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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Lobeglitazone
- Accession Number
- DB09198
- Type
- Small Molecule
- Groups
- Approved, Investigational
- 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
Structure for DB09198 (Lobeglitazone)
- Synonyms
- Not Available
- External IDs
- CKD 501 / CKD-501 / CKD501
- Product Ingredients
Ingredient UNII CAS InChI Key lobeglitazone sulfate 95C712E83P Not Available Not 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.
- 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.
Target Actions Organism APeroxisome proliferator-activated receptor gamma activatorHuman - 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
Drug Interaction Drug group Aceclofenac The metabolism of Aceclofenac can be decreased when combined with Lobeglitazone. Approved, Investigational Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Lobeglitazone. Approved, Investigational Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Lobeglitazone. Approved Acetohexamide Lobeglitazone may increase the hypoglycemic activities of Acetohexamide. Approved, Investigational, Withdrawn Acetyl sulfisoxazole The metabolism of Acetyl sulfisoxazole can be decreased when combined with Lobeglitazone. Approved, Vet Approved Acetylsalicylic acid The metabolism of Acetylsalicylic acid can be decreased when combined with Lobeglitazone. Approved, Vet Approved Adinazolam The metabolism of Adinazolam can be decreased when combined with Lobeglitazone. Approved Agomelatine The serum concentration of Agomelatine can be increased when it is combined with Lobeglitazone. Approved, Investigational Albendazole The metabolism of Albendazole can be decreased when combined with Lobeglitazone. Approved, Vet Approved Almotriptan The metabolism of Almotriptan can be decreased when combined with Lobeglitazone. Approved, Investigational Alosetron The metabolism of Alosetron can be decreased when combined with Lobeglitazone. Approved, Withdrawn Alprazolam The metabolism of Alprazolam can be decreased when combined with Lobeglitazone. Approved, Illicit, Investigational Ambrisentan The metabolism of Ambrisentan can be decreased when combined with Lobeglitazone. Approved, Investigational Aminophenazone The metabolism of Aminophenazone can be decreased when combined with Lobeglitazone. Approved, Withdrawn Aminophylline The metabolism of Aminophylline can be decreased when combined with Lobeglitazone. Approved Amiodarone The metabolism of Amiodarone can be decreased when combined with Lobeglitazone. Approved, Investigational Amitriptyline The metabolism of Amitriptyline can be decreased when combined with Lobeglitazone. Approved Amoxicillin The metabolism of Amoxicillin can be decreased when combined with Lobeglitazone. Approved, Vet Approved Amprenavir The metabolism of Amprenavir can be decreased when combined with Lobeglitazone. Approved, Investigational Anagrelide The metabolism of Anagrelide can be decreased when combined with Lobeglitazone. Approved Antipyrine The metabolism of Antipyrine can be decreased when combined with Lobeglitazone. Approved, Investigational Apixaban The metabolism of Apixaban can be decreased when combined with Lobeglitazone. Approved Aprepitant The metabolism of Aprepitant can be decreased when combined with Lobeglitazone. Approved, Investigational Arachidonic Acid The metabolism of Arachidonic Acid can be decreased when combined with Lobeglitazone. Experimental Arformoterol The metabolism of Arformoterol can be decreased when combined with Lobeglitazone. Approved, Investigational Artemether The metabolism of Artemether can be decreased when combined with Lobeglitazone. Approved Asenapine The metabolism of Asenapine can be decreased when combined with Lobeglitazone. Approved Asunaprevir The metabolism of Asunaprevir can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn Atazanavir The metabolism of Atazanavir can be decreased when combined with Lobeglitazone. Approved, Investigational Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Lobeglitazone. Approved Avatrombopag The metabolism of Avatrombopag can be decreased when combined with Lobeglitazone. Approved, Investigational Axitinib The metabolism of Axitinib can be decreased when combined with Lobeglitazone. Approved, Investigational Azelastine The metabolism of Azelastine can be decreased when combined with Lobeglitazone. Approved Bendamustine The metabolism of Bendamustine can be decreased when combined with Lobeglitazone. Approved, Investigational Benzatropine The metabolism of Benzatropine can be decreased when combined with Lobeglitazone. Approved Benzyl alcohol The metabolism of Benzyl alcohol can be decreased when combined with Lobeglitazone. Approved Betaxolol The metabolism of Betaxolol can be decreased when combined with Lobeglitazone. Approved, Investigational Bexarotene The metabolism of Bexarotene can be decreased when combined with Lobeglitazone. Approved, Investigational Bioallethrin The metabolism of Bioallethrin can be decreased when combined with Lobeglitazone. Approved, Experimental Bortezomib The metabolism of Bortezomib can be decreased when combined with Lobeglitazone. Approved, Investigational Bosentan The serum concentration of Bosentan can be increased when it is combined with Lobeglitazone. Approved, Investigational Brivaracetam The metabolism of Brivaracetam can be decreased when combined with Lobeglitazone. Approved, Investigational Bromazepam The metabolism of Bromazepam can be decreased when combined with