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Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 03/2011, Volume 54, Issue 5, pp. 1365 - 1378
Journal Article
European Journal of Pharmacology, ISSN 0014-2999, 08/2014, Volume 737, pp. 194 - 201
G protein-coupled receptor 40 (GPR40) is a Gq-coupled receptor for free fatty acids predominantly expressed in pancreatic -cells. In recent years, GPR40... 
GLP-1 | Diabetes | GPR40 | Insulin | GLYCEMIC CONTROL | TAK-875 | FATTY-ACID RECEPTOR | CA2+-INDUCED CA2+ RELEASE | INOSITOL 1,4,5-TRISPHOSPHATE RECEPTORS | DOUBLE-BLIND | PANCREATIC BETA-CELLS | PHARMACOLOGY & PHARMACY | JAPANESE PATIENTS | TYPE-2 DIABETES-MELLITUS | Glucose Intolerance - metabolism | Propionates - pharmacology | Islets of Langerhans - drug effects | Diabetes Mellitus, Experimental - drug therapy | Cricetulus | Humans | Male | Receptors, G-Protein-Coupled - agonists | Exenatide | Indans - therapeutic use | Glucose Intolerance - blood | Diabetes Mellitus, Experimental - blood | Dose-Response Relationship, Drug | Glucose Intolerance - drug therapy | Phenylpropionates - therapeutic use | Drug Interactions | Islets of Langerhans - metabolism | Diabetes Mellitus, Experimental - metabolism | Insulin Secretion | CHO Cells | Receptors, Glucagon - agonists | Cricetinae | Glucose Tolerance Test | Glucagon-Like Peptide 1 - pharmacology | Propionates - therapeutic use | Rats | Gene Knockout Techniques | Peptides - pharmacology | Phenylpropionates - pharmacology | Insulin - metabolism | Animals | Receptors, G-Protein-Coupled - deficiency | Glucagon-Like Peptide-1 Receptor | Mice | Receptors, G-Protein-Coupled - genetics | Venoms - pharmacology | Blood Glucose - metabolism | Indans - pharmacology | Type 2 diabetes | Glucagon | Phenylalanine | Glucose intolerance | Glucose | Glucose tolerance tests | Fatty acids | Cells | Dextrose | Membrane proteins | Glucose metabolism | Hyperglycemia | Analysis | Insulin resistance | G proteins
Journal Article
American Journal of Physiology - Endocrinology And Metabolism, ISSN 0193-1849, 03/2013, Volume 304, Issue 6, pp. 668 - 676
Activation of G protein-coupled receptor 40 (GPR40) by agonists increases insulin release in isolated islets, whereas it is inconclusive whether GPR40... 
Partial agonist | Insulin resistance | Fetuin-A | Diabetes | G protein-coupled receptor 40 | FETUIN-A CONCENTRATIONS | CELLS | PHYSIOLOGY | ACID | ANTAGONIST | TOLERANCE | GPR40 | partial agonist | LIVER | ENDOCRINOLOGY & METABOLISM | fetuin-A | RESISTANCE | SECRETION | ACCUMULATION | diabetes | insulin resistance | Receptors, G-Protein-Coupled - metabolism | Humans | Diet, High-Fat - adverse effects | Male | Propionates - administration & dosage | Diabetes Mellitus, Type 2 - metabolism | Receptors, G-Protein-Coupled - agonists | Insulin - blood | Liver Glycogen - metabolism | Hypoglycemic Agents - administration & dosage | Liver - drug effects | RNA Interference | Diabetes Mellitus, Type 2 - etiology | Methylamines - therapeutic use | Hypoglycemic Agents - therapeutic use | Hyperglycemia - prevention & control | Blood Glucose - analysis | Liver - metabolism | Mice, Inbred C57BL | Insulin Resistance | Methylamines - administration & dosage | Propionates - therapeutic use | Hep G2 Cells | Diabetes Mellitus, Type 2 - blood | Animals | Signal Transduction - drug effects | Receptors, G-Protein-Coupled - antagonists & inhibitors | alpha-2-HS-Glycoprotein - metabolism | Mice | Receptors, G-Protein-Coupled - genetics | Diabetes Mellitus, Type 2 - drug therapy | Glucose metabolism | Physiological aspects | Homeostasis | G proteins | Research | Health aspects | Insulin | Agonists (Biochemistry)
Journal Article
Diabetes, Obesity and Metabolism, ISSN 1462-8902, 08/2017, Volume 19, Issue 8, pp. 1127 - 1134
Aims To evaluate the efficacy and safety of fasiglifam, an orally active G‐protein‐coupled receptor 40 agonist, in combination with the dipeptidyl peptidase‐4... 
