Identification

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Name
Empagliflozin
Accession Number
DB09038
Type
Small Molecule
Groups
Approved
Description

Empagliflozin is a sodium glucose co-transporter-2 (SGLT-2) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes. SGLT2 co-transporters are responsible for reabsorption of glucose from the glomerular filtrate in the kidney. The glucuretic effect resulting from SGLT2 inhibition reduces renal absorption and lowers the renal threshold for glucose, therefore resulting in increased glucose excretion. Additionally, it contributes to reduced hyperglycaemia and also assists weight loss and blood pressure reduction.

Structure
Thumb
Synonyms
  • (1S)-1,5-anhydro-1-(4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl)-D-glucitol
  • 1-chloro-4-(glucopyranos-1-yl)-2-(4-(tetrahydrofuran-3-yloxy)benzyl)benzene
  • Empagliflozin
  • Empagliflozina
External IDs
BI 10773 / BI-10773 / BI10773
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
JardianceTablet, film coated10 mg/1OralBoehringer Ingelheim Pharmaceuticals, Inc.2014-08-01Not applicableUs00597 0152 90 nlmimage10 8d40c686
JardianceTablet, film coated25 mg/1OralAphena Pharma Solutions - Tennessee, LLC2014-08-01Not applicableUs
JardianceTablet25 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2015-08-11Not applicableCanada
JardianceTablet, film coated25 mg/1OralA-S Medication Solutions2014-08-01Not applicableUs
JardianceTablet10 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2015-08-11Not applicableCanada
JardianceTablet, film coated25 mg/1OralCardinal Health2014-08-01Not applicableUs
JardianceTablet, film coated10 mg/1OralA-S Medication Solutions2014-08-01Not applicableUs
JardianceTablet, film coated10 mg/1OralCardinal Health2014-08-01Not applicableUs
JardianceTablet, film coated25 mg/1OralBoehringer Ingelheim Pharmaceuticals, Inc.2014-08-01Not applicableUs
JardianceTablet, film coated10 mg/1OralREMEDYREPACK INC.2019-03-27Not applicableUs
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
GlyxambiEmpagliflozin (10 mg/1) + Linagliptin (5 mg/1)Tablet, film coatedOralBoehringer Ingelheim Pharmaceuticals, Inc.2015-01-30Not applicableUs0597 018220180913 8702 q7fevz
GlyxambiEmpagliflozin (25 mg) + Linagliptin (5 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-12-21Not applicableCanada
GlyxambiEmpagliflozin (10 mg/1) + Linagliptin (5 mg/1)Tablet, film coatedOralREMEDYREPACK INC.2019-04-29Not applicableUs
GlyxambiEmpagliflozin (10 mg) + Linagliptin (5 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-12-21Not applicableCanada
GlyxambiEmpagliflozin (25 mg/1) + Linagliptin (5 mg/1)Tablet, film coatedOralBoehringer Ingelheim Pharmaceuticals, Inc.2015-01-30Not applicableUs
SynjardyEmpagliflozin (5 mg/1) + Metformin hydrochloride (1000 mg/1)TabletOralBoehringer Ingelheim Pharmaceuticals, Inc.2015-08-26Not applicableUs
SynjardyEmpagliflozin (5 mg) + Metformin hydrochloride (850 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-08-03Not applicableCanada
SynjardyEmpagliflozin (5 mg/1) + Metformin hydrochloride (500 mg/1)TabletOralBoehringer Ingelheim Pharmaceuticals, Inc.2015-08-26Not applicableUs
SynjardyEmpagliflozin (5 mg) + Metformin hydrochloride (500 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-08-03Not applicableCanada
SynjardyEmpagliflozin (12.5 mg) + Metformin hydrochloride (500 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-08-03Not applicableCanada
Categories
UNII
HDC1R2M35U
CAS number
864070-44-0
Weight
Average: 450.91
Monoisotopic: 450.1445309
Chemical Formula
C23H27ClO7
InChI Key
OBWASQILIWPZMG-QZMOQZSNSA-N
InChI
InChI=1S/C23H27ClO7/c24-18-6-3-14(23-22(28)21(27)20(26)19(11-25)31-23)10-15(18)9-13-1-4-16(5-2-13)30-17-7-8-29-12-17/h1-6,10,17,19-23,25-28H,7-9,11-12H2/t17-,19+,20+,21-,22+,23-/m0/s1
IUPAC Name
(2S,3R,4R,5S,6R)-2-[4-chloro-3-({4-[(3S)-oxolan-3-yloxy]phenyl}methyl)phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
SMILES
[H][C@@]1(CCOC1)OC1=CC=C(CC2=C(Cl)C=CC(=C2)[C@]2([H])O[C@]([H])(CO)[C@@]([H])(O)[C@]([H])(O)[C@@]2([H])O)C=C1