Lobeglitazone. Approved, Illicit, Investigational Brompheniramine The metabolism of Brompheniramine can be decreased when combined with Lobeglitazone. Approved Bupivacaine The metabolism of Bupivacaine can be decreased when combined with Lobeglitazone. Approved, Investigational Buprenorphine The metabolism of Buprenorphine can be decreased when combined with Lobeglitazone. Approved, Illicit, Investigational, Vet Approved Bupropion The metabolism of Bupropion can be decreased when combined with Lobeglitazone. Approved Cabozantinib The metabolism of Cabozantinib can be decreased when combined with Lobeglitazone. Approved, Investigational Caffeine The metabolism of Caffeine can be decreased when combined with Lobeglitazone. Approved Candesartan The metabolism of Candesartan can be decreased when combined with Lobeglitazone. Experimental Candesartan cilexetil The metabolism of Candesartan cilexetil can be decreased when combined with Lobeglitazone. Approved Cannabidiol The metabolism of Cannabidiol can be decreased when combined with Lobeglitazone. Approved, Investigational Carbamazepine The metabolism of Carbamazepine can be decreased when combined with Lobeglitazone. Approved, Investigational Carbinoxamine The metabolism of Carbinoxamine can be decreased when combined with Lobeglitazone. Approved Carbutamide Lobeglitazone may increase the hypoglycemic activities of Carbutamide. Experimental Carisoprodol The metabolism of Carisoprodol can be decreased when combined with Lobeglitazone. Approved Carmustine The metabolism of Carmustine can be decreased when combined with Lobeglitazone. Approved, Investigational Carvedilol The serum concentration of Carvedilol can be increased when it is combined with Lobeglitazone. Approved, Investigational Celecoxib The metabolism of Celecoxib can be decreased when combined with Lobeglitazone. Approved, Investigational Chloramphenicol The metabolism of Chloramphenicol can be decreased when combined with Lobeglitazone. Approved, Vet Approved Chlorpromazine The metabolism of Chlorpromazine can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Chlorpropamide Lobeglitazone may increase the hypoglycemic activities of Chlorpropamide. Approved, Investigational Chlorzoxazone The metabolism of Chlorzoxazone can be decreased when combined with Lobeglitazone. Approved Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Lobeglitazone. Approved, Investigational Cinacalcet The metabolism of Cinacalcet can be decreased when combined with Lobeglitazone. Approved Cinnarizine The metabolism of Cinnarizine can be decreased when combined with Lobeglitazone. Approved, Investigational Cisapride The metabolism of Cisapride can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn Citalopram The serum concentration of Citalopram can be increased when it is combined with Lobeglitazone. Approved Clarithromycin The metabolism of Clarithromycin can be decreased when combined with Lobeglitazone. Approved Clenbuterol The metabolism of Clenbuterol can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Clevidipine The metabolism of Clevidipine can be decreased when combined with Lobeglitazone. Approved, Investigational Clobazam The metabolism of Clobazam can be decreased when combined with Lobeglitazone. Approved, Illicit clomethiazole The metabolism of clomethiazole can be decreased when combined with Lobeglitazone. Investigational Clomipramine The metabolism of Clomipramine can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Clonidine The metabolism of Clonidine can be decreased when combined with Lobeglitazone. Approved Clopidogrel The 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 Clotiazepam The metabolism of Clotiazepam can be decreased when combined with Lobeglitazone. Approved, Illicit Clozapine The metabolism of Clozapine can be decreased when combined with Lobeglitazone. Approved Conjugated estrogens The metabolism of Conjugated estrogens can be decreased when combined with Lobeglitazone. Approved Cyclobenzaprine The metabolism of Cyclobenzaprine can be decreased when combined with Lobeglitazone. Approved Cyclophosphamide The metabolism of Cyclophosphamide can be decreased when combined with Lobeglitazone. Approved, Investigational Dacarbazine The metabolism of Dacarbazine can be decreased when combined with Lobeglitazone. Approved, Investigational Dapagliflozin The metabolism of Dapagliflozin can be decreased when combined with Lobeglitazone. Approved Dapsone The metabolism of Dapsone can be decreased when combined with Lobeglitazone. Approved, Investigational Dasatinib The metabolism of Dasatinib can be decreased when combined with Lobeglitazone. Approved, Investigational Daunorubicin The metabolism of Daunorubicin can be decreased when combined with Lobeglitazone. Approved Desipramine The metabolism of Desipramine can be decreased when combined with Lobeglitazone. Approved, Investigational Deutetrabenazine The metabolism of Deutetrabenazine can be decreased when combined with Lobeglitazone. Approved, Investigational Dexfenfluramine The metabolism of Dexfenfluramine can be decreased when combined with Lobeglitazone. Approved, Illicit, Investigational, Withdrawn Dexlansoprazole The metabolism of Dexlansoprazole can be decreased when combined with Lobeglitazone. Approved, Investigational Dextromethorphan The metabolism of Dextromethorphan can be decreased when combined with Lobeglitazone. Approved Diazepam The metabolism of Diazepam can be decreased when combined with Lobeglitazone. Approved, Illicit, Investigational, Vet Approved Diclofenac The metabolism