Compounds > pf 04971729
Page last updated: 2024-11-13

pf 04971729

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Description

ertugliflozin: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44814423
CHEMBL ID1770248
CHEBI ID188719
SCHEMBL ID181047
MeSH IDM0571292

Synonyms (61)

Synonym
(1s,2s,3s,4r,5s)-5-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol
CHEBI:188719
ertugliflozin
1210344-57-2
pf04971729
mk-8835
pf-04971729-00
CHEMBL1770248 ,
pf-04971729
D10313
ertugliflozin (usan/inn)
(1s,2s,3s,4r,5s)-5-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1-(hydroxymethyl)-6,8-dioxa-bicyclo[3.2.1]octane-2,3,4-triol
bdbm50342885
5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1-hydroxymethyl-6,8-dioxabicyclo(3.2.1)octane-2,3,4-triol
unii-6c282481ip
steglatro
pf 04971729
beta-l-idopyranose, 1,6-anhydro-1-c-(4-chloro-3-((4-ethoxyphenyl)methyl)phenyl)-5-c-(hydroxymethyl)-
ertugliflozin [usan:inn]
pf 04971729-00
(1s,2s,3s,4r,5s)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1-hydroxymethyl-6,8-dioxabicyclo(3.2.1)octane-2,3,4-triol
6c282481ip ,
HY-15461
CS-0976
S5413
1,6-anhydro-1-c-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-c-(hydroxymethyl)-beta-l-idopyranose
ertugliflozin [mi]
beta-l-idopyranose, 1,6-anhydro-1-c-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-c-(hydroxymethyl)-
ertugliflozin [usan]
(1s,2s,3s,4r,5s)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol
ertugliflozin [inn]
ertugliflozin [orange book]
ertugliflozin [who-dd]
MCIACXAZCBVDEE-CUUWFGFTSA-N
(1s,2s,3s,4r,5s)-5-[4-chloro-3-(4-ethoxy-benzyl)-phenyl]-1-hydroxymethyl-6,8-dioxa-bicyclo[3.2.1]octane-2,3,4-triol
SCHEMBL181047
J-504029
gtpl8376
AC-29007
DTXSID40153120
AKOS025404928
mfcd21609259
EX-A407
pf-04971729;ertugliflozin
(1s,2s,3s,4r,5s)-5-{4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl}-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol
DB11827
AS-35204
Q27077223
AMY32613
CCG-269087
(1s,2s,3s,4r,5s)-5-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1-hydroxymethyl-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol
ertugliflozin component of stelujan
ertugliflozine
ertugliflozin component of segluromet
segluromet component ertugliflozin
a10bk04
stelujan component ertugliflozin
(1s,2s,3s,4r,5s)-5-(4-chloro-3-((4-ethoxyphenyl)methyl)phenyl)-1-(hydroxymethyl)-6,8-dioxabicyclo(3.2.1)octane-2,3,4-triol
ertugliflozina
ertugliflozinum
EN300-7393259

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"7% of patients (9/328) withdrew because of adverse events (AEs); the frequency of AEs was evenly distributed across groups."( Dose-ranging efficacy and safety study of ertugliflozin, a sodium-glucose co-transporter 2 inhibitor, in patients with type 2 diabetes on a background of metformin.
Amin, NB; Jain, SM; Lee, DS; Nucci, G; Rusnak, JM; Wang, X, 2015)		0.42
" There was no significant difference between treatments in the proportion of participants with symptomatic hypoglycaemia or adverse events associated with urinary tract infection or hypovolaemia."( Phase III, efficacy and safety study of ertugliflozin monotherapy in people with type 2 diabetes mellitus inadequately controlled with diet and exercise alone.
Dagogo-Jack, S; Darekar, A; Davies, M; Derosa, G; Focht, K; Frias, J; Golm, G; Johnson, J; Lauring, B; Saur, D; Terra, SG, 2017)		0.46
" Ertugliflozin was not associated with increased incidence of urinary tract infections, symptomatic hypoglycaemia or hypovolaemia adverse events compared with placebo/metformin."( Long-term efficacy and safety of ertugliflozin monotherapy in patients with inadequately controlled T2DM despite diet and exercise: VERTIS MONO extension study.
Aronson, R; Darekar, A; Frias, J; Goldman, A; Lauring, B; Terra, SG, 2018)		0.48
" The VERTIS cardiovascular (CV) outcomes trial (NCT01986881) has a primary objective to demonstrate non-inferiority of ertugliflozin versus placebo on major adverse CV events: time to the first event of CV death, nonfatal myocardial infarction, or nonfatal stroke."( Design and baseline characteristics of the eValuation of ERTugliflozin effIcacy and Safety CardioVascular outcomes trial (VERTIS-CV).
