Identification

Name
Empagliflozin
Accession Number
DB09038
Description

Empagliflozin is an inhibitor of sodium-glucose co-transporter-2 (SGLT2), the transporters primarily responsible for the reabsorption of glucose in the kidney.10 It is used clinically as an adjunct to diet and exercise, often in combination with other drug therapies,15,16,13 for the management of type 2 diabetes mellitus.18

The first known inhibitor of SGLTs, phlorizin, was isolated from the bark of apple trees in 1835 and researched extensively into the 20th century, but was ultimately deemed inappropriate for clinical use given its lack of specificity and significant gastrointestinal side effects.12 Attempts at overcoming these limitations first saw the development of O-glucoside analogs of phlorizin (e.g. remogliflozin etabonate), but these molecules proved relatively pharmacokinetically unstable. The development of C-glucoside phlorizin analogs remedied the issues observed in the previous generation, and led to the FDA approval of canagliflozin in 2013 and both dapagliflozin and empagliflozin in 2014.12 As the most recently approved of the "flozin" drugs, empagliflozin carries the highest selectivity for SGLT2 over SGLT1 (approximately 2700-fold).

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 450.91
Monoisotopic: 450.1445309
Chemical Formula
C23H27ClO7
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
  • Empagliflozine
  • Empagliflozinum
External IDs
  • BI 10773
  • BI-10773
  • BI10773

Pharmacology

Indication

Empagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes. It is also indicated to reduce the risk of cardiovascular death in adult patients with both type 2 diabetes mellitus and established cardiovascular disease.18

Empagliflozin is also available as a combination product with either metformin16 and linagliptin15 as an adjunct to diet and exercise in the management of type 2 diabetes mellitus in adults.

An extended-release combination product containing empagliflozin, metformin, and linagliptin was approved by the FDA in January 2020 for the improvement of glycemic control in adults with type 2 diabetes mellitus when used adjunctively with diet and exercise.13

Empagliflozin is not approved for use in patients with type 1 diabetes.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Empagliflozin lowers blood glucose levels by preventing glucose reabsorption in the kidneys, thereby increasing the amount of glucose excreted in the urine.18 It has a relatively long duration of action requiring only once-daily dosing. Patients should be monitored closely for signs and symptoms of ketoacidosis regardless of blood glucose level as empagliflozin may precipitate diabetic ketoacidosis in the absence of hyperglycemia.18 As its mechanism of action is contingent on the renal excretion of glucose, empagliflozin may be held in cases of acute kidney injury and/or discontinued in patients who develop chronic renal disease.

The overexcretion of glucose creates a sugar-rich urogenital environment which increases the risk of urogenital infections - including urosepsis, pyelonephritis, mycotic infections, and even Fournier's gangrene - in both male and female patients - monitor closely for signs and symptoms of developing infection.18

Mechanism of action

The vast majority of glucose filtered through the glomerulus is reabsorbed within the proximal tubule, primarily via SGLT2 (sodium-glucose linked co-transporter-2) which is responsible for ~90% of the total glucose reabsorption within the kidneys. Na+/K+-ATPase on the basolateral membrane of proximal tubular cells utilize ATP to actively pump Na+ ions into the interstitium surrounding the tubule, establishing a Na+ gradient within the tubular cell. SGLT2 on the apical membrane of these cells then utilize this gradient to facilitate secondary active co-transport of both Na+ and glucose out of the filtrate, thereby reabsorbing glucose back into the blood – inhibiting this co-transport, then, allows for a marked increase in glucosuria and decrease in blood glucose levels.10 Empagliflozin is a potent inhibitor of renal SGLT2 transporters located in the proximal tubules of the kidneys and works to lower blood glucose levels via an increase in glucosuria.18

Empagliflozin also appears to exert cardiovascular benefits - specifically in the prevention of heart failure - independent of its blood glucose-lowering effects, though the exact mechanism of this benefit is not precisely understood. Several theories have been posited, including the potential inhibition of Na+/H+ exchanger (NHE) 1 in the myocardium and NHE3 in the proximal tubule, reduction of pre-load via diuretic/natriuretic effects and reduction of blood pressure, prevention of cardiac fibrosis via suppression of pro-fibrotic markers, and reduction of pro-inflammatory adipokines.11

