Compounds > lobeglitazone
Page last updated: 2024-12-11

lobeglitazone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

lobeglitazone: putative antidiabetic agent for type 2 diabetes; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9826451
CHEMBL ID3585580
CHEBI ID136052
SCHEMBL ID2742697
MeSH IDM0542511

Synonyms (18)

Synonym
lobeglitazone
CHEBI:136052
unii-my89f08k5d
my89f08k5d ,
ckd501
607723-33-1
lobeglitazone [inn]
lobeglitazone [who-dd]
(5rs)-5((4-(2-((6-(4-methoxyphenoxy)pyrimidin-4-yl)methylamino)ethoxy)phenyl)methyl)-1,3-thiazolidine-2,4-dione
2,4-thiazolidinedione, 5-((4-(2-((6-(4-methoxyphenoxy)-4-pyrimidinyl)methylamino)ethoxy)phenyl)methyl)-
SCHEMBL2742697
CHEMBL3585580
DB09198
5-(4-(2-((6-(4-methoxyphenoxy)pyrimidin-4-yl)(methyl)amino)ethoxy)benzyl)thiazolidine-2,4-dione
Q18350076
SB16869
5-[[4-[2-[[6-(4-methoxyphenoxy)pyrimidin-4-yl]-methylamino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
EX-A8011

Research Excerpts

Overview

Lobeglitazone (LGZ) is a novel ligand of PPAR-γ; and its role in EMT and metastasis in papillary thyroid carcinoma (PTC) is poorly understood. It is a recently approved peroxisome proliferator-activated receptor- gamma agonist for the treatment of type 2 diabetes mellitus.

ExcerptReferenceRelevance
"Lobeglitazone (LGZ) is a novel ligand of PPAR-γ; and its role in EMT and metastasis in papillary thyroid carcinoma (PTC) is poorly understood."( Lobeglitazone, A Peroxisome Proliferator-Activated Receptor-Gamma Agonist, Inhibits Papillary Thyroid Cancer Cell Migration and Invasion by Suppressing p38 MAPK Signaling Pathway.
Baek, HS; Ha, J; Han, JS; Jin, JQ; Lim, DJ, 2021)		2.79
"Lobeglitazone is a novel thiazolidinedione agent that improves insulin resistance and has similar glycemic efficacy to pioglitazone."( Lobeglitazone, a novel thiazolidinedione, for secondary prevention in patients with ischemic stroke: a nationwide nested case-control study.
Baik, M; Jeon, J; Kim, J; Yoo, J, 2023)		3.07
"Lobeglitazone is a peroxisome proliferator-activated receptor gamma ligand and a type of thiazolidinedione that elicits anti-inflammatory effects."( Lobeglitazone inhibits LPS-induced NLRP3 inflammasome activation and inflammation in the liver.
Han, E; Han, S; Hwang, JS; Jang, BK; Kim, MK; Lee, SH; Park, JY; Seo, HY, 2023)		3.07
"Lobeglitazone (Lobe) is a novel thiazolidinedione antidiabetic drug that reduces insulin resistance by activating peroxisome proliferator-activated receptor-gamma (PPARγ). "( Effects of lobeglitazone on insulin resistance and hepatic steatosis in high-fat diet-fed mice.
Choi, BH; Hahm, JR; Jeong, EA; Jin, Z; Kim, HJ; Kim, KE; Lee, JE; Lee, JY; Oh, J; Park, KA; Roh, GS; Yi, CO, 2018)		2.31
"Lobeglitazone is a recently approved peroxisome proliferator-activated receptor-γ agonist for the treatment of type 2 diabetes mellitus in Korea. "( Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-γ agonist, after a single oral administration in healthy female subjects.
Cho, JY; Jang, IJ; Kim, C; Kim, J; Kim, TE; Lim, KS; Park, MK; Yoon, SH; Yu, KS, 2014)		2.12