of Diclofenac can be decreased when combined with Lobeglitazone. Approved, Vet Approved Dicoumarol The metabolism of Dicoumarol can be decreased when combined with Lobeglitazone. Approved Diltiazem The metabolism of Diltiazem can be decreased when combined with Lobeglitazone. Approved, Investigational Dinoprostone The metabolism of Dinoprostone can be decreased when combined with Lobeglitazone. Approved Diphenhydramine The metabolism of Diphenhydramine can be decreased when combined with Lobeglitazone. Approved, Investigational Doconexent The metabolism of Doconexent can be decreased when combined with Lobeglitazone. Approved, Investigational Dolasetron The metabolism of Dolasetron can be decreased when combined with Lobeglitazone. Approved, Investigational Domperidone The metabolism of Domperidone can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Donepezil The metabolism of Donepezil can be decreased when combined with Lobeglitazone. Approved Dopamine The metabolism of Dopamine can be decreased when combined with Lobeglitazone. Approved Dorzolamide The metabolism of Dorzolamide can be decreased when combined with Lobeglitazone. Approved Doxazosin The metabolism of Doxazosin can be decreased when combined with Lobeglitazone. Approved Doxepin The metabolism of Doxepin can be decreased when combined with Lobeglitazone. Approved, Investigational Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Lobeglitazone. Approved, Illicit Duloxetine The metabolism of Duloxetine can be decreased when combined with Lobeglitazone. Approved Eletriptan The metabolism of Eletriptan can be decreased when combined with Lobeglitazone. Approved, Investigational Eltrombopag The metabolism of Eltrombopag can be decreased when combined with Lobeglitazone. Approved Enasidenib The metabolism of Enasidenib can be decreased when combined with Lobeglitazone. Approved, Investigational Enfuvirtide The metabolism of Enfuvirtide can be decreased when combined with Lobeglitazone. Approved, Investigational Epoprostenol The metabolism of Epoprostenol can be decreased when combined with Lobeglitazone. Approved Ergotamine The metabolism of Ergotamine can be decreased when combined with Lobeglitazone. Approved Erlotinib The metabolism of Erlotinib can be decreased when combined with Lobeglitazone. Approved, Investigational Escitalopram The metabolism of Escitalopram can be decreased when combined with Lobeglitazone. Approved, Investigational Esomeprazole The metabolism of Esomeprazole can be decreased when combined with Lobeglitazone. Approved, Investigational Estradiol The metabolism of Estradiol can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Estradiol acetate The metabolism of Estradiol acetate can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Estradiol benzoate The metabolism of Estradiol benzoate can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Estradiol cypionate The metabolism of Estradiol cypionate can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Estradiol dienanthate The metabolism of Estradiol dienanthate can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Estradiol valerate The metabolism of Estradiol valerate can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Estrone The metabolism of Estrone can be decreased when combined with Lobeglitazone. Approved Estrone sulfate The metabolism of Estrone sulfate can be decreased when combined with Lobeglitazone. Approved Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Lobeglitazone. Approved, Investigational Ethanol The metabolism of Ethanol can be decreased when combined with Lobeglitazone. Approved Etizolam The metabolism of Etizolam can be decreased when combined with Lobeglitazone. Approved Etodolac The metabolism of Etodolac can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Etoposide The metabolism of Etoposide can be decreased when combined with Lobeglitazone. Approved Etoricoxib The metabolism of Etoricoxib can be decreased when combined with Lobeglitazone. Approved, Investigational Etravirine The metabolism of Etravirine can be decreased when combined with Lobeglitazone. Approved Famotidine The metabolism of Famotidine can be decreased when combined with Lobeglitazone. Approved Flunarizine The metabolism of Flunarizine can be decreased when combined with Lobeglitazone. Approved Flunitrazepam The metabolism of Flunitrazepam can be decreased when combined with Lobeglitazone. Approved, Illicit Fluorouracil The metabolism of Fluorouracil can be decreased when combined with Lobeglitazone. Approved Fluoxetine The metabolism of Fluoxetine can be decreased when combined with Lobeglitazone. Approved, Vet Approved Flurbiprofen The metabolism of Flurbiprofen can be decreased when combined with Lobeglitazone. Approved, Investigational Flutamide The metabolism of Flutamide can be decreased when combined with Lobeglitazone. Approved, Investigational Fluvastatin The metabolism of Fluvastatin can be decreased when combined with Lobeglitazone. Approved Fluvoxamine The metabolism of Fluvoxamine can be decreased when combined with Lobeglitazone. Approved, Investigational Formoterol The metabolism of Formoterol can be decreased when combined with Lobeglitazone. Approved, Investigational Fosphenytoin The metabolism of Fosphenytoin can be decreased when combined with Lobeglitazone. Approved, Investigational Frovatriptan The metabolism of Frovatriptan can be decreased when combined with Lobeglitazone. Approved, Investigational Gavestinel The metabolism of Gavestinel can be decreased when combined with Lobeglitazone. Investigational