Cannon, CP; Charbonnel, B; Cosentino, F; Dagogo-Jack, S; Gallo, S; Golm, G; Huyck, S; Lauring, B; Mancuso, J; Masiukiewicz, U; McGuire, DK; Pratley, R; Shih, WJ; Terra, SG, 2018)		0.48
"3% of patients experienced adverse events with placebo, ertugliflozin 5- and 15 mg, respectively."( Safety and efficacy of ertugliflozin in Asian patients with type 2 diabetes mellitus inadequately controlled with metformin monotherapy: VERTIS Asia.
Huyck, S; Ji, L; Lauring, B; Liu, S; Liu, Y; Miao, H; Mu, Y; Pan, S; Qiu, Y; Terra, SG; Wang, W; Xie, Y; Yan, P; Yang, M, 2019)		0.51
" Safety evaluation included overall and prespecified adverse events based on pooled data (broad pool) from seven phase 3 studies (including studies in the efficacy analysis)."( Efficacy and safety of ertugliflozin in East/Southeast Asian patients with type 2 diabetes mellitus.
Cater, NB; Darekar, A; Gantz, I; Hickman, A; Huyck, S; Liu, J; Patel, S; Pong, A; Terra, SG; Wu, L, 2020)		0.56
" Incidence of adverse events was 52."( Efficacy and Safety of Ertugliflozin in Patients with Overweight and Obesity with Type 2 Diabetes Mellitus.
Gallo, S; Hannachi, H; Heymsfield, SB; Liu, J; Pong, A; Raji, A; Terra, SG, 2020)		0.56
" Safety evaluation included overall and prespecified adverse events (AEs)."( Efficacy and safety of ertugliflozin in older patients with type 2 diabetes: A pooled analysis of phase III studies.
Charbonnel, B; Dagogo-Jack, S; Ellison, MC; Gantz, I; Hickman, A; Huyck, S; Liu, J; Patel, S; Pong, A; Pratley, R; Tarasenko, L; Terra, SG, 2020)		0.56
" Common adverse effects, including genital mycotic infections and so on, were reviewed."( Effectiveness and safety of ertugliflozin for type 2 diabetes: A meta-analysis of data from randomized controlled trials.
Hou, X; Wang, W; Zhang, F, 2022)		0.72
" The primary objective of VERTIS CV was to show non-inferiority of ertugliflozin to placebo with respect to the primary outcome, major adverse cardiovascular events (a composite of death from cardiovascular causes, non-fatal myocardial infarction, or non-fatal stroke)."( Cardiorenal outcomes, kidney function, and other safety outcomes with ertugliflozin in older adults with type 2 diabetes (VERTIS CV): secondary analyses from a randomised, double-blind trial.
Adamsons, I; Cannon, CP; Cherney, DZI; Cosentino, F; Dagogo-Jack, S; Essex, MN; Jones, PLS; Lawrence, D; Liu, J; McGuire, DK; Pratley, RE, 2023)		0.91
" The study outcomes were major adverse cardiovascular events, hospitalisation for heart failure or cardiovascular death, cardiovascular death, hospitalisation for heart failure, prespecified kidney composite outcomes, kidney function, and other assessments of safety."( Cardiorenal outcomes, kidney function, and other safety outcomes with ertugliflozin in older adults with type 2 diabetes (VERTIS CV): secondary analyses from a randomised, double-blind trial.
Adamsons, I; Cannon, CP; Cherney, DZI; Cosentino, F; Dagogo-Jack, S; Essex, MN; Jones, PLS; Lawrence, D; Liu, J; McGuire, DK; Pratley, RE, 2023)		0.91

Pharmacokinetics

ExcerptReferenceRelevance
" Blood and urine samples were collected predose and over 96 hours postdose for pharmacokinetic evaluation and measurement of urinary glucose excretion over 24 hours."( The Effect of Renal Impairment on the Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Subjects With Type 2 Diabetes Mellitus.
Cutler, DL; Hickman, A; O'Gorman, M; Sahasrabudhe, V; Saur, D; Shi, H; Terra, SG; Zhou, Z, 2017)		0.46
" Because concurrent induction of these enzymes could affect ertugliflozin exposure, this study assessed the effect of multiple doses of rifampin on the pharmacokinetic properties of single-dose ertugliflozin."( Effect of Rifampin on the Pharmacokinetics of Ertugliflozin in Healthy Subjects.
Cutler, DL; Dawra, VK; Hickman, A; Liang, Y; Matschke, K; Sahasrabudhe, V; Saur, D; Shi, H; Terra, SG, 2018)		0.48
" Plasma samples for ertugliflozin pharmacokinetic analysis were collected during 72hours after dosing on day 1 of period 1 and day 8 of period 2 and analyzed using a validated HPLC-MS/MS method."( Effect of Rifampin on the Pharmacokinetics of Ertugliflozin in Healthy Subjects.
Cutler, DL; Dawra, VK; Hickman, A; Liang, Y; Matschke, K; Sahasrabudhe, V; Saur, D; Shi, H; Terra, SG, 2018)		0.48
" This study was conducted to assess the effect of hepatic impairment on the pharmacokinetic (PK), safety, and tolerability profiles of ertugliflozin after administration of a single, 15-mg oral dose."( Pharmacokinetics of Single-dose Ertugliflozin in Patients With Hepatic Impairment.