Pharmacology

Indication

Empagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

Empagliflozin is a sodium glucose co-transporter-2 (SGLT-2) inhibitor. SGLT2 co-transporters are responsible for reabsorption of glucose from the glomerular filtrate in the kidney. The glucuretic effect resulting from SGLT2 inhibition reduces renal absorption and lowers the renal threshold for glucose, resulting in increased glucose excretion. Additionally, it contributes to reduced hyperglycaemia, assists weight loss, and reduces blood pressure.

TargetActionsOrganism
USodium/glucose cotransporter 2
antagonist
inhibitor
Humans
Additional Data Available
Adverse Effects

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Blackbox Warnings

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Absorption

Following oral administration, peak plasma concentrations were reached at 1.5 hours post-dose and then declined in a biphasic manner with a rapid distribution phase and a relatively slow terminal phase. Administration following a high-fat and high-calorie meal results in a slightly lower exposure with AUC decreasing by approximately 16% and Cmax decreasing by approximately 37% compared to fasted condition.

Volume of distribution

73.8 L

Protein binding

Plasma protein binding was found to be 86.2%

Metabolism

In vitro studies suggest that empaglifozin is primarily metabolized by glucuronidation by 5'-diphospho-glucuronosyltransferases UG2B7, UGT1A3, UGT1A8, and UGT1A9. The most abundant metabolites are three glucuronide metabolites: 2-O-, 3-O-, and 6-O-glucuronide. Empagliflozin does not inhibit, inactivate, or induce CYP450 isoforms. It is a substrate for p-glycoprotein (p-gp), however in vitro studies suggest that it is unlikely to cause interactions with drugs that are p-gp substrates.

Route of elimination

After oral administration, empaglifozin was 41.2% eliminated in feces and 54.4% eliminated in urine.

Half life

Terminal elimination half life was found to be 12.4 h based on population pharmacokinetic analysis.

Clearance

Apparent oral clearance was found to be 10.6 L/h based on population pharmacokinetic analysis.

Toxicity

The most commonly reported adverse effects for empaglifozin were urinary tract infections, female genital mycotic infections, and dyslipidemia. Because empagliflozin causes osmotic diuresis adverse reactions related to volume depletion were also reported (decreased systolic blood pressure, dehydration, hypotension, orthostatic hypotension, hypovolemia, and syncope). Impaired renal function and hypoglycemia were also reported.

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

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
2,4-thiazolidinedioneEmpagliflozin may increase the hypoglycemic activities of 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Empagliflozin can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Empagliflozin.
AbacavirAbacavir may decrease the excretion rate of Empagliflozin which could result in a higher serum level.
AcarboseEmpagliflozin may increase the hypoglycemic activities of Acarbose.
AcebutololThe therapeutic efficacy of Acebutolol can be increased when used in combination with Empagliflozin.
AceclofenacAceclofenac may decrease the excretion rate of Empagliflozin which could result in a higher serum level.
AcemetacinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Acemetacin.
AcetaminophenAcetaminophen may decrease the excretion rate of Empagliflozin which could result in a higher serum level.
AcetazolamideThe therapeutic efficacy of Empagliflozin can be increased when used in combination with Acetazolamide.
Additional Data Available
  • Extended Description
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    Severity

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Food Interactions
Not Available