Gemfibrozil The metabolism of Lobeglitazone can be decreased when combined with Gemfibrozil. Approved Genistein The metabolism of Genistein can be decreased when combined with Lobeglitazone. Investigational Glibornuride Lobeglitazone may increase the hypoglycemic activities of Glibornuride. Investigational, Withdrawn Gliclazide Lobeglitazone may increase the hypoglycemic activities of Gliclazide. Approved Glimepiride Lobeglitazone may increase the hypoglycemic activities of Glimepiride. Approved Glipizide Lobeglitazone may increase the hypoglycemic activities of Glipizide. Approved, Investigational Gliquidone Lobeglitazone may increase the hypoglycemic activities of Gliquidone. Approved, Investigational Glisoxepide Lobeglitazone may increase the hypoglycemic activities of Glisoxepide. Investigational Glucosamine The metabolism of Glucosamine can be decreased when combined with Lobeglitazone. Approved, Investigational Glyburide Lobeglitazone may increase the hypoglycemic activities of Glyburide. Approved Grepafloxacin The metabolism of Grepafloxacin can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn Guanabenz The metabolism of Guanabenz can be decreased when combined with Lobeglitazone. Approved, Investigational Guanfacine The metabolism of Guanfacine can be decreased when combined with Lobeglitazone. Approved, Investigational Haloperidol The metabolism of Haloperidol can be decreased when combined with Lobeglitazone. Approved Halothane The metabolism of Halothane can be decreased when combined with Lobeglitazone. Approved, Vet Approved Hesperetin The metabolism of Hesperetin can be decreased when combined with Lobeglitazone. Approved Hexobarbital The metabolism of Hexobarbital can be decreased when combined with Lobeglitazone. Approved Histamine The metabolism of Histamine can be decreased when combined with Lobeglitazone. Approved, Investigational Hydromorphone The metabolism of Hydromorphone can be decreased when combined with Lobeglitazone. Approved, Illicit Ibuprofen The metabolism of Ibuprofen can be decreased when combined with Lobeglitazone. Approved Icotinib The metabolism of Icotinib can be decreased when combined with Lobeglitazone. Approved, Investigational Idarubicin The metabolism of Idarubicin can be decreased when combined with Lobeglitazone. Approved Ifosfamide The metabolism of Ifosfamide can be decreased when combined with Lobeglitazone. Approved Iloperidone The metabolism of Iloperidone can be decreased when combined with Lobeglitazone. Approved Imatinib The metabolism of Imatinib can be decreased when combined with Lobeglitazone. Approved Imipramine The metabolism of Imipramine can be decreased when combined with Lobeglitazone. Approved Imiquimod The metabolism of Imiquimod can be decreased when combined with Lobeglitazone. Approved, Investigational Indisulam The metabolism of Indisulam can be decreased when combined with Lobeglitazone. Investigational Indomethacin The metabolism of Indomethacin can be decreased when combined with Lobeglitazone. Approved, Investigational Irbesartan The metabolism of Irbesartan can be decreased when combined with Lobeglitazone. Approved, Investigational Ixazomib The metabolism of Ixazomib can be decreased when combined with Lobeglitazone. Approved, Investigational Ketamine The metabolism of Ketamine can be decreased when combined with Lobeglitazone. Approved, Vet Approved Ketobemidone The metabolism of Ketobemidone can be decreased when combined with Lobeglitazone. Approved, Investigational Ketoprofen The metabolism of Ketoprofen can be decreased when combined with Lobeglitazone. Approved, Vet Approved Lansoprazole The metabolism of Lansoprazole can be decreased when combined with Lobeglitazone. Approved, Investigational Lapatinib The metabolism of Lapatinib can be decreased when combined with Lobeglitazone. Approved, Investigational Leflunomide The metabolism of Leflunomide can be decreased when combined with Lobeglitazone. Approved, Investigational Lesinurad The metabolism of Lesinurad can be decreased when combined with Lobeglitazone. Approved, Investigational Levobupivacaine The metabolism of Levobupivacaine can be decreased when combined with Lobeglitazone. Approved, Investigational Levomilnacipran The metabolism of Levomilnacipran can be decreased when combined with Lobeglitazone. Approved, Investigational Licofelone The metabolism of Licofelone can be decreased when combined with Lobeglitazone. Investigational Lidocaine The metabolism of Lidocaine can be decreased when combined with Lobeglitazone. Approved, Vet Approved Lofexidine The metabolism of Lofexidine can be decreased when combined with Lobeglitazone. Approved, Investigational Lomefloxacin The metabolism of Lomefloxacin can be decreased when combined with Lobeglitazone. Approved, Investigational Loratadine The metabolism of Loratadine can be decreased when combined with Lobeglitazone. Approved, Investigational Lorcaserin The metabolism of Lorcaserin can be decreased when combined with Lobeglitazone. Approved Lornoxicam The metabolism of Lornoxicam can be decreased when combined with Lobeglitazone. Approved, Investigational Losartan The metabolism of Losartan can be decreased when combined with Lobeglitazone. Approved Lumiracoxib The metabolism of Lumiracoxib can be decreased when combined with Lobeglitazone. Approved, Investigational Macitentan The metabolism of Macitentan can be decreased when combined with Lobeglitazone. Approved Malathion The metabolism of Malathion can be decreased when combined with Lobeglitazone. Approved, Investigational