Cutler, DL; Hickman, A; Matschke, K; Raje, S; Sahasrabudhe, V; Saur, D; Shi, H; Terra, SG; Zhou, S, 2018)		0.48
" The newly developed method was successfully applied to investigate the pharmacokinetic interactions of ERTU with mefenamic acid (MEF) and ketoconazole (KET)."( A novel high-performance liquid chromatographic method combined with fluorescence detection for determination of ertugliflozin in rat plasma: Assessment of pharmacokinetic drug interaction potential of ertugliflozin with mefenamic acid and ketoconazole.
Han, DG; Yoon, IS; Yun, H, 2019)		0.51
" A population pharmacokinetic (popPK) model was developed to characterize the pharmacokinetics (PK) of ertugliflozin and quantify the influence of intrinsic (eg, body weight, age, sex, race, estimated glomerular filtration rate [eGFR], T2DM) and extrinsic (eg, food) covariates on the PK parameters of ertugliflozin."( Population Pharmacokinetic Model for Ertugliflozin in Healthy Subjects and Patients With Type 2 Diabetes Mellitus.
Dawra, VK; Fediuk, DJ; Sahasrabudhe, V; Sweeney, K; Zhou, S, 2021)		0.62
" This analysis evaluated the drug-drug interaction (DDI) following co-administration of ertugliflozin with the UGT inhibitor mefenamic acid (MFA) using physiologically-based pharmacokinetic (PBPK) modeling."( Physiologically-Based Pharmacokinetic Modeling of the Drug-Drug Interaction of the UGT Substrate Ertugliflozin Following Co-Administration with the UGT Inhibitor Mefenamic Acid.
Callegari, E; Goosen, TC; Lin, J; Sahasrabudhe, V; Tse, S, 2021)		0.62
" Two population pharmacokinetic (PK) analyses were conducted, using data from up to 17 phase 1 to 3 studies, to characterize ertugliflozin PK parameters in select ethnic subgroups: (1) East/Southeast (E/SE) Asian vs non-E/SE Asian subjects; (2) Asian subjects from mainland China vs Asian subjects from the rest of the world and non-Asian subjects."( Population Pharmacokinetic Analyses of Ertugliflozin in Select Ethnic Populations.
Dawra, VK; Fediuk, DJ; Sahasrabudhe, V; Sweeney, K; Zhou, S, 2021)		0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
" This analysis evaluated the drug-drug interaction (DDI) following co-administration of ertugliflozin with the UGT inhibitor mefenamic acid (MFA) using physiologically-based pharmacokinetic (PBPK) modeling."( Physiologically-Based Pharmacokinetic Modeling of the Drug-Drug Interaction of the UGT Substrate Ertugliflozin Following Co-Administration with the UGT Inhibitor Mefenamic Acid.
Callegari, E; Goosen, TC; Lin, J; Sahasrabudhe, V; Tse, S, 2021)		0.62

Bioavailability

ExcerptReferenceRelevance
" Moderate to good bioavailability in rats (69%) and dogs (94%) was observed after oral dosing."( Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus.
Chupka, J; Feng, B; Kalgutkar, AS; Kimoto, E; Mascitti, V; Miao, Z; Robinson, RP; Tan, B; Tugnait, M; Walsky, RL; Yang, X; Zhu, T, 2011)		0.37
" Overall, these data suggest that ertugliflozin is well absorbed in humans, and eliminated largely via glucuronidation."( Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
Amin, N; Callegari, E; Kalgutkar, AS; Mascitti, V; Miao, Z; Nucci, G; Sharma, R; Tugnait, M; Vaz, AD, 2013)		0.39
" Ertugliflozin demonstrated roughly 100% bioavailability following a single dose of 15 mg."( Ertugliflozin for the treatment of type 2 diabetes.
Kuhad, A; Razdan, K; Sharma, R, 2019)		0.51
" Therefore, a study was conducted to estimate the relative bioavailability of ertugliflozin when administered in non-commercial formulated tablets containing the amorphous form vs."( Relative bioavailability of ertugliflozin tablets containing the amorphous form versus tablets containing the cocrystal form.
Arora, KK; Hickman, A; Kong, A; Matschke, K; Nickerson, B; Rodríguez Spong, B; Sahasrabudhe, V; Shi, H, 2022)		0.72
"Any dissociation of ertugliflozin to the amorphous form that occurs in tablets containing the cocrystal will not have any clinically meaningful impact on the oral bioavailability of ertugliflozin."( Relative bioavailability of ertugliflozin tablets containing the amorphous form versus tablets containing the cocrystal form.