Effects

ExcerptReferenceRelevance
"Lobeglitazone has been developed for the treatment of type 2 diabetes mellitus. "( Lack of the effect of lobeglitazone, a peroxisome proliferator-activated receptor-γ agonist, on the pharmacokinetics and pharmacodynamics of warfarin.
Huh, W; Jung, JA; Kim, C; Kim, JR; Kim, TE; Ko, JW; Lee, SY, 2015)		2.17

Treatment

ExcerptReferenceRelevance
"Lobeglitazone-treated patients showed significantly decreased CAP values (313.4 dB/m at baseline vs."( Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness.
Cho, YM; Jin, HY; Kim, JH; Kim, SR; Lee, BW; Lee, YH; Rhee, EJ, 2017)		2.62

Toxicity

ExcerptReferenceRelevance
"Overall adverse events (AEs) occurred in 381 patients (17."( A Real-World Study of Long-Term Safety and Efficacy of Lobeglitazone in Korean Patients with Type 2 Diabetes Mellitus.
Chun, SW; Chung, CH; Han, SJ; Jeong, IK; Kim, BY; Kim, HS; Kim, S; Kim, SK; Kwon, HS; Lee, JH; Lee, MY; Lim, S; Min, JY; Noh, JH; Park, CY; Park, HK; Song, KH; Won, JC; Yu, JM, 2022)		0.97
" Overall treatment-emergent adverse events (including weight gain, oedema and hypoglycaemia) occurred more frequently in the standard-dose group."( A double-blind, Randomized controlled trial on glucose-lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase-4 inhibitor therapy: REFIND study.
Bae, JC; Han, JM; Kim, ES; Kim, IJ; Kim, MK; Kim, SS; Kim, YI; Koh, G; Kwon, MJ; Kwon, SK; Lee, CW; Nam-Goong, IS; Park, JH; Ryang, S; Yoo, S, 2022)		0.93
"Adding low-dose lobeglitazone to metformin and DPP4 inhibitor combination resulted in a non-inferior glucose-lowering outcome and fewer adverse events compared with standard-dose lobeglitazone."( A double-blind, Randomized controlled trial on glucose-lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase-4 inhibitor therapy: REFIND study.
Bae, JC; Han, JM; Kim, ES; Kim, IJ; Kim, MK; Kim, SS; Kim, YI; Koh, G; Kwon, MJ; Kwon, SK; Lee, CW; Nam-Goong, IS; Park, JH; Ryang, S; Yoo, S, 2022)		1.28

Pharmacokinetics

Coadministration of lobeglitazone and dapagliflozin had no apparent clinically relevant effects on the pharmacokinetic properties of either drug.