References

Synthesis Reference

Wang XJ, Zhang L, Byrne D, Nummy L, Weber D, Krishnamurthy D, Yee N, Senanayake CH: Efficient synthesis of Empagliflozin, an inhibitor of SGLT-2, utilizing an AlCl3-promoted silane reduction of a beta-glycopyranoside. Org Lett. 2014 Aug 15;16(16):4090-3. doi: 10.1021/ol501755h. Epub 2014 Jul 25. Pubmed

General References
  1. Scheen AJ: Pharmacokinetics, Pharmacodynamics and Clinical Use of SGLT2 Inhibitors in Patients with Type 2 Diabetes Mellitus and Chronic Kidney Disease. Clin Pharmacokinet. 2015 Jul;54(7):691-708. doi: 10.1007/s40262-015-0264-4. [PubMed:25805666]
  2. Gangadharan Komala M, Mather A: Empagliflozin for the treatment of Type 2 diabetes. Expert Rev Clin Pharmacol. 2014 May;7(3):271-9. doi: 10.1586/17512433.2014.908703. Epub 2014 Apr 9. [PubMed:24716752]
  3. Lamos EM, Younk LM, Davis SN: Empagliflozin, a sodium glucose co-transporter 2 inhibitor, in the treatment of type 1 diabetes. Expert Opin Investig Drugs. 2014 Jun;23(6):875-82. doi: 10.1517/13543784.2014.909407. Epub 2014 Apr 19. [PubMed:24746173]
  4. Liakos A, Karagiannis T, Athanasiadou E, Sarigianni M, Mainou M, Papatheodorou K, Bekiari E, Tsapas A: Efficacy and safety of empagliflozin for type 2 diabetes: a systematic review and meta-analysis. Diabetes Obes Metab. 2014 Oct;16(10):984-93. doi: 10.1111/dom.12307. Epub 2014 May 28. [PubMed:24766495]
  5. Haring HU, Merker L, Seewaldt-Becker E, Weimer M, Meinicke T, Broedl UC, Woerle HJ: Empagliflozin as add-on to metformin in patients with type 2 diabetes: a 24-week, randomized, double-blind, placebo-controlled trial. Diabetes Care. 2014 Jun;37(6):1650-9. doi: 10.2337/dc13-2105. Epub 2014 Apr 10. [PubMed:24722494]
  6. Neumiller JJ: Empagliflozin: a new sodium-glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes. Drugs Context. 2014 Jun 11;3:212262. doi: 10.7573/dic.212262. eCollection 2014. [PubMed:24991224]
  7. Bogdanffy MS, Stachlewitz RF, van Tongeren S, Knight B, Sharp DE, Ku W, Hart SE, Blanchard K: Nonclinical safety of the sodium-glucose cotransporter 2 inhibitor empagliflozin. Int J Toxicol. 2014 Nov-Dec;33(6):436-49. doi: 10.1177/1091581814551648. Epub 2014 Sep 26. [PubMed:25260362]
  8. Authors unspecified: Empagliflozin (Jardiance) for diabetes. Med Lett Drugs Ther. 2014 Oct 13;56(1453):99-100. [PubMed:25296258]
  9. Jahagirdar V, Barnett AH: Empagliflozin for the treatment of type 2 diabetes. Expert Opin Pharmacother. 2014 Nov;15(16):2429-41. doi: 10.1517/14656566.2014.966078. [PubMed:25301180]
External Links
KEGG Drug
D10459
PubChem Compound
11949646
PubChem Substance
310264986
ChemSpider
10123957
BindingDB
150162
ChEBI
82720
ChEMBL
CHEMBL2107830
PharmGKB
PA166163327
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Empagliflozin
ATC Codes
A10BD19 — Linagliptin and empagliflozinA10BD20 — Metformin and empagliflozinA10BK03 — Empagliflozin
AHFS Codes
  • 68:20.18 — Sodium-glucose Cotransporter 2 (SGLT2) Inhibitors
FDA label
Download (604 KB)
MSDS
Download (99 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentHealthy Volunteers1
1Active Not RecruitingTreatmentType 2 Diabetes Mellitus1
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceDiabetes Mellitus (DM)1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedHealth Services ResearchType2 Diabetes1