Arora, KK; Hickman, A; Kong, A; Matschke, K; Nickerson, B; Rodríguez Spong, B; Sahasrabudhe, V; Shi, H, 2022)		0.72

Dosage Studied

ExcerptRelevanceReference
" Plasma samples for ertugliflozin pharmacokinetic analysis were collected during 72hours after dosing on day 1 of period 1 and day 8 of period 2 and analyzed using a validated HPLC-MS/MS method."( Effect of Rifampin on the Pharmacokinetics of Ertugliflozin in Healthy Subjects.
Cutler, DL; Dawra, VK; Hickman, A; Liang, Y; Matschke, K; Sahasrabudhe, V; Saur, D; Shi, H; Terra, SG, 2018)		0.48
" The approved fixed-dose combination (FDC) of ertugliflozin and immediate-release metformin is dosed twice daily (BID)."( A PK/PD study comparing twice-daily to once-daily dosing regimens of ertugliflozin in healthy subjects
.
Bass, A; Cutler, D; Dawra, VK; Hickman, A; Liang, Y; Sahasrabudhe, V; Shi, H; Terra, SG; Zhou, S, 2019)		0.51
" Ertugliflozin absorption was rapid, with maximum plasma concentrations observed 1 hour after dosing under fasted conditions and 2 to 4 hours after dosing under fed conditions."( Pharmacokinetic Properties of Single and Multiple Doses of Ertugliflozin, a Selective Inhibitor of SGLT2, in Healthy Chinese Subjects.
Hickman, A; Krishna, R; Li, Y; Liang, Y; Liu, Z; Matschke, K; Mu, Y; Sahasrabudhe, V; Shi, H, 2020)		0.56
"6 hours) than presently available gliflozins, which translates into single daily dosing and dose reduction allowing for patient compliance."( Ertugliflozin for the treatment of type 2 diabetes.
Kuhad, A; Razdan, K; Sharma, R, 2019)		0.51
" A 2-compartment popPK model with first-order absorption and a lag time and first-order elimination, described the plasma concentration-time profile of ertugliflozin after single and multiple dosing in healthy subjects and in patients with T2DM."( Population Pharmacokinetic Model for Ertugliflozin in Healthy Subjects and Patients With Type 2 Diabetes Mellitus.
Dawra, VK; Fediuk, DJ; Sahasrabudhe, V; Sweeney, K; Zhou, S, 2021)		0.62
" Approaches included (1) quantitative systems pharmacology modeling to predict dose-response relationships, (2) dose-response modeling and model-based meta-analysis for dose selection and efficacy comparisons, (3) population pharmacokinetics (PKs) modeling to characterize PKs and quantify population variability in PK parameters, (4) regression modeling to evaluate ertugliflozin dose-proportionality and the impact of uridine 5'-diphospho-glucuronosyltransferase (UGT) 1A9 genotype on ertugliflozin PKs, and (5) physiologically-based PK modeling to assess the risk of UGT-mediated drug-drug interactions."( End-to-end application of model-informed drug development for ertugliflozin, a novel sodium-glucose cotransporter 2 inhibitor.
Callegari, E; Dawra, VK; Fediuk, DJ; Liang, Y; Musante, CJ; Nucci, G; Sahasrabudhe, V; Sweeney, K; Zhou, S, 2021)		0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny compound containing two aryl groups connected by a single C atom.
[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]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium/glucose cotransporter 1Homo sapiens (human)IC50 (µMol)1.43730.06071.61058.4440AID1447832; AID1546222; AID595067
Sodium/glucose cotransporter 2Homo sapiens (human)IC50 (µMol)0.00140.00050.16534.1000AID1413443; AID1447831; AID1546223
Sodium/glucose cotransporter 2Rattus norvegicus (Norway rat)IC50 (µMol)0.00120.00120.04860.0960AID594035
Solute carrier family 5 member 4Homo sapiens (human)IC50 (µMol)0.00090.00090.06960.2600AID595066
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
chloride transmembrane transportSodium/glucose cotransporter 1Homo sapiens (human)
glucose transmembrane transportSodium/glucose cotransporter 1Homo sapiens (human)
alpha-glucoside transportSodium/glucose cotransporter 1Homo sapiens (human)
intestinal D-glucose absorptionSodium/glucose cotransporter 1Homo sapiens (human)
response to inorganic substanceSodium/glucose cotransporter 1Homo sapiens (human)
pentose transmembrane transportSodium/glucose cotransporter 1Homo sapiens (human)
fucose transmembrane transportSodium/glucose cotransporter 1Homo sapiens (human)
galactose transmembrane transportSodium/glucose cotransporter 1Homo sapiens (human)
myo-inositol transportSodium/glucose cotransporter 1Homo sapiens (human)
transepithelial water transportSodium/glucose cotransporter 1Homo sapiens (human)
renal glucose absorptionSodium/glucose cotransporter 1Homo sapiens (human)
glucose import across plasma membraneSodium/glucose cotransporter 1Homo sapiens (human)
sodium ion import across plasma membraneSodium/glucose cotransporter 1Homo sapiens (human)
intestinal hexose absorptionSodium/glucose cotransporter 1Homo sapiens (human)
transport across blood-brain barrierSodium/glucose cotransporter 1Homo sapiens (human)