ExcerptReferenceRelevance
" The objective of this study was to develop a rapid and sensitive method for the determination of CKD-501 in rat plasma and to assess the applicability of the assay to pharmacokinetic studies."( Quantification of CKD-501, lobeglitazone, in rat plasma using a liquid-chromatography/tandem mass spectrometry method and its applications to pharmacokinetic studies.
Chung, SJ; Hwang, IC; Kim, CY; Kim, DD; Lee, JH; Shim, CK; Woo, YA, 2009)		0.65
"This study's aim was to evaluate the tolerability and pharmacokinetic (PK) properties of lobeglitazone to satisfy regulatory requirements for marketing approval in Korea."( Tolerability and pharmacokinetics of lobeglitazone (CKD-501), a peroxisome proliferator-activated receptor-γ agonist: a single- and multiple-dose, double-blind, randomized control study in healthy male Korean subjects.
Cho, JY; Jang, IJ; Kim, DH; Kim, JR; Kim, JW; Shin, HS; Shin, KH; Shin, SG; Yi, S; Yoon, SH; Yu, KS, 2011)		0.86
" The primary objective of this study was to investigate potential pharmacokinetic interactions between lobeglitazone and metformin in healthy Korean subjects."( Assessment of the pharmacokinetics of co-administered metformin and lobeglitazone, a thiazolidinedione antihyperglycemic agent, in healthy subjects.
Cho, JY; Jang, IJ; Kim, TE; Shin, D; Shin, SG; Yoon, SH; Yu, KS, 2012)		0.83
" A single 2 or 4 mg oral dose of lobeglitazone or a placebo was randomly administered to 22 female subjects, and pharmacokinetic blood samples were obtained after dosing."( Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-γ agonist, after a single oral administration in healthy female subjects.
Cho, JY; Jang, IJ; Kim, C; Kim, J; Kim, TE; Lim, KS; Park, MK; Yoon, SH; Yu, KS, 2014)		0.96
" In spite of the pharmacokinetic difference, dose adjustment based on sex alone is not needed in clinical use because therapy should be individualized for each patient to achieve glycemic control."( Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-γ agonist, after a single oral administration in healthy female subjects.
Cho, JY; Jang, IJ; Kim, C; Kim, J; Kim, TE; Lim, KS; Park, MK; Yoon, SH; Yu, KS, 2014)		0.68
" To address such potential concern, we evaluated the effects of ketoconazole, a prototypic CYP3A4 inhibitor, on the pharmacokinetic (PK) properties and associated adverse effects of lobeglitazone."( Effect of ketoconazole on lobeglitazone pharmacokinetics in Korean volunteers.
Kim, C; Kim, KH; Kim, YN; Lee, JI; Ok Kim, C; Park, MS; Sil Oh, E, 2014)		0.89
" We evaluated the pharmacokinetic interactions between lobeglitazone and amlodipine in healthy male Korean subjects."( Pharmacokinetic Interaction Between Amlodipine and Lobeglitazone, a Novel Peroxisome Proliferator-activated Receptor-γ Agonist, in Healthy Subjects.
Kim, C; Kim, CO; Park, MS; Sil Oh, E, 2015)		0.92
" Thus, 21 participants completed the study schedule to compare the pharmacokinetic parameters of lobeglitazone, and 22 participants completed the study of amlodipine."( Pharmacokinetic Interaction Between Amlodipine and Lobeglitazone, a Novel Peroxisome Proliferator-activated Receptor-γ Agonist, in Healthy Subjects.
Kim, C; Kim, CO; Park, MS; Sil Oh, E, 2015)		0.89
" Individual pharmacokinetic properties were determined by noncompartmental methods."( Pharmacokinetics and bioequivalence of 0.5 mg lobeglitazone tablets in healthy male subjects
.
Jeon, JY; Kim, MG; Lee, SJ; Park, SJ, 2018)		0.74
"28 subjects completed the study and were included in the pharmacokinetic analysis."( Pharmacokinetics and bioequivalence of 0.5 mg lobeglitazone tablets in healthy male subjects
.
Jeon, JY; Kim, MG; Lee, SJ; Park, SJ, 2018)		0.74
" This study aimed to evaluate the effect of the coadministration of lobeglitazone and dapagliflozin on their individual pharmacokinetic properties at steady state in healthy male volunteers in the fasted state."( Evaluation of the Pharmacokinetic Interaction Between Lobeglitazone and Dapagliflozin at Steady State.
Jang, K; Jeon, JY; Kim, MG; Moon, SJ, 2020)		1.04
" Blood samples were taken periodically over a 48-h period after dosing to derive total plasma lobeglitazone and dapagliflozin pharmacokinetic properties; safety profile was evaluated throughout the study."( Evaluation of the Pharmacokinetic Interaction Between Lobeglitazone and Dapagliflozin at Steady State.
Jang, K; Jeon, JY; Kim, MG; Moon, SJ, 2020)		1.03
"Coadministration of lobeglitazone and dapagliflozin had no apparent clinically relevant effects on the pharmacokinetic properties of either drug."( Evaluation of the Pharmacokinetic Interaction Between Lobeglitazone and Dapagliflozin at Steady State.
Jang, K; Jeon, JY; Kim, MG; Moon, SJ, 2020)		1.13
" The objective of this study was to investigate a possible pharmacokinetic interaction between lobeglitazone and sitagliptin after multiple oral administrations in healthy Korean men."( An Assessment of Pharmacokinetic Interaction Between Lobeglitazone and Sitagliptin After Multiple Oral Administrations in Healthy Men.
Kim, MG; Moon, SJ; Yu, KS, 2020)		1.03
"Nineteen men from study 1 and 17 from study 2 completed the pharmacokinetic sampling and were included in the analyses."( An Assessment of Pharmacokinetic Interaction Between Lobeglitazone and Sitagliptin After Multiple Oral Administrations in Healthy Men.
Kim, MG; Moon, SJ; Yu, KS, 2020)		0.81
" This study was conducted to evaluate the pharmacokinetic (PK) drug-drug interactions between empagliflozin and lobeglitazone in healthy subjects."( No Relevant Pharmacokinetic Drug-Drug Interaction Between the Sodium-Glucose Co-Transporter-2 Inhibitor Empagliflozin and Lobeglitazone, a Peroxisome Proliferator-Activated Receptor-γ Agonist, in Healthy Subjects.
Hwang, JG; Kim, YK; Park, MK, 2021)		1.04
"In this open-label, single-dose, parallel-group study, we compared the pharmacokinetic profile and safety of lobeglitazone, a thiazolidinedione acting as an agonist for peroxisome proliferator-activated receptors, in patients with hepatic impairment (HI) and healthy matched controls for age, sex, and body weight."( Effects of Hepatic Impairment on the Pharmacokinetic Profile and Safety of Lobeglitazone.
Ahn, SH; Chung, YE; Kim, BK; Kim, CO; Kim, DY; Kim, JK; Kim, SM; Kim, SU; Lee, JI; Oh, ES; Park, J; Park, MS, 2022)		1.16