1CompletedOtherDiabetes Mellitus (DM) / Pharmacodynamics / Pharmacokinetics1
1CompletedTreatmentHealthy Volunteers35
1CompletedTreatmentHealthy Volunteers / Hepatic Insufficiency1
1CompletedTreatmentType 2 Diabetes Mellitus8
1Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
1RecruitingBasic ScienceAging / Blood Sugar / Cognitive / Ketones1
1RecruitingTreatmentPatients1
2Active Not RecruitingBasic ScienceBody Weights / Pre-Diabetic1
2Active Not RecruitingTreatmentDiabetes Mellitus (DM)1
2CompletedBasic ScienceRenal Dysfunction1
2CompletedTreatmentAcute Heart Failure (AHF) / Congestive Heart Failure / Heart Failure; With Decompensation1
2CompletedTreatmentBMI >30 kg/m2 / Type 1 Insulin-Dependent Diabetes Mellitus / Type 2 Diabetes Mellitus1
2CompletedTreatmentHealthy Volunteers / Type 2 Diabetes Mellitus1
2CompletedTreatmentHeart Failure / Type 2 Diabetes Mellitus1
2CompletedTreatmentPosttransplant Diabetes Mellitus1
2CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus3
2CompletedTreatmentType 2 Diabetes Mellitus8
2Enrolling by InvitationTreatmentNAFLD / Non-Alcoholic Fatty Liver Disease (NAFLD) / Pediatric NAFLD1
2Not Yet RecruitingTreatmentBMI >30 kg/m2 / Non-diabetic Chronic Kidney Disease1
2RecruitingTreatmentAcute Decompensated Heart Failure (ADHF)1
2RecruitingTreatmentAcute Heart Failure (AHF) / Type 2 Diabetes Mellitus1
2RecruitingTreatmentChronic Heart Failure (CHF)1
2RecruitingTreatmentChronic Kidney Disease stage3 / Chronic Kidney Disease stage4 / Diabetic Kidney Disease / Type 2 Diabetes Mellitus1
2RecruitingTreatmentEnd Stage Renal Disease (ESRD)1
2RecruitingTreatmentG6PC3 / Glucose 6 Phosphatase Deficiency / Glycogen Storage Disease Type I1
2RecruitingTreatmentHeart Failure With Reduced Ejection Fraction (HFrEF)1
2RecruitingTreatmentType 2 Diabetes Mellitus2
2TerminatedTreatmentDiabetes Mellitus (DM) / Diabetes Mellitus and Heart Failure / Diabetes Type 2 With Heart Failure / Type 2 Diabetes Mellitus (T2DM) With Heart Failure (HF)1
2, 3CompletedHealth Services ResearchPolycystic Ovaries Syndrome1
2, 3CompletedTreatmentInappropriate ADH Syndrome1
2, 3CompletedTreatmentSIADH1
2, 3RecruitingTreatmentHyponatremias / SIAD - Syndrome of Inappropriate Antidiuresis1
3CompletedTreatmentBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
3CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
3CompletedTreatmentHeart Failure2
3CompletedTreatmentHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus2
3CompletedTreatmentHyperglycemias / Type 2 Diabetes Mellitus1
3CompletedTreatmentImpaired Renal Function / Type 2 Diabetes Mellitus1
3CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus2
3CompletedTreatmentType 2 Diabetes Mellitus17
3Not Yet RecruitingTreatmentDiabetic Kidney Disease / Type 2 Diabetes Mellitus1
3Not Yet RecruitingTreatmentHeart Failure1
3Not Yet RecruitingTreatmentInsulin Resistance - Type A / Insulin Resistance - Type B / Insulin resistance syndrome / Lipoatrophic Diabetes Mellitus1
3RecruitingBasic ScienceDiabetic Nephropathies1
3RecruitingPreventionGestational Diabetes Mellitus (GDM)1
3RecruitingPreventionInsulin Resistance / Prediabetic State1
3RecruitingTreatmentAcute Myocardial Infarction (AMI)1
3RecruitingTreatmentChronic Kidney Disease (CKD)1
3RecruitingTreatmentHeart Failure3
3RecruitingTreatmentType 2 Diabetes Mellitus2
3RecruitingTreatmentType1 Diabetes Mellitus1