TargetActionsOrganism
ASodium/glucose cotransporter 2
inhibitor
Humans
Absorption

Following oral administration, peak plasma concentrations are reached in approximately 1.5 hours (Tmax). At steady-state, plasma AUC and Cmax were 1870 nmol·h/L and 259 nmol/L, respectively, following therapy with empagliflozin 10mg daily and 4740 nmol·h/L and 687 nmol/L, respectively, following therapy with empagliflozin 25mg daily.18 Administration with food does not significantly affect the absorption of empagliflozin.

Volume of distribution

The estimated apparent steady-state volume of distribution is 73.8 L.18

Protein binding

Empagliflozin is approximately 86.2% protein-bound in plasma.18

Metabolism

Empagliflozin undergoes minimal metabolism. It is primarily metabolized via glucuronidation by 5'-diphospho-glucuronosyltransferases 2B7, 1A3, 1A8, and 1A9 to yield three glucuronide metabolites: 2-O-, 3-O-, and 6-O-glucuronide.18 No metabolite represented more than 10% of total drug-related material.

Hover over products below to view reaction partners

Route of elimination

After oral administration of radiolabeled empagliflozin approximately 41.2% of the administered dose was found eliminated in feces and 54.4% eliminated in urine. The majority of radioactivity in the feces was due to unchanged parent drug while approximately half of the radioactivity in urine was due to unchanged parent drug.18

Half-life

The apparent terminal elimination half-life was found to be 12.4 h based on population pharmacokinetic analysis.18

Clearance

Apparent oral clearance was found to be 10.6 L/h based on a population pharmacokinetic analysis.18

Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

Experience with empagliflozin overdose is limited - employ standard symptomatic and supportive measures, as well as gastric decontamination when appropriate. The use of hemodialysis in empagliflozin overdose has not been studied but is unlikely to be of benefit given the drug's relatively high protein-binding.18

Affected organisms
  • Humans and other mammals
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
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Empagliflozin.
AcebutololThe therapeutic efficacy of Acebutolol can be increased when used in combination with Empagliflozin.
AcetazolamideAcetazolamide may increase the diuretic activities of Empagliflozin.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Acetohexamide is combined with Empagliflozin.
Acetyl sulfisoxazoleThe therapeutic efficacy of Empagliflozin can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidThe risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Empagliflozin.
AlbiglutideThe risk or severity of hypoglycemia can be increased when Empagliflozin is combined with Albiglutide.
AlclometasoneThe risk or severity of hyperglycemia can be increased when Alclometasone is combined with Empagliflozin.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Empagliflozin.
AliskirenThe risk or severity of adverse effects can be increased when Empagliflozin is combined with Aliskiren.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Products

Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
JardianceTablet, film coated25 mg/1OralAphena Pharma Solutions - Tennessee, LLC2014-08-01Not applicableUS flag
JardianceTablet, film coated25 mg/1OralA-S Medication Solutions2014-08-01Not applicableUS flag
JardianceTablet, film coated25 mg/1OralREMEDYREPACK INC.2019-11-22Not applicableUS flag
JardianceTablet, film coated10 mg/1OralCardinal Health2014-08-01Not applicableUS flag
JardianceTabletOralBoehringer Ingelheim (Canada) Ltd Ltee2015-08-11Not applicableCanada flag
JardianceTablet, film coated25 mg/1OralBoehringer Ingelheim Pharmaceuticals, Inc.2014-08-01Not applicableUS flag
JardianceTablet, film coated10 mg/1OralA-S Medication Solutions2014-08-01Not applicableUS flag
JardianceTablet, film coated10 mg/1OralREMEDYREPACK INC.2019-03-27Not applicableUS flag
JardianceTabletOralBoehringer Ingelheim (Canada) Ltd Ltee2015-08-11Not applicableCanada flag
JardianceTablet, film coated10 mg/1OralBoehringer Ingelheim Pharmaceuticals, Inc.2014-08-01Not applicableUS flag00597 0152 90 nlmimage10 8d40c686
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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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 EndRegionImage
GlyxambiEmpagliflozin (10 mg/1) + Linagliptin (5 mg/1)Tablet, film coatedOralREMEDYREPACK INC.2019-04-29Not applicableUS flag
GlyxambiEmpagliflozin (10 mg) + Linagliptin (5 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-12-21Not applicableCanada flag
GlyxambiEmpagliflozin (25 mg/1) + Linagliptin (5 mg/1)Tablet, film coatedOralBoehringer Ingelheim Pharmaceuticals, Inc.2015-01-30Not applicableUS flag
GlyxambiEmpagliflozin (10 mg/1) + Linagliptin (5 mg/1)Tablet, film coatedOralBoehringer Ingelheim Pharmaceuticals, Inc.2015-01-30Not applicableUS flag0597 018220180913 8702 q7fevz
GlyxambiEmpagliflozin (25 mg) + Linagliptin (5 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-12-21Not applicableCanada flag
SynjardyEmpagliflozin (12.5 mg) + Metformin hydrochloride (500 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-08-03Not applicableCanada flag
SynjardyEmpagliflozin (5 mg) + Metformin hydrochloride (850 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-08-03Not applicableCanada flag
SynjardyEmpagliflozin (5 mg/1) + Metformin hydrochloride (1000 mg/1)TabletOralBoehringer Ingelheim Pharmaceuticals, Inc.2015-08-26Not applicableUS flag
SynjardyEmpagliflozin (5 mg) + Metformin hydrochloride (1000 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-08-03Not applicableCanada flag
SynjardyEmpagliflozin (12.5 mg) + Metformin hydrochloride (1000 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-08-03Not applicableCanada flag

Categories

ATC Codes
A10BD19 — Linagliptin and empagliflozinA10BD20 — Metformin and empagliflozinA10BK03 — Empagliflozin
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Alcohol / Alkyl aryl ether / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Benzenoid / C-glycosyl compound / Chlorobenzene / Dialkyl ether / Diphenylmethane
show 17 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
aromatic ether, monochlorobenzenes, C-glycosyl compound, tetrahydrofuryl ether (CHEBI:82720)

Chemical Identifiers

UNII
HDC1R2M35U
CAS number
864070-44-0
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

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.

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]
  10. Kalra S: Sodium Glucose Co-Transporter-2 (SGLT2) Inhibitors: A Review of Their Basic and Clinical Pharmacology. Diabetes Ther. 2014 Dec;5(2):355-66. doi: 10.1007/s13300-014-0089-4. Epub 2014 Nov 26. [PubMed:25424969]
  11. Verma S, McMurray JJV: SGLT2 inhibitors and mechanisms of cardiovascular benefit: a state-of-the-art review. Diabetologia. 2018 Oct;61(10):2108-2117. doi: 10.1007/s00125-018-4670-7. Epub 2018 Aug 22. [PubMed:30132036]
  12. Choi CI: Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitors from Natural Products: Discovery of Next-Generation Antihyperglycemic Agents. Molecules. 2016 Aug 27;21(9). pii: molecules21091136. doi: 10.3390/molecules21091136. [PubMed:27618891]
  13. FDA Approved Drug Products: Trijardy XR (empagliflozin/linagliptin/metformin) extended-release tablets [Link]
  14. FDA Summary Review: Empagliflozin [Link]
  15. FDA Approved Drug Products: Glyxambi (empagliflozin/linagliptin) oral tablets [Link]
  16. FDA Approved Drug Products: Synjardy (empagliflozin/metformin) oral tablets [Link]
  17. FDA Approved Drug Products: Synjardy XR (empagliflozin/metformin) extended-release tablets [Link]
  18. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
  19. Health Canada Product Monograph: Jardiance (empagliflozin) oral tablets [Link]
  20. CaymanChem: Empagliflozin MSDS [Link]
KEGG Drug
D10459
PubChem Compound
11949646
PubChem Substance
310264986
ChemSpider
10123957
BindingDB
150162
RxNav
1545653
ChEBI
82720
ChEMBL
CHEMBL2107830
ZINC
ZINC000036520252
PharmGKB
PA166163327
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Empagliflozin
AHFS Codes
  • 68:20.18 — Sodium-glucose Cotransporter 2 (SGLT2) Inhibitors