Compound-Compound Interactions

ExcerptReferenceRelevance
" This study was conducted to evaluate the pharmacokinetic (PK) drug-drug interactions between empagliflozin and lobeglitazone in healthy subjects."( No Relevant Pharmacokinetic Drug-Drug Interaction Between the Sodium-Glucose Co-Transporter-2 Inhibitor Empagliflozin and Lobeglitazone, a Peroxisome Proliferator-Activated Receptor-γ Agonist, in Healthy Subjects.
Hwang, JG; Kim, YK; Park, MK, 2021)		1.04

Bioavailability

ExcerptReferenceRelevance
" In rats, LB appeared to be readily absorbed after an oral administration (an absolute bioavailability of ∼95%)."( Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats.
Ahn, SH; Chung, SJ; Jeong, YS; Kim, DD; Lee, JH; Lee, W; Noh, CK; Yim, CS, 2015)		0.65

Dosage Studied

Lobeglitazone and warfarin can be coadministered without dosage adjustments for either drug.

ExcerptRelevanceReference
" These findings indicate that lobeglitazone and warfarin can be coadministered without dosage adjustments for either drug."( Lack of the effect of lobeglitazone, a peroxisome proliferator-activated receptor-γ agonist, on the pharmacokinetics and pharmacodynamics of warfarin.
Huh, W; Jung, JA; Kim, C; Kim, JR; Kim, TE; Ko, JW; Lee, SY, 2015)		1.02
" Blood samples were taken periodically over a 48-h period after dosing to derive total plasma lobeglitazone and dapagliflozin pharmacokinetic properties; safety profile was evaluated throughout the study."( Evaluation of the Pharmacokinetic Interaction Between Lobeglitazone and Dapagliflozin at Steady State.
Jang, K; Jeon, JY; Kim, MG; Moon, SJ, 2020)		1.03
" Serial blood samples were collected up to 48 h after dosing on the fifth day."( An Assessment of Pharmacokinetic Interaction Between Lobeglitazone and Sitagliptin After Multiple Oral Administrations in Healthy Men.
Kim, MG; Moon, SJ; Yu, KS, 2020)		0.81
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1231389Lipophilicity, log P of the compound2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions.
AID1231390Drug absorption in orally dosed human2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (48)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (2.08)29.6817
2010's26 (54.17)24.3611
2020's21 (43.75)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.88