glucose transmembrane transportSodium/glucose cotransporter 1Homo sapiens (human)
sodium ion transportSodium/glucose cotransporter 1Homo sapiens (human)
alpha-glucoside transportSodium/glucose cotransporter 2Homo sapiens (human)
carbohydrate metabolic processSodium/glucose cotransporter 2Homo sapiens (human)
hexose transmembrane transportSodium/glucose cotransporter 2Homo sapiens (human)
renal glucose absorptionSodium/glucose cotransporter 2Homo sapiens (human)
glucose import across plasma membraneSodium/glucose cotransporter 2Homo sapiens (human)
sodium ion import across plasma membraneSodium/glucose cotransporter 2Homo sapiens (human)
sodium ion transportSodium/glucose cotransporter 2Homo sapiens (human)
sodium ion transmembrane transportSolute carrier family 5 member 4Homo sapiens (human)
proton transmembrane transportSolute carrier family 5 member 4Homo sapiens (human)
sodium ion transportSolute carrier family 5 member 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
galactose transmembrane transporter activitySodium/glucose cotransporter 1Homo sapiens (human)
glucose transmembrane transporter activitySodium/glucose cotransporter 1Homo sapiens (human)
myo-inositol:sodium symporter activitySodium/glucose cotransporter 1Homo sapiens (human)
water transmembrane transporter activitySodium/glucose cotransporter 1Homo sapiens (human)
glucose:sodium symporter activitySodium/glucose cotransporter 1Homo sapiens (human)
protein bindingSodium/glucose cotransporter 1Homo sapiens (human)
pentose transmembrane transporter activitySodium/glucose cotransporter 1Homo sapiens (human)
fucose transmembrane transporter activitySodium/glucose cotransporter 1Homo sapiens (human)
alpha-glucoside transmembrane transporter activitySodium/glucose cotransporter 1Homo sapiens (human)
galactose:sodium symporter activitySodium/glucose cotransporter 1Homo sapiens (human)
D-glucose transmembrane transporter activitySodium/glucose cotransporter 1Homo sapiens (human)
low-affinity glucose:sodium symporter activitySodium/glucose cotransporter 2Homo sapiens (human)
glucose:sodium symporter activitySodium/glucose cotransporter 2Homo sapiens (human)
protein bindingSodium/glucose cotransporter 2Homo sapiens (human)
alpha-glucoside transmembrane transporter activitySodium/glucose cotransporter 2Homo sapiens (human)
D-glucose transmembrane transporter activitySodium/glucose cotransporter 2Homo sapiens (human)
glucose:sodium symporter activitySolute carrier family 5 member 4Homo sapiens (human)
protein bindingSolute carrier family 5 member 4Homo sapiens (human)
proton transmembrane transporter activitySolute carrier family 5 member 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
early endosomeSodium/glucose cotransporter 1Homo sapiens (human)
plasma membraneSodium/glucose cotransporter 1Homo sapiens (human)
apical plasma membraneSodium/glucose cotransporter 1Homo sapiens (human)
brush border membraneSodium/glucose cotransporter 1Homo sapiens (human)
intracellular organelleSodium/glucose cotransporter 1Homo sapiens (human)
perinuclear region of cytoplasmSodium/glucose cotransporter 1Homo sapiens (human)
extracellular exosomeSodium/glucose cotransporter 1Homo sapiens (human)
intracellular vesicleSodium/glucose cotransporter 1Homo sapiens (human)
plasma membraneSodium/glucose cotransporter 1Homo sapiens (human)
plasma membraneSodium/glucose cotransporter 2Homo sapiens (human)
membraneSodium/glucose cotransporter 2Homo sapiens (human)
apical plasma membraneSodium/glucose cotransporter 2Homo sapiens (human)
extracellular exosomeSodium/glucose cotransporter 2Homo sapiens (human)
plasma membraneSodium/glucose cotransporter 2Homo sapiens (human)
plasma membraneSolute carrier family 5 member 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (59)

Assay IDTitleYearJournalArticle
AID1447832Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes.
AID594022Half life in Sprague-Dawley rat at 2 mg/kg, iv2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID594037Selectivity ratio of IC50 for GLUT1 to IC50 for human SGLT22011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214275AUC (0 to infinity) in healthy human at 25 mg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID594028Oral bioavailability in Sprague-Dawley rat at 5 mg/kg2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID594023Inhibition of human OAT12011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID595069Fraction unbound in rat plasma at 1000 ng/mL by equilibrium dialysis method2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1546221Toxicity in human T2DM patients assessed as reduction in systolic blood pressure at 10 mg, po for 4 weeks2019European journal of medicinal chemistry, Dec-15, Volume: 184Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review.