antidiabetic drug | glycaemic control | insulin secretagogue | type 2 diabetes | phase I‐II study | randomized trial | phase I-II study | DIPEPTIDYL PEPTIDASE-4 INHIBITOR | INITIAL COMBINATION THERAPY | EFFICACY | FASTING HYPERGLYCEMIA | SAFETY | INSULIN-SECRETION | TAK-875 | GPR40 AGONIST | ENDOCRINOLOGY & METABOLISM | DOUBLE-BLIND | JAPANESE PATIENTS | Sulfones - therapeutic use | United States - epidemiology | Hypoglycemia - epidemiology | Metformin - therapeutic use | Receptors, G-Protein-Coupled - metabolism | Dipeptidyl-Peptidase IV Inhibitors - adverse effects | Dipeptidyl-Peptidase IV Inhibitors - therapeutic use | Humans | Middle Aged | Sulfones - adverse effects | Benzofurans - administration & dosage | Male | Receptors, G-Protein-Coupled - agonists | Metformin - adverse effects | Hemoglobins, Abnormal - analysis | Incidence | Dose-Response Relationship, Drug | Hypoglycemia - prevention & control | Drug Therapy, Combination - adverse effects | Hyperglycemia | Female | Hypoglycemia - chemically induced | Drug Resistance | Hypoglycemic Agents - therapeutic use | Benzofurans - therapeutic use | Double-Blind Method | Combined Modality Therapy - adverse effects | Benzofurans - adverse effects | Diabetes Mellitus, Type 2 - blood | Incretins - adverse effects | Sitagliptin Phosphate - therapeutic use | Incretins - therapeutic use | Diabetes Mellitus, Type 2 - drug therapy | Hypoglycemic Agents - adverse effects | Incretins - administration & dosage | Sitagliptin Phosphate - adverse effects | Sulfones - administration & dosage | Type 2 diabetes | Enzymes | Medical research | Care and treatment | Glycosylated hemoglobin | Medicine, Experimental | Insulin resistance | Hypoglycemic agents | Diabetes therapy | Hypoglycemia | Diabetes
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2012, Volume 55, Issue 8, pp. 3756 - 3776
Journal Article
Toxicological Sciences, ISSN 1096-6080, 06/2018, Volume 163, Issue 2, pp. 374 - 384
Abstract TAK-875, a GPR40 agonist, was withdrawn from Phase III clinical trials due to drug-induced liver injury (DILI). Mechanistic studies were conducted to... 
Metabolic activation | DILI | TAK-875 | Hepatic transporters | Acyl glucuronide | hepatic transporters | BILE-SALTS | SALT EXPORT PUMP | MITOCHONDRIAL-FUNCTION | PHASE-III | acyl glucuronide | RECEPTOR 40 AGONIST | ADVERSE-REACTIONS | ACID-CONTAINING DRUGS | metabolic activation | GPR40 AGONIST | DOUBLE-BLIND | TOXICOLOGY | JAPANESE PATIENTS | Index Medicus
Journal Article
DRUG METABOLISM AND DISPOSITION, ISSN 0090-9556, 05/2019, Volume 47, Issue 5, pp. 525 - 534
Fasiglifam, a potent and highly selective agonist of G protein-coupled receptor 40, was developed for the treatment of type 2 diabetes mellitus. However, phase... 
TRANSPORT | HEPATOCYTES | PHARMACOKINETICS | EFFICACY | SAFETY | INJURY | PHARMACOLOGY & PHARMACY | RECEPTOR 40 AGONIST | HEPATIC-UPTAKE | TAK-875 | JAPANESE PATIENTS
Journal Article
Biomolecules and Therapeutics, ISSN 1976-9148, 11/2018, Volume 26, Issue 6, pp. 599 - 607
Fasiglifam (TAK-875) a G-protein coupled receptor 40 (GPR40) agonist, significantly improves hyperglycemia without hypoglycemia and weight gain, the major side... 
Fasiglifam | Zebrafish | Reactive oxygen species | G-protein coupled receptor 40 | GPR40 | Hepatotoxicity | OXIDATIVE STRESS | INSULIN-SECRETION | JUVENILE RATS | INDUCED LIVER-INJURY | IN-VITRO | HEPATOCELLULAR-CARCINOMA | GLUCOSE-HOMEOSTASIS | DOUBLE-BLIND | PHARMACOLOGY & PHARMACY | TYPE-2 DIABETES-MELLITUS | Original
Journal Article
Biomolecules & Therapeutics(구 응용약물학회지), ISSN 1976-9148, 2018, Volume 26, Issue 6, pp. 599 - 607
Fasiglifam (TAK-875) a G-protein coupled receptor 40 (GPR40) agonist, significantly improves hyperglycemia without hypoglycemia and weight gain, the major side... 
Fasiglifam | Zebrafish | Reactive oxygen species | G-protein coupled receptor 40 | GPR40 | Hepatotoxicity
Journal Article