Empagliflozin
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
- 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
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- 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
- Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects
- 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
Target Actions Organism ASodium/glucose cotransporter 2 inhibitorHumans - 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
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- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Empagliflozin. Acebutolol The therapeutic efficacy of Acebutolol can be increased when used in combination with Empagliflozin. Acetazolamide Acetazolamide may increase the diuretic activities of Empagliflozin. Acetohexamide The risk or severity of hypoglycemia can be increased when Acetohexamide is combined with Empagliflozin. Acetyl sulfisoxazole The therapeutic efficacy of Empagliflozin can be increased when used in combination with Acetyl sulfisoxazole. Acetylsalicylic acid The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Empagliflozin. Albiglutide The risk or severity of hypoglycemia can be increased when Empagliflozin is combined with Albiglutide. Alclometasone The risk or severity of hyperglycemia can be increased when Alclometasone is combined with Empagliflozin. Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Empagliflozin. Aliskiren The risk or severity of adverse effects can be increased when Empagliflozin is combined with Aliskiren. Improve patient outcomesBuild effective decision support tools with the industry’s most comprehensive drug-drug interaction checker.Learn more - Food Interactions
- Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.
Products
- Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets
- Product Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Jardiance Tablet, film coated 10 mg Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Jardiance Tablet, film coated 10 mg/1 Oral Cardinal Health 2014-08-01 Not applicable US Jardiance Tablet, film coated 25 mg Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Jardiance Tablet, film coated 10 mg Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Jardiance Tablet, film coated 25 mg Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Jardiance Tablet, film coated 10 mg Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Jardiance Tablet, film coated 25 mg Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Jardiance Tablet, film coated 25 mg/1 Oral Boehringer Ingelheim Pharmaceuticals, Inc. 2014-08-01 Not applicable US Jardiance Tablet, film coated 10 mg Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Jardiance Tablet, film coated 10 mg/1 Oral A-S Medication Solutions 2014-08-01 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Glyxambi Empagliflozin (10 mg) + Linagliptin (5 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Glyxambi Empagliflozin (10 mg) + Linagliptin (5 mg) Tablet Oral Boehringer Ingelheim (Canada) Ltd Ltee 2016-12-21 Not applicable Canada Glyxambi Empagliflozin (25 mg) + Linagliptin (5 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Glyxambi Empagliflozin (25 mg/1) + Linagliptin (5 mg/1) Tablet, film coated Oral Boehringer Ingelheim Pharmaceuticals, Inc. 2015-01-30 Not applicable US Glyxambi Empagliflozin (25 mg) + Linagliptin (5 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Glyxambi Empagliflozin (10 mg) + Linagliptin (5 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Glyxambi Empagliflozin (10 mg) + Linagliptin (5 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Glyxambi Empagliflozin (25 mg) + Linagliptin (5 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Glyxambi Empagliflozin (25 mg) + Linagliptin (5 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU Glyxambi Empagliflozin (10 mg) + Linagliptin (5 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU
Categories
- ATC Codes
- A10BD19 — Linagliptin and empagliflozin
- A10BD — Combinations of oral blood glucose lowering drugs
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- A10BD — Combinations of oral blood glucose lowering drugs
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Alimentary Tract and Metabolism
- BCRP/ABCG2 Substrates
- Benzene Derivatives
- Blood Glucose Lowering Agents
- Diuretics
- Drugs that are Mainly Renally Excreted
- Drugs Used in Diabetes
- Glycosides
- Hypotensive Agents
- OAT3/SLC22A8 Substrates
- OATP1B1/SLCO1B1 Substrates
- OATP1B3 substrates
- P-glycoprotein substrates
- Sodium-glucose co-transporter 2 (SGLT2) inhibitors