Maprotiline The metabolism of Maprotiline can be decreased when combined with Lobeglitazone. Approved, Investigational Medical Cannabis The metabolism of Medical Cannabis can be decreased when combined with Lobeglitazone. Experimental, Investigational Mefenamic acid The metabolism of Mefenamic acid can be decreased when combined with Lobeglitazone. Approved Melatonin The metabolism of Melatonin can be decreased when combined with Lobeglitazone. Approved, Nutraceutical, Vet Approved Meloxicam The metabolism of Meloxicam can be decreased when combined with Lobeglitazone. Approved, Vet Approved Menadione The metabolism of Menadione can be decreased when combined with Lobeglitazone. Approved, Nutraceutical Mephenytoin The metabolism of Mephenytoin can be decreased when combined with Lobeglitazone. Investigational, Withdrawn Meprobamate The metabolism of Meprobamate can be decreased when combined with Lobeglitazone. Approved, Illicit Mestranol The metabolism of Mestranol can be decreased when combined with Lobeglitazone. Approved Metahexamide Lobeglitazone may increase the hypoglycemic activities of Metahexamide. Experimental Methadone The metabolism of Methadone can be decreased when combined with Lobeglitazone. Approved Methoxyflurane The metabolism of Methoxyflurane can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Methsuximide The metabolism of Methsuximide can be decreased when combined with Lobeglitazone. Approved Methylphenobarbital The metabolism of Methylphenobarbital can be decreased when combined with Lobeglitazone. Approved Metoprolol The metabolism of Metoprolol can be decreased when combined with Lobeglitazone. Approved, Investigational Metronidazole The metabolism of Metronidazole can be decreased when combined with Lobeglitazone. Approved Mexiletine The metabolism of Mexiletine can be decreased when combined with Lobeglitazone. Approved, Investigational Mianserin The metabolism of Mianserin can be decreased when combined with Lobeglitazone. Approved, Investigational Mirtazapine The metabolism of Mirtazapine can be decreased when combined with Lobeglitazone. Approved Moclobemide The metabolism of Moclobemide can be decreased when combined with Lobeglitazone. Approved, Investigational Montelukast The metabolism of Montelukast can be decreased when combined with Lobeglitazone. Approved Muraglitazar The metabolism of Muraglitazar can be decreased when combined with Lobeglitazone. Investigational Nabiximols The metabolism of Nabiximols can be decreased when combined with Lobeglitazone. Approved, Investigational Nabumetone The metabolism of Nabumetone can be decreased when combined with Lobeglitazone. Approved Naproxen The metabolism of Naproxen can be decreased when combined with Lobeglitazone. Approved, Vet Approved Nateglinide The metabolism of Nateglinide can be decreased when combined with Lobeglitazone. Approved, Investigational Nelfinavir The metabolism of Nelfinavir can be decreased when combined with Lobeglitazone. Approved Netupitant The metabolism of Netupitant can be decreased when combined with Lobeglitazone. Approved, Investigational Nevirapine The metabolism of Nevirapine can be decreased when combined with Lobeglitazone. Approved Niclosamide The metabolism of Niclosamide can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Nicotine The metabolism of Nicotine can be decreased when combined with Lobeglitazone. Approved Nifedipine The metabolism of Nifedipine can be decreased when combined with Lobeglitazone. Approved Nilutamide The metabolism of Nilutamide can be decreased when combined with Lobeglitazone. Approved, Investigational Nitric Oxide The metabolism of Nitric Oxide can be decreased when combined with Lobeglitazone. Approved Nortriptyline The metabolism of Nortriptyline can be decreased when combined with Lobeglitazone. Approved Olanzapine The metabolism of Olanzapine can be decreased when combined with Lobeglitazone. Approved, Investigational Olodaterol The metabolism of Olodaterol can be decreased when combined with Lobeglitazone. Approved Omeprazole The metabolism of Omeprazole can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Ondansetron The metabolism of Ondansetron can be decreased when combined with Lobeglitazone. Approved Ospemifene The metabolism of Ospemifene can be decreased when combined with Lobeglitazone. Approved, Investigational Oxaliplatin The metabolism of Oxaliplatin can be decreased when combined with Lobeglitazone. Approved, Investigational Oxaprozin The metabolism of Oxaprozin can be decreased when combined with Lobeglitazone. Approved Oxiconazole The metabolism of Oxiconazole can be decreased when combined with Lobeglitazone. Approved Oxtriphylline The metabolism of Oxtriphylline can be decreased when combined with Lobeglitazone. Approved Paclitaxel The metabolism of Paclitaxel can be decreased when combined with Lobeglitazone. Approved, Vet Approved Palonosetron The metabolism of Palonosetron can be decreased when combined with Lobeglitazone. Approved, Investigational Pantoprazole The metabolism of Pantoprazole can be decreased when combined with Lobeglitazone. Approved Paramethadione The metabolism of Paramethadione can be decreased when combined with Lobeglitazone. Approved Parecoxib The metabolism of Parecoxib can be decreased when combined with Lobeglitazone. Approved Pazopanib The metabolism of Pazopanib can be decreased when combined with Lobeglitazone. Approved Pentamidine The metabolism of Pentamidine can be decreased when combined with Lobeglitazone. Approved, Investigational