.Approved
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Lobeglitazone.Approved, Investigational, Vet Approved
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Lobeglitazone.Withdrawn
TestosteroneThe metabolism of Testosterone can be decreased when combined with Lobeglitazone.Approved, Investigational
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Lobeglitazone.Approved, Investigational, Withdrawn
TheobromineThe metabolism of Theobromine can be decreased when combined with Lobeglitazone.Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Lobeglitazone.Approved
ThiabendazoleThe metabolism of Thiabendazole can be decreased when combined with Lobeglitazone.Approved, Vet Approved
ThiamylalThe metabolism of Thiamylal can be decreased when combined with Lobeglitazone.Approved, Vet Approved
ThioridazineThe metabolism of Thioridazine can be decreased when combined with Lobeglitazone.Withdrawn
ThiothixeneThe metabolism of Thiothixene can be decreased when combined with Lobeglitazone.Approved
TiclopidineThe metabolism of Ticlopidine can be decreased when combined with Lobeglitazone.Approved
TimololThe metabolism of Timolol can be decreased when combined with Lobeglitazone.Approved
TipranavirThe metabolism of Tipranavir can be decreased when combined with Lobeglitazone.Approved, Investigational
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Lobeglitazone.Approved
TofacitinibThe metabolism of Tofacitinib can be decreased when combined with Lobeglitazone.Approved, Investigational
TolbutamideThe metabolism of Tolbutamide can be decreased when combined with Lobeglitazone.Approved
TolterodineThe metabolism of Tolterodine can be decreased when combined with Lobeglitazone.Approved, Investigational
TorasemideThe metabolism of Torasemide can be decreased when combined with Lobeglitazone.Approved
ToremifeneThe metabolism of Toremifene can be decreased when combined with Lobeglitazone.Approved, Investigational
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Lobeglitazone.Approved, Investigational
TreprostinilThe metabolism of Treprostinil can be decreased when combined with Lobeglitazone.Approved, Investigational
TretinoinThe metabolism of Tretinoin can be decreased when combined with Lobeglitazone.Approved, Investigational, Nutraceutical
TriamtereneThe metabolism of Triamterene can be decreased when combined with Lobeglitazone.Approved
TrifluoperazineThe metabolism of Trifluoperazine can be decreased when combined with Lobeglitazone.Approved
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Lobeglitazone.Approved
TrimethoprimThe metabolism of Trimethoprim can be decreased when combined with Lobeglitazone.Approved, Vet Approved
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Lobeglitazone.Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Lobeglitazone.Withdrawn
UlipristalThe metabolism of Ulipristal can be decreased when combined with Lobeglitazone.Approved
VadimezanThe metabolism of Vadimezan can be decreased when combined with Lobeglitazone.Investigational
ValdecoxibThe metabolism of Valdecoxib can be decreased when combined with Lobeglitazone.Investigational, Withdrawn
Valproic AcidThe metabolism of Valproic Acid can be decreased when combined with Lobeglitazone.Approved, Investigational
ValsartanThe metabolism of Valsartan can be decreased when combined with Lobeglitazone.Approved, Investigational
VenlafaxineThe metabolism of Venlafaxine can be decreased when combined with Lobeglitazone.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Lobeglitazone.Approved
VicrivirocThe metabolism of Vicriviroc can be decreased when combined with Lobeglitazone.Investigational
VismodegibThe metabolism of Vismodegib can be decreased when combined with Lobeglitazone.Approved
VoriconazoleThe metabolism of Voriconazole can be decreased when combined with Lobeglitazone.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Lobeglitazone.Approved
VoxilaprevirThe metabolism of Voxilaprevir can be decreased when combined with Lobeglitazone.Approved
WarfarinThe metabolism of Warfarin can be decreased when combined with Lobeglitazone.Approved
XimelagatranThe metabolism of Ximelagatran can be decreased when combined with Lobeglitazone.Approved, Investigational, Withdrawn
ZafirlukastThe metabolism of Zafirlukast can be decreased when combined with Lobeglitazone.Approved, Investigational
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Lobeglitazone.Approved
ZaltoprofenThe metabolism of Zaltoprofen can be decreased when combined with Lobeglitazone.Approved
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Lobeglitazone.Approved
ZileutonThe metabolism of Zileuton can be decreased when combined with Lobeglitazone.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Ziprasidone can be decreased when combined with Lobeglitazone.Approved
ZolmitriptanThe metabolism of Zolmitriptan can be decreased when combined with Lobeglitazone.Approved, Investigational
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Lobeglitazone.Approved
ZopicloneThe metabolism of Zopiclone can be decreased when combined with Lobeglitazone.Approved
Food Interactions
Not Available

References

Synthesis Reference

Kim BY, Ahn JB, Lee HW, Kang SK, Lee JH, Shin JS, Ahn SK, Hong CI, Yoon SS: Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione. Eur J Med Chem. 2004 May;39(5):433-47.