3RecruitingTreatmentType2 Diabetes Mellitus1
3TerminatedTreatmentType 2 Diabetes Mellitus1
3Unknown StatusTreatmentType 2 Diabetes Mellitus1
3WithdrawnTreatmentType 2 Diabetes Mellitus1
4Active Not RecruitingDiagnosticCardiovascular Disease (CVD) / Diabetes Mellitus (DM)1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedPreventionObesity, Visceral1
4CompletedTreatmentDiabetes Mellitus (DM)1
4CompletedTreatmentDiabetes Mellitus (DM) / Impaired Renal Function / Safety Issues1
4CompletedTreatmentHeart Failure / Type 2 Diabetes Mellitus1
4CompletedTreatmentNon-Alcoholic Fatty Liver Disease (NAFLD) / Type 2 Diabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus2
4Not Yet RecruitingPreventionHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4Not Yet RecruitingTreatmentArrhythmia / Diabetes Mellitus (DM) / Heart Failure1
4Not Yet RecruitingTreatmentNAFLD - Nonalcoholic Fatty Liver Disease / Type2 Diabetes1
4Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
4Not Yet RecruitingTreatmentType 2 Diabetes With Renal Manifestations1
4Not Yet RecruitingTreatmentType2 Diabetes Mellitus1
4RecruitingDiagnosticArrythmia, Cardiac / Coronary Heart Disease (CHD) / Type 2 Diabetes Mellitus1
4RecruitingOtherBMI >30 kg/m2 / Metabolic Syndromes / Type 2 Diabetes Mellitus1
4RecruitingTreatmentCardiovascular Disease (CVD)1
4RecruitingTreatmentCoronary Heart Disease (CHD) / Diabetes Mellitus (DM)1
4RecruitingTreatmentDiabetes Complications / Hypoglycemic Agents / Type 1 Insulin-Dependent Diabetes Mellitus / Vascular Stiffness1
4RecruitingTreatmentDiabetes Mellitus (DM) / Fat; Intolerance, Pancreas1
4RecruitingTreatmentDiabetic Nephropathies / Type 2 Diabetes Mellitus1
4RecruitingTreatmentDiastolic Dysfunction / Type 2 Diabetes Mellitus1
4RecruitingTreatmentFrailty / Obese experiencing rapid weight loss / Sarcopenia / Type 2 Diabetes Mellitus1
4RecruitingTreatmentHeart Failure1
4RecruitingTreatmentHeart Failure, Diastolic / Type 2 Diabetes Mellitus1
4RecruitingTreatmentKidney Transplant; Complications / New Onset Diabetes After Transplant1
4RecruitingTreatmentNAFLD / Type2 Diabetes1
4RecruitingTreatmentNocturnal Hypertension / Type 2 Diabetes Mellitus1
4RecruitingTreatmentType 2 Diabetes Mellitus3
4RecruitingTreatmentType II Diabetes in Subjects BMI 27 to 32 / Type II Diabetes in the Not so Obese1
4RecruitingTreatmentType2 Diabetes2
4TerminatedTreatmentType 2 Diabetes Mellitus2
4WithdrawnTreatmentAdvanced Glycation End Products / Diabetes Mellitus (DM) / SGLT-2 Inhibitors1
4WithdrawnTreatmentDiabetic Nephropathy Type 21
Not AvailableActive Not RecruitingNot AvailableType 2 Diabetes Mellitus8
Not AvailableActive Not RecruitingBasic ScienceType 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableBMI >30 kg/m21
Not AvailableCompletedNot AvailableCardiovascular Disease (CVD) / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableType 2 Diabetes Mellitus4
Not AvailableCompletedBasic ScienceDiabetes After Total Pancreatectomy1
Not AvailableCompletedDiagnosticLate Dumping Syndrome / Post-gastrointestinal bypass surgery / Postprandial Hypoglycemia1
Not AvailableCompletedTreatmentNon Alcoholic Fatty Liver Diseases (NAFLD)1
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus2
Not AvailableNot Yet RecruitingTreatmentReperfusion Injury, Myocardial1