Pentobarbital The metabolism of Pentobarbital can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Pentoxifylline The metabolism of Pentoxifylline can be decreased when combined with Lobeglitazone. Approved, Investigational Perphenazine The metabolism of Perphenazine can be decreased when combined with Lobeglitazone. Approved Pethidine The metabolism of Pethidine can be decreased when combined with Lobeglitazone. Approved Phenacetin The metabolism of Phenacetin can be decreased when combined with Lobeglitazone. Withdrawn Phenobarbital The metabolism of Phenobarbital can be decreased when combined with Lobeglitazone. Approved, Investigational Phenprocoumon The metabolism of Phenprocoumon can be decreased when combined with Lobeglitazone. Approved, Investigational Phenylbutazone The metabolism of Phenylbutazone can be decreased when combined with Lobeglitazone. Approved, Vet Approved Phenytoin The metabolism of Phenytoin can be decreased when combined with Lobeglitazone. Approved, Vet Approved Pimozide The metabolism of Pimozide can be decreased when combined with Lobeglitazone. Approved Pioglitazone The metabolism of Pioglitazone can be decreased when combined with Lobeglitazone. Approved, Investigational Piperaquine The metabolism of Piperaquine can be decreased when combined with Lobeglitazone. Approved, Investigational Pipotiazine The metabolism of Pipotiazine can be decreased when combined with Lobeglitazone. Approved, Investigational Pirfenidone The serum concentration of Pirfenidone can be increased when it is combined with Lobeglitazone. Approved, Investigational Piroxicam The metabolism of Piroxicam can be decreased when combined with Lobeglitazone. Approved, Investigational Pitavastatin The metabolism of Pitavastatin can be decreased when combined with Lobeglitazone. Approved Podofilox The metabolism of Podofilox can be decreased when combined with Lobeglitazone. Approved Pomalidomide The metabolism of Pomalidomide can be decreased when combined with Lobeglitazone. Approved Prasugrel The metabolism of Prasugrel can be decreased when combined with Lobeglitazone. Approved Pravastatin The metabolism of Pravastatin can be decreased when combined with Lobeglitazone. Approved Praziquantel The metabolism of Praziquantel can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Pregabalin Pregabalin may increase the fluid retaining activities of Lobeglitazone. Approved, Illicit, Investigational Primaquine The metabolism of Primaquine can be decreased when combined with Lobeglitazone. Approved Primidone The metabolism of Primidone can be decreased when combined with Lobeglitazone. Approved, Vet Approved Progesterone The metabolism of Progesterone can be decreased when combined with Lobeglitazone. Approved, Vet Approved Proguanil The metabolism of Proguanil can be decreased when combined with Lobeglitazone. Approved Promazine The metabolism of Promazine can be decreased when combined with Lobeglitazone. Approved, Vet Approved Propafenone The metabolism of Propafenone can be decreased when combined with Lobeglitazone. Approved Propofol The metabolism of Propofol can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Propranolol The metabolism of Propranolol can be decreased when combined with Lobeglitazone. Approved, Investigational Pyrazinamide The metabolism of Pyrazinamide can be decreased when combined with Lobeglitazone. Approved, Investigational Quazepam The metabolism of Quazepam can be decreased when combined with Lobeglitazone. Approved, Illicit Quetiapine The metabolism of Quetiapine can be decreased when combined with Lobeglitazone. Approved Quinidine The metabolism of Quinidine can be decreased when combined with Lobeglitazone. Approved, Investigational Quinine The metabolism of Quinine can be decreased when combined with Lobeglitazone. Approved Rabeprazole The metabolism of Rabeprazole can be decreased when combined with Lobeglitazone. Approved, Investigational Ramelteon The metabolism of Ramelteon can be decreased when combined with Lobeglitazone. Approved, Investigational Ranitidine The metabolism of Ranitidine can be decreased when combined with Lobeglitazone. Approved Rasagiline The metabolism of Rasagiline can be decreased when combined with Lobeglitazone. Approved Resveratrol The metabolism of Resveratrol can be decreased when combined with Lobeglitazone. Approved, Experimental, Investigational Rifabutin The metabolism of Rifabutin can be decreased when combined with Lobeglitazone. Approved, Investigational Rifampicin The metabolism of Lobeglitazone can be increased when combined with Rifampicin. Approved Riluzole The metabolism of Riluzole can be decreased when combined with Lobeglitazone. Approved, Investigational Ritonavir The metabolism of Ritonavir can be decreased when combined with Lobeglitazone. Approved, Investigational Rizatriptan The metabolism of Rizatriptan can be decreased when combined with Lobeglitazone. Approved Rofecoxib The metabolism of Rofecoxib can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn Romidepsin The metabolism of Romidepsin can be decreased when combined with Lobeglitazone. Approved, Investigational Ropinirole The metabolism of Ropinirole can be decreased when combined with Lobeglitazone. Approved, Investigational Ropivacaine The metabolism of Ropivacaine can be decreased when combined with Lobeglitazone. Approved Rosiglitazone The metabolism of Rosiglitazone can be decreased when combined with Lobeglitazone. Approved, Investigational Rosuvastatin The metabolism of Rosuvastatin can be decreased when combined with