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index53.88 (24.57)
Research Supply Index4.20 (2.92)
Research Growth Index6.71 (4.65)
Search Engine Demand Index80.74 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (53.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials17 (34.69%)5.53%
Reviews3 (6.12%)6.00%
Case Studies0 (0.00%)4.05%
Observational1 (2.04%)0.25%
Other28 (57.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
3-hydroxybutyric acid
3-Hydroxybutyric Acid: BUTYRIC ACID substituted in the beta or 3 position. It is one of the ketone bodies produced in the liver.. 3-hydroxybutyric acid : A straight-chain 3-hydroxy monocarboxylic acid comprising a butyric acid core with a single hydroxy substituent in the 3- position; a ketone body whose levels are raised during ketosis, used as an energy source by the brain during fasting in humans. Also used to synthesise biodegradable plastics.		2.610(omega-1)-hydroxy fatty acid;
3-hydroxy monocarboxylic acid;
hydroxybutyric acid		human metabolite
amlodipine
Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.		9.4111dihydropyridine;
ethyl ester;
methyl ester;
monochlorobenzenes;
primary amino compound		antihypertensive agent;
calcium channel blocker;
vasodilator agent
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		9.411dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
metformin
Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.		8.7107guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
pioglitazone
Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.		6.2951aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
2,4-thiazolidinedione
thiazolidine-2,4-dione: structure in first source. 1,3-thiazolidine-2,4-dione : A thiazolidenedione carrying oxo substituents at positions 2 and 4.		2.6120thiazolidenedione
troglitazone
Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity.		3.2110chromanes;
thiazolidinone		anticoagulant;
anticonvulsant;
antineoplastic agent;
antioxidant;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
hypoglycemic agent;
platelet aggregation inhibitor;
vasodilator agent
rotenone
Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.		2.3110organic heteropentacyclic compound;
rotenones		antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin
atorvastatin
[no description available]		7.1510aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
glucose, (beta-d)-isomer
beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.		6.3432D-glucopyranoseepitope;
mouse metabolite
rosiglitazone
[no description available]		3.5820aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
as 605240
5-quinoxalin-6-ylmethylenethiazolidine-2,4-dione: a PI3Kgamma inhibitor; structure in first source. (5Z)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidine-2,4-dione : A quinoxaline derivative that is quinoxaline in which the hydrogen at position 6 is replaced by a (2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl group. It is a potent inhibitor of the PI3Kgamma, with an IC50 of 8 nM and inhibits the progression of joint inflammation and damage in both lymphocyte-independent and dependent mouse models of rheumatoid arthritis.		3.2110quinoxaline derivative;
thiazolidinediones		anti-inflammatory agent;
antirheumatic drug;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
dapagliflozin
[no description available]		5.6341aromatic ether;
C-glycosyl compound;
monochlorobenzenes		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
5-(2,2-difluorobenzo(1,3)dioxol-5-ylmethylene)thiazolidine-2,4-dione
5-(2,2-difluorobenzo(1,3)dioxol-5-ylmethylene)thiazolidine-2,4-dione: a PI3Kgamma inhibitor; structure in first source		3.2110
sitagliptin phosphate
Sitagliptin Phosphate: A pyrazine-derived DIPEPTIDYL-PEPTIDASE IV INHIBITOR and HYPOGLYCEMIC AGENT that increases the levels of the INCRETIN hormones GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). It is used in the treatment of TYPE 2 DIABETES.		8.3563
empagliflozin
[no description available]		9.6211aromatic ether;
C-glycosyl compound;
monochlorobenzenes;
tetrahydrofuryl ether		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		8.511benzenes;
hydroxycoumarin;
methyl ketone
ConditionIndicatedRelationship StrengthStudiesTrials
Diabetes Mellitus, Adult-Onset
[description not available]		011.39199
Cirrhosis
[description not available]		02.4110
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		113.39199