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingDiagnosticCardiovascular Heart Disease / Diabetes1
4Active Not RecruitingTreatmentHeart Failure1
4Active Not RecruitingTreatmentType II Diabetes in Subjects BMI 27 to 32 / Type II Diabetes in the Not so Obese1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedPreventionObesity, Visceral1
4CompletedTreatmentCardiovascular Heart Disease1
4CompletedTreatmentCoronary Artery Disease (CAD) / Diabetes Mellitus / Percutaneous Coronary Intervention (PCI)1
4CompletedTreatmentDiabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus / Heart Failure1
4CompletedTreatmentDiabetes Mellitus / Impaired kidney function / Safety Issues1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral
Tablet, coatedOral10 mg
Tablet, coatedOral25 mg
TabletOral
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral10 mg
Tablet, coated10 mg
Tablet
Tablet, coated25 mg
Tablet, delayed releaseOral1000 mg
Tablet, film coatedOral12.5 mg
Tablet, film coatedOral25 mg
TabletOral
Tablet, coatedOral12.5 mg
Tablet, coatedOral5 mg
Tablet, extended releaseOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
USWO201416191No2014-04-032034-04-03US flag
US7407955No2008-08-052023-08-12US flag
US6488962No2002-12-032020-06-20US flag
US6303661No2001-10-162017-04-24US flag
US6890898No2005-05-102019-02-02US flag
US7078381No2006-07-182019-02-02US flag
US7459428No2008-12-022019-02-02US flag
US8119648No2012-02-212023-08-12US flag
US8178541No2012-05-152023-08-12US flag
US8846695No2014-09-302030-06-04US flag
US9173859No2015-11-032027-05-04US flag
US8673927No2014-03-182027-05-04US flag
US8883805No2014-11-112025-11-26US flag
US9155705No2015-10-132030-05-21US flag
US8551957No2013-10-082029-10-19US flag
US7713938No2010-05-112027-04-15US flag
US7579449No2009-08-252025-11-05US flag
US9415016No2016-08-162029-04-02US flag
US9949998No2018-04-242034-06-11US flag
US9949997No2018-04-242034-05-17US flag
US10022379No2018-07-172029-04-02US flag
US10258637No2019-04-162034-04-03US flag
US10406172No2019-09-102030-06-15US flag
US10596120No2012-03-072032-03-07US flag
US10610489No2010-09-302030-09-30US flag
Additional Data Available
  • Filed On
    Filed On

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

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility0.28 mg/mLCanadian monograph
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
Polarizability46.12 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

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
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]
  2. DailyMed Label: Jardiance (empagliflozin) tablet, film coated [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
Gene Name
UGT2B7
Uniprot ID
P16662
Uniprot Name
UDP-glucuronosyltransferase 2B7
Molecular Weight
60694.12 Da
References
  1. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A3
Uniprot ID
P35503
Uniprot Name
UDP-glucuronosyltransferase 1-3
Molecular Weight
60337.835 Da
References
  1. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A8
Uniprot ID
Q9HAW9
Uniprot Name
UDP-glucuronosyltransferase 1-8
Molecular Weight
59741.035 Da
References
  1. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
Gene Name
UGT1A9
Uniprot ID
O60656
Uniprot Name
UDP-glucuronosyltransferase 1-9
Molecular Weight
59940.495 Da
References
  1. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]

Drug created on March 31, 2015 20:20 / Updated on September 27, 2020 08:17

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