AID595067Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID595074Plasma clearance in Sprague-Dawley rat at 2 mg/kg, iv2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID594021Volume of distribution at steady state in Sprague-Dawley rat at 2 mg/kg, iv2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID594033Average free plasma concentration in Sprague-Dawley rat at 30 mg/kg, po after 24 hrs2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214255Drug metabolism in healthy human plasma at 25 mg, po by HPLC-radiocardiogram analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID594038Selectivity ratio of IC50 for GLUT2 to IC50 for human SGLT22011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214278Drug excretion in healthy human urine at 25 mg, po by HPLC-radiocardiogram analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID594027Tmax in Sprague-Dawley rat at 5 mg/kg, po2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID594025Inhibition of human OCT22011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214279Drug excretion in healthy human feces at 25 mg, po by HPLC-radiocardiogram analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID1214253Total drug excretion in healthy human at 25 mg, po by HPLC-radiocardiogram analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID594026Cmax in Sprague-Dawley rat at 5 mg/kg, po2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214262Drug recovery in beagle dog at 10 mg/kg, po after 1 to 144 hrs2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID595066Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214269Oral bioavailability in Sprague-Dawley rat at 2 mg/kg2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID1214267Drug level in bile duct-cannulated dog bile at 10 mg/kg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID1447831Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes.
AID594029Inhibition of rat OCT2 expressed in HEK293 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1546232Selectivity ratio of IC50 for inhibition of human SGLT1 to IC50 for inhibition of human SGLT22019European journal of medicinal chemistry, Dec-15, Volume: 184Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review.
AID594036Inhibition of SGLT2 in po dosed Sprague-Dawley rat after 24 hrs2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214270Oral bioavailability in beagle dog at 2 mg/kg2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID595071Apparent intrinsic clearance in human hepatocytes assessed per million of cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214257Metabolic stability in human liver microsomes assessed as retention time at 10 mg by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID1214274AUC (0 to last) in healthy human at 25 mg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID594031Antidiabetic activity in po dosed Sprague-Dawley rat assessed as increase of urinary glucose excretion after 24 hrs2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID595065Lipophilicity, log D of the compound2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214260Drug recovery in Sprague-Dawley rat urine at 25 mg/kg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID1214276Terminal half life in healthy human at 25 mg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID595070Apparent intrinsic clearance in human liver microsomes assessed per mg of protein2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1546223Inhibition of human SGLT22019European journal of medicinal chemistry, Dec-15, Volume: 184Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review.
AID1214271Terminal elimination half life in human at 0.5 to 300 mg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID594035Inhibition of rat SGLT22011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID594030Inhibition of rat OCT3 expressed in HEK293 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214265Drug level in bile duct-cannulated rat bile at 25 mg/kg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID594040Selectivity ratio of IC50 for GLUT4 to IC50 for human SGLT22011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID594024Inhibition of human OAT32011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1546218Tmax in human at 5 mg, po2019European journal of medicinal chemistry, Dec-15, Volume: 184Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review.
AID1413443Inhibition of SGLT2 (unknown origin)2018MedChemComm, Aug-01, Volume: 9, Issue:8
Sodium-glucose cotransporter 2 (SGLT-2) inhibitors: a new antidiabetic drug class.
AID1413444Selectivity ratio of IC50 for SGLT1 (unknown origin) to IC50 for SGLT2 (unknown origin)2018MedChemComm, Aug-01, Volume: 9, Issue:8
Sodium-glucose cotransporter 2 (SGLT-2) inhibitors: a new antidiabetic drug class.
AID1447833Selectivity ratio of IC50 for human SGLT1 expressed in CHO cells to IC50 for human SGLT2 expressed in CHO cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes.
AID594039Selectivity ratio of IC50 for GLUT3 to IC50 for human SGLT22011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1214272Cmax in healthy human at 25 mg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID594032Antidiabetic activity in Sprague-Dawley rat assessed as increase of urinary glucose excretion assessed per 200 gram of body weight at 30 mg/kg, po after 24 hrs2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID594034fAUC (0 to 24 hrs) in Sprague-Dawley rat at 30 mg/kg, po after 24 hrs2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID595068Fraction unbound in human plasma at 1000 ng/mL by equilibrium dialysis method2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1546220Toxicity in human T2DM patients assessed as reduction in systolic blood pressure at 5 mg, po for 4 weeks2019European journal of medicinal chemistry, Dec-15, Volume: 184Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review.
AID1214273Tmax in healthy human at 25 mg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
AID1546219Antidiabetic activity in human T2DM patients assessed as reduction in HbA1c level at 25 mg, po for 12 weeks relative to control2019European journal of medicinal chemistry, Dec-15, Volume: 184Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review.
AID1546222Inhibition of human SGLT12019European journal of medicinal chemistry, Dec-15, Volume: 184Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review.