Lobeglitazone. Approved Rotigotine The metabolism of Rotigotine can be decreased when combined with Lobeglitazone. Approved Rucaparib The metabolism of Rucaparib can be decreased when combined with Lobeglitazone. Approved, Investigational Rupatadine The metabolism of Rupatadine can be decreased when combined with Lobeglitazone. Approved Salicylic acid The metabolism of Salicylic acid can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Selegiline The metabolism of Selegiline can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Seratrodast The metabolism of Seratrodast can be decreased when combined with Lobeglitazone. Approved Sertraline The metabolism of Sertraline can be decreased when combined with Lobeglitazone. Approved Sildenafil The metabolism of Sildenafil can be decreased when combined with Lobeglitazone. Approved, Investigational Sitaxentan The metabolism of Sitaxentan can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn Stiripentol The metabolism of Stiripentol can be decreased when combined with Lobeglitazone. Approved Sulfadiazine The metabolism of Sulfadiazine can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Sulfamethoxazole The metabolism of Sulfamethoxazole can be decreased when combined with Lobeglitazone. Approved Sulfamoxole The metabolism of Sulfamoxole can be decreased when combined with Lobeglitazone. Approved Sulfinpyrazone The metabolism of Sulfinpyrazone can be decreased when combined with Lobeglitazone. Approved Sulfisoxazole The metabolism of Sulfisoxazole can be decreased when combined with Lobeglitazone. Approved, Vet Approved Suprofen The metabolism of Suprofen can be decreased when combined with Lobeglitazone. Approved, Withdrawn Tacrine The metabolism of Tacrine can be decreased when combined with Lobeglitazone. Investigational, Withdrawn Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Lobeglitazone. Approved Tapentadol The metabolism of Tapentadol can be decreased when combined with Lobeglitazone. Approved Telithromycin The metabolism of Telithromycin can be decreased when combined with Lobeglitazone. Approved Temafloxacin The metabolism of Temafloxacin can be decreased when combined with Lobeglitazone. Withdrawn Temazepam The metabolism of Temazepam can be decreased when combined with Lobeglitazone. Approved, Investigational Teniposide The metabolism of Teniposide can be decreased when combined with Lobeglitazone. Approved Tenoxicam The metabolism of Tenoxicam can be decreased when combined with Lobeglitazone. Approved Terbinafine The metabolism of Terbinafine can be decreased when combined with Lobeglitazone. Approved, Investigational, Vet Approved Terfenadine The metabolism of Terfenadine can be decreased when combined with Lobeglitazone. Approved, Withdrawn Testosterone The metabolism of Testosterone can be decreased when combined with Lobeglitazone. Approved, Investigational Testosterone cypionate The metabolism of Testosterone cypionate can be decreased when combined with Lobeglitazone. Approved Testosterone enanthate The metabolism of Testosterone enanthate can be decreased when combined with Lobeglitazone. Approved Testosterone undecanoate The metabolism of Testosterone undecanoate can be decreased when combined with Lobeglitazone. Approved, Investigational Thalidomide The metabolism of Thalidomide can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn Theobromine The metabolism of Theobromine can be decreased when combined with Lobeglitazone. Approved, Investigational Theophylline The metabolism of Theophylline can be decreased when combined with Lobeglitazone. Approved Thiabendazole The metabolism of Thiabendazole can be decreased when combined with Lobeglitazone. Approved, Vet Approved Thiamylal The metabolism of Thiamylal can be decreased when combined with Lobeglitazone. Approved, Vet Approved Thioridazine The metabolism of Thioridazine can be decreased when combined with Lobeglitazone. Approved, Withdrawn Thiothixene The metabolism of Thiothixene can be decreased when combined with Lobeglitazone. Approved Ticlopidine The metabolism of Ticlopidine can be decreased when combined with Lobeglitazone. Approved Timolol The metabolism of Timolol can be decreased when combined with Lobeglitazone. Approved Tipranavir The metabolism of Tipranavir can be decreased when combined with Lobeglitazone. Approved, Investigational Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Lobeglitazone. Approved, Investigational Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Lobeglitazone. Approved, Investigational Tolazamide Lobeglitazone may increase the hypoglycemic activities of Tolazamide. Approved, Investigational Tolbutamide Lobeglitazone may increase the hypoglycemic activities of Tolbutamide. Approved, Investigational Tolperisone The metabolism of Tolperisone can be decreased when combined with Lobeglitazone. Approved, Investigational Tolterodine The metabolism of Tolterodine can be decreased when combined with Lobeglitazone. Approved, Investigational Torasemide The metabolism of Torasemide can be decreased when combined with Lobeglitazone. Approved Toremifene The metabolism of Toremifene can be decreased when combined with Lobeglitazone. Approved, Investigational Trabectedin The metabolism of Trabectedin can be decreased when combined with Lobeglitazone. Approved, Investigational Treprostinil The metabolism of Treprostinil can be decreased when combined with Lobeglitazone. Approved, Investigational Tretinoin The metabolism of Tretinoin can be decreased when combined with Lobeglitazone. Approved, Investigational, Nutraceutical