General References
  1. Lee YH, Kim JH, Kim SR, Jin HY, Rhee EJ, Cho YM, Lee BW: Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness. J Korean Med Sci. 2017 Jan;32(1):60-69. doi: 10.3346/jkms.2017.32.1.60. [PubMed:27914133]
  2. Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ: Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3. [PubMed:25648999]
  3. Jin SM, Park CY, Cho YM, Ku BJ, Ahn CW, Cha BS, Min KW, Sung YA, Baik SH, Lee KW, Yoon KH, Lee MK, Park SW: Lobeglitazone and pioglitazone as add-ons to metformin for patients with type 2 diabetes: a 24-week, multicentre, randomized, double-blind, parallel-group, active-controlled, phase III clinical trial with a 28-week extension. Diabetes Obes Metab. 2015 Jun;17(6):599-602. doi: 10.1111/dom.12435. Epub 2015 Feb 8. [PubMed:25580775]
  4. Kim BY, Ahn JB, Lee HW, Kang SK, Lee JH, Shin JS, Ahn SK, Hong CI, Yoon SS: Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione. Eur J Med Chem. 2004 May;39(5):433-47. [PubMed:15110969]
  5. Lee JH, Ahn SH, Maeng HJ, Lee W, Kim DD, Chung SJ: The identification of lobeglitazone metabolites in rat liver microsomes and the kinetics of the in vivo formation of the major metabolite M1 in rats. J Pharm Biomed Anal. 2015 Nov 10;115:375-82. doi: 10.1016/j.jpba.2015.07.040. Epub 2015 Jul 30. [PubMed:26275726]
External Links
PubChem Compound
9826451
PubChem Substance
310265106
ChemSpider
8002194
ChEBI
136052
ChEMBL
CHEMBL3585580
Wikipedia
Lobeglitazone

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Male Volunteers1
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableLiver Dysfunction1
1CompletedTreatmentHealthy Volunteers / Impaired Renal Function1
1CompletedTreatmentType 2 Diabetes Mellitus5
1Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
2CompletedTreatmentType 2 Diabetes Mellitus1
3CompletedTreatmentType 2 Diabetes Mellitus2
4CompletedTreatmentNon-Alcoholic Fatty Liver Disease (NAFLD) / Type 2 Diabetes Mellitus1
4RecruitingTreatmentType 2 Diabetes Mellitus2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0181 mg/mLALOGPS
logP3.84ALOGPS
logP4.31ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)7.61ChemAxon
pKa (Strongest Basic)3.96ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area102.88 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity129.63 m3·mol-1ChemAxon
Polarizability49.64 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
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

Taxonomy

Description
This compound belongs to the class of organic compounds known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
Kingdom
Organic compounds
Super Class
Organic oxygen compounds
Class
Organooxygen compounds
Sub Class
Ethers
Direct Parent
Diarylethers
Alternative Parents
Phenoxy compounds / Methoxybenzenes / Anisoles / Dialkylarylamines / Thiazolidinediones / Alkyl aryl ethers / Aminopyrimidines and derivatives / Imidolactams / Heteroaromatic compounds / Dicarboximides
show 7 more
Substituents
Diaryl ether / Phenoxy compound / Anisole / Phenol ether / Methoxybenzene / Dialkylarylamine / Alkyl aryl ether / Aminopyrimidine / Thiazolidinedione / Monocyclic benzene moiety
show 18 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Activator
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. Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ: Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3. [PubMed:25648999]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
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. Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ: Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3. [PubMed:25648999]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
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. Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ: Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3. [PubMed:25648999]
Kind
Protein
Organism
Human
Pharmacological action
No
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. Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ: Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3. [PubMed:25648999]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
No
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. Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ: Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3. [PubMed:25648999]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as estrone-3-sulfate (PubMed:10873595). Mediates transport of prostaglandins (PG) E1 and E2, thyroxine (T4), deltorphin II, BQ-123 an...
Gene Name
SLCO3A1
Uniprot ID
Q9UIG8
Uniprot Name
Solute carrier organic anion transporter family member 3A1
Molecular Weight
76552.135 Da
References
  1. Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ: Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3. [PubMed:25648999]
Kind
Protein
Organism
Human
Pharmacological action
No
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ: Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3. [PubMed:25648999]

Drug created on October 16, 2015 16:12 / Updated on October 02, 2017 06:14