AID1346950Human Sodium/glucose cotransporter 1 (Hexose transporter family)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
AID1346965Human Sodium/glucose cotransporter 2 (Hexose transporter family)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (92)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's46 (50.00)24.3611
2020's46 (50.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.79

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index9.79 (24.57)
Research Supply Index4.89 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.79)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials39 (41.94%)5.53%
Reviews21 (22.58%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other33 (35.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
beta-alanine
[no description available]		2.2110amino acid zwitterion;
beta-amino acid		agonist;
fundamental metabolite;
human metabolite;
inhibitor;
neurotransmitter
uric acid
Uric Acid: An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.. uric acid : An oxopurine that is the final oxidation product of purine metabolism.. 6-hydroxy-1H-purine-2,8(7H,9H)-dione : A tautomer of uric acid having oxo groups at C-2 and C-8 and a hydroxy group at C-6.. 7,9-dihydro-1H-purine-2,6,8(3H)-trione : An oxopurine in which the purine ring is substituted by oxo groups at positions 2, 6, and 8.		4.7211uric acidEscherichia coli metabolite;
human metabolite;
mouse metabolite
glimepiride
glimepiride: structure given in first source		6.8632sulfonamide
hydrochlorothiazide
Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure.		4.4111benzothiadiazine;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
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.		2.2110dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
mefenamic acid
Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis.		4.9621aminobenzoic acid;
secondary amino compound		analgesic;
antipyretic;
antirheumatic drug;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
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.		13.172115guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
aldosterone
[no description available]		4.411111beta-hydroxy steroid;
18-oxo steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
mineralocorticoid;
primary alpha-hydroxy ketone;
steroid aldehyde		human metabolite;
mouse metabolite
uridine
[no description available]		4.6211uridinesdrug metabolite;
fundamental metabolite;
human metabolite
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		2.2110monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
phlorhizin
[no description available]		3.3110aryl beta-D-glucoside;
dihydrochalcones;
monosaccharide derivative		antioxidant;
plant metabolite
pyrrolidonecarboxylic acid
Pyrrolidonecarboxylic Acid: A cyclized derivative of L-GLUTAMIC ACID. Elevated blood levels may be associated with problems of GLUTAMINE or GLUTATHIONE metabolism.. 5-oxo-L-proline : An optically active form of 5-oxoproline having L-configuration.		2.17105-oxoproline;
L-proline derivative;
non-proteinogenic L-alpha-amino acid		algal metabolite
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		2.2110
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.		7.9361D-glucopyranoseepitope;
mouse metabolite
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		3.5611aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
glycosides
[no description available]		3.7120
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		2.4110antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
sergliflozin etabonate
sergliflozin: a hypoglycemic agent that inhibits SGLT2 sodium-glucose transporter; structure in first source		3.2510glycoside
ozenoxacin
ozenoxacin: an antibacterial for treatment of impetigo; structure in first source		2.2110quinolines
remogliflozin etabonate
remogliflozin etabonate: orally administered hypoglycemic agent; structure in first source		3.2510glycoside
dapagliflozin
[no description available]		5.6460aromatic ether;
C-glycosyl compound;
monochlorobenzenes		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
ipragliflozin
[no description available]		4.220glycoside
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.		10.96117
empagliflozin
[no description available]		5.6760aromatic ether;
C-glycosyl compound;
monochlorobenzenes;
tetrahydrofuryl ether		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
1,5-anhydro-1-(5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl)-1-thioglucitol
[no description available]		3.3110diarylmethane
vx-770
ivacaftor: a CFTR potentiator; structure in first source. ivacaftor : An aromatic amide obtained by formal condensation of the carboxy group of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid with the amino group of 5-amino-2,4-di-tert-butylphenol. Used for the treatment of cystic fibrosis.		2.2110aromatic amide;
monocarboxylic acid amide;
phenols;
quinolone		CFTR potentiator;
orphan drug
canagliflozin
canagliflozin hydrate : A hydrate that is the hemihydrate form of canagliflozin. Used for treatment of type II diabetes via inhibition of sodium-glucose transport protein subtype 2.		5.6460C-glycosyl compound;
organofluorine compound;
thiophenes		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
deberza
[no description available]		3.31102-benzofurans
semaglutide
[no description available]		2.2110lipopeptide;
polypeptide		anti-obesity agent;
appetite depressant;
glucagon-like peptide-1 receptor agonist;
hypoglycemic agent;
neuroprotective agent
oxyntomodulin
Glucagon-Like Peptides: Peptides derived from proglucagon which is also the precursor of pancreatic GLUCAGON. Despite expression of proglucagon in multiple tissues, the major production site of glucagon-like peptides (GLPs) is the INTESTINAL L CELLS. GLPs include glucagon-like peptide 1, glucagon-like peptide 2, and the various truncated forms.		2.2110
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.1710cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Diabetes Mellitus, Adult-Onset