Triamterene The metabolism of Triamterene can be decreased when combined with Lobeglitazone. Approved Trifluoperazine The metabolism of Trifluoperazine can be decreased when combined with Lobeglitazone. Approved, Investigational Trimethadione The metabolism of Trimethadione can be decreased when combined with Lobeglitazone. Approved Trimethoprim The metabolism of Lobeglitazone can be decreased when combined with Trimethoprim. Approved, Vet Approved Trimipramine The metabolism of Trimipramine can be decreased when combined with Lobeglitazone. Approved Troglitazone The metabolism of Troglitazone can be decreased when combined with Lobeglitazone. Investigational, Withdrawn Ulipristal The metabolism of Ulipristal can be decreased when combined with Lobeglitazone. Approved Vadimezan The metabolism of Vadimezan can be decreased when combined with Lobeglitazone. Investigational Valdecoxib The metabolism of Valdecoxib can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn Valproic Acid The metabolism of Valproic Acid can be decreased when combined with Lobeglitazone. Approved, Investigational Valsartan The metabolism of Valsartan can be decreased when combined with Lobeglitazone. Approved, Investigational Venlafaxine The metabolism of Venlafaxine can be decreased when combined with Lobeglitazone. Approved Verapamil The metabolism of Verapamil can be decreased when combined with Lobeglitazone. Approved Vicriviroc The metabolism of Vicriviroc can be decreased when combined with Lobeglitazone. Investigational Vismodegib The metabolism of Vismodegib can be decreased when combined with Lobeglitazone. Approved, Investigational Voriconazole The metabolism of Voriconazole can be decreased when combined with Lobeglitazone. Approved, Investigational Vortioxetine The metabolism of Vortioxetine can be decreased when combined with Lobeglitazone. Approved, Investigational Voxilaprevir The metabolism of Voxilaprevir can be decreased when combined with Lobeglitazone. Approved, Investigational Warfarin The metabolism of Warfarin can be decreased when combined with Lobeglitazone. Approved Ximelagatran The metabolism of Ximelagatran can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn Zafirlukast The metabolism of Zafirlukast can be decreased when combined with Lobeglitazone. Approved, Investigational Zalcitabine The metabolism of Zalcitabine can be decreased when combined with Lobeglitazone. Approved, Investigational Zaltoprofen The metabolism of Zaltoprofen can be decreased when combined with Lobeglitazone. Approved, Investigational Zidovudine The metabolism of Zidovudine can be decreased when combined with Lobeglitazone. Approved Zileuton The metabolism of Zileuton can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn Ziprasidone The metabolism of Ziprasidone can be decreased when combined with Lobeglitazone. Approved Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Lobeglitazone. Approved, Investigational Zolpidem The metabolism of Zolpidem can be decreased when combined with Lobeglitazone. Approved Zopiclone The metabolism of Zopiclone can be decreased when combined with Lobeglitazone. Approved Zotepine The metabolism of Zotepine can be decreased when combined with Lobeglitazone. Approved, Investigational, Withdrawn - 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
- 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]
- 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]
- 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]
- 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]
- 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
Phase Status Purpose Conditions Count 1 Completed Not Available Healthy Male Volunteers 1 1 Completed Not Available Healthy Volunteers 1 1 Completed Not Available Liver Dysfunction 1 1 Completed Treatment Healthy Volunteers / Impaired Renal Function 1 1 Completed Treatment Type 2 Diabetes Mellitus 5 1 Not Yet Recruiting Treatment Type 2 Diabetes Mellitus 1 2 Completed Treatment Type 2 Diabetes Mellitus 1 3 Completed Treatment Type 2 Diabetes Mellitus 2 4 Completed Treatment Non-Alcoholic Fatty Liver Disease (NAFLD) / Type 2 Diabetes Mellitus 1 4 Recruiting Treatment Type 2 Diabetes Mellitus 2
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
Property Value Source Water Solubility 0.0181 mg/mL ALOGPS logP 3.84 ALOGPS logP 4.31 ChemAxon logS -4.4 ALOGPS pKa (Strongest Acidic) 7.61 ChemAxon pKa (Strongest Basic) 3.96 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 7 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 102.88 Å2 ChemAxon Rotatable Bond Count 10 ChemAxon Refractivity 129.63 m3·mol-1 ChemAxon Polarizability 49.64 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not 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
- 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
- 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]
- Jung JA, Lee SY, Kim TE, Kim JR, Kim C, Huh W, Ko JW: Lack of the effect of lobeglitazone, a peroxisome proliferator-activated receptor-gamma agonist, on the pharmacokinetics and pharmacodynamics of warfarin. Drug Des Devel Ther. 2015 Mar 2;9:737-43. doi: 10.2147/DDDT.S76591. eCollection 2015. [PubMed:25767371]
- 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
- 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
- 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
- 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
- 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
- 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 June 08, 2018 11:22