- Sodium-glucose Cotransporter 2 (SGLT2) Inhibitors
- Sodium-Glucose Transporter 2 Inhibitors
- UGT1A3 substrates
- UGT1A9 Substrates
- UGT2B7 substrates
- 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
- OC[C@H]1O[C@H]([C@H](O)[C@@H](O)[C@@H]1O)C1=CC=C(Cl)C(CC2=CC=C(O[C@H]3CCOC3)C=C2)=C1
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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- Authors unspecified: Empagliflozin (Jardiance) for diabetes. Med Lett Drugs Ther. 2014 Oct 13;56(1453):99-100. [PubMed:25296258]
- 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]
- 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]
- 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]
- 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]
- FDA Approved Drug Products: Trijardy XR (empagliflozin/linagliptin/metformin) extended-release tablets [Link]
- FDA Summary Review: Empagliflozin [Link]
- FDA Approved Drug Products: Glyxambi (empagliflozin/linagliptin) oral tablets [Link]
- FDA Approved Drug Products: Synjardy (empagliflozin/metformin) oral tablets [Link]
- FDA Approved Drug Products: Synjardy XR (empagliflozin/metformin) extended-release tablets [Link]
- FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
- Health Canada Product Monograph: Jardiance (empagliflozin) oral tablets [Link]
- CaymanChem: Empagliflozin MSDS [Link]
- External Links
- KEGG Drug
- D10459
- PubChem Compound
- 11949646
- PubChem Substance
- 310264986
- ChemSpider
- 10123957
- BindingDB
- 150162
- 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
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Heart Failure 1 4 Active Not Recruiting Treatment Type II Diabetes in Subjects BMI 27 to 32 1 4 Completed Basic Science Type 2 Diabetes Mellitus 1 4 Completed Prevention Obesity, Visceral 1 4 Completed Treatment Cardiovascular Disease (CVD) 1 4 Completed Treatment Coronary Artery Disease (CAD) / Diabetes Mellitus / Percutaneous Coronary Intervention (PCI) 1 4 Completed Treatment Coronary Heart Disease (CHD) / Diabetes Mellitus 1 4 Completed Treatment Diabetes Mellitus 1 4 Completed Treatment Diabetes Mellitus / Heart Failure 1 4 Completed Treatment Diabetes Mellitus / Impaired kidney function / Safety Issues 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral Tablet, film coated Oral 5 mg Tablet Oral 10 mg Tablet Oral 25 mg Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 25 mg/1 Tablet, coated Oral Tablet, coated Oral 10 mg Tablet, film coated Oral 10 mg Tablet, coated Oral 25 mg Tablet, film coated Oral 25 mg Tablet, film coated Oral 1000 MG Tablet, film coated Oral 500 MG Tablet, film coated Oral 850 MG Tablet, delayed release Oral 1000 mg Tablet, film coated Oral 12.5 mg Tablet Oral Tablet, coated Oral 12.5 mg Tablet, coated Oral 5 mg Tablet, extended release Oral Tablet, coated Oral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region USWO201416191 No 2014-04-03 2034-04-03 US US7407955 No 2008-08-05 2023-08-12 US US6488962 No 2002-12-03 2020-06-20 US US6303661 No 2001-10-16 2017-04-24 US US6890898 No 2005-05-10 2019-02-02 US US7078381 No 2006-07-18 2019-02-02 US US7459428 No 2008-12-02 2019-02-02 US US8119648 No 2012-02-21 2023-08-12 US US8178541 No 2012-05-15 2023-08-12 US US8846695 No 2014-09-30 2030-06-04 US US9173859 No 2015-11-03 2027-05-04 US US8673927 No 2014-03-18 2027-05-04 US US8883805 No 2014-11-11 2025-11-26 US US9155705 No 2015-10-13 2030-05-21 US US8551957 No 2013-10-08 2029-10-19 US US7713938 No 2010-05-11 2027-04-15 US US7579449 No 2009-08-25 2025-11-05 US US9415016 No 2016-08-16 2029-04-02 US US9949998 No 2018-04-24 2034-06-11 US US9949997 No 2018-04-24 2034-05-17 US US10022379 No 2018-07-17 2029-04-02 US US10258637 No 2019-04-16 2034-04-03 US US10406172 No 2019-09-10 2030-06-15 US US10596120 No 2012-03-07 2032-03-07 US US10610489 No 2010-09-30 2030-09-30 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 0.28 mg/mL Canadian monograph - Predicted Properties
Property Value Source Water Solubility 0.111 mg/mL ALOGPS logP 1.79 ALOGPS logP 1.66 ChemAxon logS -3.6 ALOGPS pKa (Strongest Acidic) 12.57 ChemAxon pKa (Strongest Basic) -3 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 7 ChemAxon Hydrogen Donor Count 4 ChemAxon Polar Surface Area 108.61 Å2 ChemAxon Rotatable Bond Count 6 ChemAxon Refractivity 113.79 m3·mol-1 ChemAxon Polarizability 46.12 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not 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
- 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]
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets [Link]
Drug created on April 01, 2015 02:20 / Updated on February 24, 2021 19:34