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		07.4110
Familial Nonmedullary Thyroid Cancer
[description not available]		02.3110
Cancer of the Thyroid
[description not available]		02.3110
Thyroid Neoplasms
Tumors or cancer of the THYROID GLAND.		02.3110
Liver Dysfunction
[description not available]		02.4110
Liver Diseases
Pathological processes of the LIVER.		02.4110
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.5820
Apoplexy
[description not available]		02.610
Acute Ischemic Stroke
[description not available]		02.610
Cardiac Failure
[description not available]		03.0120
Insulin Sensitivity
[description not available]		04.6851
Ischemic Stroke
Stroke due to BRAIN ISCHEMIA resulting in interruption or reduction of blood flow to a part of the brain. When obstruction is due to a BLOOD CLOT formed within in a cerebral blood vessel it is a thrombotic stroke. When obstruction is formed elsewhere and moved to block a cerebral blood vessel (see CEREBRAL EMBOLISM) it is referred to as embolic stroke. Wake-up stroke refers to ischemic stroke occurring during sleep while cryptogenic stroke refers to ischemic stroke of unknown origin.		07.610
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		03.0120
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		09.6851
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		07.610
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.8220
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		02.6920
Weight Gain
Increase in BODY WEIGHT over existing weight.		02.610
Innate Inflammatory Response
[description not available]		02.610
Cirrhosis, Liver
[description not available]		02.610
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		07.610
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		02.610
Atherogenesis
[description not available]		02.5720
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		07.5720
Fasting Hypoglycemia
HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.		02.2510
Hypoglycemia
A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.		02.2510
Cardiometabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components not only include metabolic dysfunctions of METABOLIC SYNDROME but also HYPERTENSION, and ABDOMINAL OBESITY.		03.6411
Metabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components of metabolic syndrome include ABDOMINAL OBESITY; atherogenic DYSLIPIDEMIA; HYPERTENSION; HYPERGLYCEMIA; INSULIN RESISTANCE; a proinflammatory state; and a prothrombotic (THROMBOSIS) state.		08.6411
Alloxan Diabetes
[description not available]		02.3110
Atherosclerotic Parkinsonism
[description not available]		02.3110
Parkinson Disease, Secondary
Conditions which feature clinical manifestations resembling primary Parkinson disease that are caused by a known or suspected condition. Examples include parkinsonism caused by vascular injury, drugs, trauma, toxin exposure, neoplasms, infections and degenerative or hereditary conditions. Clinical features may include bradykinesia, rigidity, parkinsonian gait, and masked facies. In general, tremor is less prominent in secondary parkinsonism than in the primary form. (From Joynt, Clinical Neurology, 1998, Ch38, pp39-42)		02.3110
Liver Steatosis
[description not available]		02.5820
Fatty Liver
Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS.		02.5820
Atheroma
[description not available]		02.5420
Atypical Lipoma
[description not available]		02.110
Atypical Lipomatous Tumor
[description not available]		02.110
Lipoma
A benign tumor composed of fat cells (ADIPOCYTES). It can be surrounded by a thin layer of connective tissue (encapsulated), or diffuse without the capsule.		02.110
Liposarcoma
A malignant tumor derived from primitive or embryonal lipoblastic cells. It may be composed of well-differentiated fat cells or may be dedifferentiated: myxoid (LIPOSARCOMA, MYXOID), round-celled, or pleomorphic, usually in association with a rich network of capillaries. Recurrences are common and dedifferentiated liposarcomas metastasize to the lungs or serosal surfaces. (From Dorland, 27th ed; Stedman, 25th ed)		02.110
Neointima
The new and thickened layer of scar tissue that forms on a PROSTHESIS, or as a result of vessel injury especially following ANGIOPLASTY or stent placement.		07.1110
Fatty Liver, Nonalcoholic
[description not available]		07.5844
Non-alcoholic Fatty Liver Disease
Fatty liver finding without excessive ALCOHOL CONSUMPTION.		07.5844