[description not available]		023.7934591
Glycosuria
The appearance of an abnormally large amount of GLUCOSE in the urine, such as more than 500 mg/day in adults. It can be due to HYPERGLYCEMIA or genetic defects in renal reabsorption (RENAL GLYCOSURIA).		06.0531
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.		125.7934591
Fungal Diseases
[description not available]		015.885352
Mycoses
Diseases caused by FUNGI.		015.885352
Cardiac Failure
[description not available]		09.751312
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.		111.751312
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		011.582319
Apnea, Obstructive Sleep
[description not available]		04.9111
Sleep Apnea, Obstructive
A disorder characterized by recurrent apneas during sleep despite persistent respiratory efforts. It is due to upper airway obstruction. The respiratory pauses may induce HYPERCAPNIA or HYPOXIA. Cardiac arrhythmias and elevation of systemic and pulmonary arterial pressures may occur. Frequent partial arousals occur throughout sleep, resulting in relative SLEEP DEPRIVATION and daytime tiredness. Associated conditions include OBESITY; ACROMEGALY; MYXEDEMA; micrognathia; MYOTONIC DYSTROPHY; adenotonsilar dystrophy; and NEUROMUSCULAR DISEASES. (From Adams et al., Principles of Neurology, 6th ed, p395)		04.9111
Cirrhosis
[description not available]		07.61109
Cardiac Hypertrophy
Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.		02.4110
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		07.61109
Cardiomegaly
Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.		02.4110
Liver Steatosis
[description not available]		07.5599
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.		07.5599
Fasting Hypoglycemia
HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.		010.94108
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.		010.94108
Cardiovascular Stroke
[description not available]		05.3121
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		05.3121
Arteriolosclerosis
Thickening of the walls of small ARTERIES or ARTERIOLES due to cell proliferation or HYALINE deposition.		03.9911
Diabetic Angiopathies
VASCULAR DISEASES that are associated with DIABETES MELLITUS.		02.2110
Overweight
A status with BODY WEIGHT that is above certain standards. In the scale of BODY MASS INDEX, overweight is defined as having a BMI of 25.0-29.9 kg/m2. Overweight may or may not be due to increases in body fat (ADIPOSE TISSUE), hence overweight does not equal over fat.		08.5266
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).		03.6411
Female Genital Diseases
[description not available]		014.835050
Genital Diseases, Male
Pathological processes involving the male reproductive tract (GENITALIA, MALE).		014.835050
Genital Diseases, Female
Pathological processes involving the female reproductive tract (GENITALIA, FEMALE).		014.835050
Insulin Sensitivity
[description not available]		07.61160
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.		07.61160
Atherogenesis
[description not available]		08.4365
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		08.4365
Diabetic Glomerulosclerosis
[description not available]		08.4465
Diabetic Nephropathies
KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.		08.4465
Chronic Kidney Diseases
[description not available]		02.3110
Renal Insufficiency, Chronic
Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)		02.3110
Disease Exacerbation
[description not available]		02.3110
Alloxan Diabetes
[description not available]		02.7220
Albuminuria
The presence of albumin in the urine, an indicator of KIDNEY DISEASES.		04.6211
Left Ventricular Hypertrophy
[description not available]		02.3110
Left Ventricular Dysfunction
[description not available]		02.3110
Cardiac Remodeling, Ventricular
[description not available]		02.3110
Hypertrophy, Left Ventricular
Enlargement of the LEFT VENTRICLE of the heart. This increase in ventricular mass is attributed to sustained abnormal pressure or volume loads and is a contributor to cardiovascular morbidity and mortality.		02.3110
Ventricular Dysfunction, Left
A condition in which the LEFT VENTRICLE of the heart was functionally impaired. This condition usually leads to HEART FAILURE; MYOCARDIAL INFARCTION; and other cardiovascular complications. Diagnosis is made by measuring the diminished ejection fraction and a depressed level of motility of the left ventricular wall.		02.3110
Diabetic Cardiomyopathies
Diabetes complications in which VENTRICULAR REMODELING in the absence of CORONARY ATHEROSCLEROSIS and hypertension results in cardiac dysfunctions, typically LEFT VENTRICULAR DYSFUNCTION. The changes also result in myocardial hypertrophy, myocardial necrosis and fibrosis, and collagen deposition due to impaired glucose tolerance.		02.3110
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		15.0610
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		04.4511
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		04.4511
Weight Reduction
[description not available]		07.1232
Weight Loss
Decrease in existing BODY WEIGHT.		07.1232
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		05.7521
Hyperglycemia, Postprandial
Abnormally high BLOOD GLUCOSE level after a meal.		08.1855
Hyperglycemia
Abnormally high BLOOD GLUCOSE level.		08.1855
Liver Dysfunction
[description not available]		04.4811
Liver Diseases
Pathological processes of the LIVER.		04.4811
Genital Tract Infections
[description not available]		05.9122
Vulvovaginitis
Inflammation of the VULVA and the VAGINA, characterized by discharge, burning, and PRURITUS.		04.5111
Adverse Drug Event
[description not available]		04.5111
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		04.5111
Blood Pressure, High
[description not available]		08.06101
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		08.06101
Urinary Tract Infections
Inflammatory responses of the epithelium of the URINARY TRACT to microbial invasions. They are often bacterial infections with associated BACTERIURIA and PYURIA.		04.4111