Not AvailableRecruitingNot AvailableType 2 Diabetes Mellitus3
Not AvailableRecruitingNot AvailableType2 Diabetes1
Not AvailableRecruitingOtherArterial Hypertension / Body Weight Changes / Type 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentType1diabetes1
Not AvailableRecruitingTreatmentType2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, film coatedOral
TabletOral10 mg
TabletOral25 mg
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral25 mg/1
TabletOral
Tablet, extended releaseOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
USWO201416191No2014-04-032034-04-03Us
US7407955No2008-08-052023-08-12Us
US6488962No2002-12-032020-06-20Us
US6303661No2001-10-162017-04-24Us
US6890898No2005-05-102019-02-02Us
US7078381No2006-07-182019-02-02Us
US7459428No2008-12-022019-02-02Us
US8119648No2012-02-212023-08-12Us
US8178541No2012-05-152023-08-12Us
US8846695No2014-09-302030-06-04Us
US9173859No2015-11-032027-05-04Us
US8673927No2014-03-182027-05-04Us
US8883805No2014-11-112025-11-26Us
US8551957No2013-10-082029-10-19Us
US7713938No2010-05-112027-04-15Us
US7579449No2009-08-252025-11-05Us
US9949998No2018-04-242034-06-11Us
US9949997No2018-04-242034-05-17Us
US10258637No2014-04-032034-04-03Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.111 mg/mLALOGPS
logP1.79ALOGPS
logP1.66ChemAxon
logS-3.6ALOGPS
pKa (Strongest Acidic)12.57ChemAxon
pKa (Strongest Basic)-3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area108.61 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity113.79 m3·mol-1ChemAxon
Polarizability45.24 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as phenolic glycosides. These are organic compounds containing a phenolic structure attached to a glycosyl moiety. Some examples of phenolic structures include lignans, and flavonoids. Among the sugar units found in natural glycosides are D-glucose, L-Fructose, and L rhamnose.
Kingdom
Organic compounds
Super Class
Organic oxygen compounds
Class
Organooxygen compounds
Sub Class
Carbohydrates and carbohydrate conjugates
Direct Parent
Phenolic glycosides
Alternative Parents
Diphenylmethanes / C-glycosyl compounds / Phenoxy compounds / Phenol ethers / Alkyl aryl ethers / Chlorobenzenes / Aryl chlorides / Oxanes / Monosaccharides / Tetrahydrofurans
show 7 more
Substituents
Phenolic glycoside / Diphenylmethane / C-glycosyl compound / Phenoxy compound / Phenol ether / Alkyl aryl ether / Chlorobenzene / Halobenzene / Aryl chloride / Aryl halide
show 17 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
aromatic ether, monochlorobenzenes, C-glycosyl compound, tetrahydrofuryl ether (CHEBI:82720)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Inhibitor
General Function
Low-affinity glucose:sodium symporter activity
Specific Function
Sodium-dependent glucose transporter. Has a Na(+) to glucose coupling ratio of 1:1.Efficient substrate transport in mammalian kidney is provided by the concerted action of a low affinity high capac...
Gene Name
SLC5A2
Uniprot ID
P31639
Uniprot Name
Sodium/glucose cotransporter 2
Molecular Weight
72895.995 Da
References
  1. Vivian EM: Sodium-glucose co-transporter 2 (SGLT2) inhibitors: a growing class of antidiabetic agents. Drugs Context. 2014 Dec 19;3:212264. doi: 10.7573/dic.212264. eCollection 2014. [PubMed:25598831]

Drug created on March 31, 2015 20:20 / Updated on November 11, 2019 07:01