Identification
- Summary
Dapagliflozin is a sodium-glucose cotransporter 2 inhibitor used in the management of type 2 diabetes mellitus.
- Brand Names
- Edistride, Farxiga, Forxiga, Qtern, Qternmet, Xigduo
- Generic Name
- Dapagliflozin
- DrugBank Accession Number
- DB06292
- Background
Dapagliflozin is a sodium-glucose cotransporter 2 inhibitor indicated for managing diabetes mellitus type 2.1 When combined with diet and exercise in adults, dapagliflozin helps to improve glycemic control by inhibiting glucose reabsorption in the proximal tubule of the nephron and causing glycosuria.1 Dapagliflozin was approved by the FDA on Jan 08, 2014.3
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Dapagliflozin (DB06292)
- Weight
- Average: 408.873
Monoisotopic: 408.133966239 - Chemical Formula
- C21H25ClO6
- Synonyms
- (2S,3R,4R,5S,6R)-2-(4-Chloro-3-(4-ethoxybenzyl)phenyl)-6- (hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol
- Dapagliflozin
- Dapagliflozina
- External IDs
- BMS 512148
- BMS-512148
Pharmacology
- Indication
Dapagliflozin is indicated as an adjunct treatment to improve glycemic control in adult patients with type 2 diabetes mellitus along with diet and exercise7,1,2.For patients with chronic kidney disease at risk of progression, dapagliflozin in used to reduce the risk of sustained eGFR decline, end-stage kidney disease, cardiovascular death, and hospitalization for heart failure.7 Dapagliflozin is also indicated to either reduce the risk of cardiovascular death, hospitalization for heart failure, and urgent heart failure visit in adults with heart failure or reduce the risk of hospitalization for heart failure in adults with type 2 diabetes mellitus and either established cardiovascular disease or multiple cardiovascular risk factors.7 Combination products with dapagliflozin also exist, either as a dapagliflozin-saxagliptin or dapagliflozin-metformin hydrochloride formulation.5,6 Both are used as an adjunct treatment to diet and exercise to improve glycemic control in adult with type 2 diabetes.5,6
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Dapagliflozin inhibits the sodium-glucose contransporter 2(SGLT2) which is primarily located in the proximal tubule of the nephron1. SGLT2 facilitates 90% of glucose reabsorption in the kidneys and so its inhibition allows for glucose to be excreted in the urine1. This excretion allows for better glycemic control and potentially weight loss in patients with type 2 diabetes mellitus1.
- Mechanism of action
Dapagliflozin inhibits the sodium-glucose contransporter 2(SGLT2) which is primarily located in the proximal tubule of the nephron1. SGLT2 facilitates 90% of glucose reabsorption in the kidneys and so its inhibition allows for glucose to be excreted in the urine1. This excretion allows for better glycemic control and potentially weight loss in patients with type 2 diabetes mellitus1.
Target Actions Organism ASodium/glucose cotransporter 2 antagonistinhibitorHumans - Absorption
Oral dapagliflozin reaches a maximum concentration within 1 hour of administration when patients have been fasting1. When patients have consumed a high fat meal, the time to maximum concentration increases to 2 hours and the maximum concentration decreases by half though a dose adjustment is not necessaryLabel. Oral dapagliflozin is 78% bioavailableLabel.
- Volume of distribution
118L2.
- Protein binding
- Metabolism
Dapagliflozin is primarily glucuronidated to become the inactive 3-O-glucuronide metabolite(60.7%)Label,1,2. Dapagliflozin also produces another minor glucuronidated metabolite(5.4%), a de-ethylated metabolite(<5%), and a hydroxylated metabolite(<5%)1. Metabolism of dapagliflozin is mediated by cytochrome p-450(CYP)1A1, CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP3A4, uridine diphosphate glucuronyltransferase(UGT)1A9, UGT2B4, and UGT2B72. Glucuronidation to the major metabolite is mediated by UGT1A9Label,2.
Hover over products below to view reaction partners
- Route of elimination
75.2% of dapagliflozin is recovered in the urine with 1.6% of the dose unchanged by metabolism1. 21% of the dose is excreted in the feces with 15% of the dose unchanged by metabolismLabel.
- Half-life
After a single oral dose of 10 mg of dapagliflozin, the mean plasma terminal half-life is approximately 12.9 hours.7 In healthy subjects given a single oral dose of 50 mg of dapagliflozin, the mean terminal half-life was 13.8 hours.1
- Clearance
Oral plasma clearance was 4.9 mL/min/kg, and renal clearance was 5.6 mL/min1.
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Age, gender, race, and body weight do not affect dapagliflozin dosing requirementsLabel,2. Although age does not affect dosing requirements, safety has not been established in pediatric populations and patients at an especially advanced age may be more susceptible to adverse effectsLabel. Animal studies in pregnancy showed no fetal toxicity in the first trimester but exposure later in pregnancy was associated with renal pelvic dilatation and maternal toxicity at much higher doses than the maximum recommended human doseLabel. Due to this data, dapagliflozin is not recommended in the second and third trimester of pregnancyLabel. Dapagliflozin is excreted in milk from rats, though this may not necessarily be the case in humansLabel. Children under 2 years old who are exposed to dapagliflozin may be at risk of improper kidney developmentLabel. Dapagliflozin is not recommended in patients with a creatinine clearance below 45mL/min and is contraindicated in patients with creatinine clearance below 30mL/minLabel. Dose adjustments are not necessary in patients with hepatic impairment at any stage, although the risk and benefit to the patient must be assessed as there is limited data on dapagliflozin use in this populationLabel.
- 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 softwareAbaloparatide The risk or severity of adverse effects can be increased when Abaloparatide is combined with Dapagliflozin. Abametapir The serum concentration of Dapagliflozin can be increased when it is combined with Abametapir. Abatacept The metabolism of Dapagliflozin can be increased when combined with Abatacept. Abiraterone The serum concentration of Dapagliflozin can be increased when it is combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Dapagliflozin. Acarbose Dapagliflozin may increase the hypoglycemic activities of Acarbose. Acebutolol The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Acebutolol. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Dapagliflozin. Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Dapagliflozin. Acetazolamide The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Acetazolamide. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Avoid excessive or chronic alcohol consumption. Binge drinking or drinking alcohol often may predispose patients to ketoacidosis.
- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Dapagliflozin propanediol monohydrate 887K2391VH 960404-48-2 GOADIQFWSVMMRJ-UPGAGZFNSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Dapagliflozin Viatris Tablet, film coated 5 mg Oral Viatris Limited 2023-04-04 Not applicable EU 
Dapagliflozin Viatris Tablet, film coated 10 mg Oral Viatris Limited 2023-04-04 Not applicable EU Dapagliflozin Viatris Tablet, film coated 5 mg Oral Viatris Limited 2023-04-04 Not applicable EU Dapagliflozin Viatris Tablet, film coated 5 mg Oral Viatris Limited 2023-04-04 Not applicable EU Dapagliflozin Viatris Tablet, film coated 10 mg Oral Viatris Limited 2023-04-04 Not applicable EU Dapagliflozin Viatris Tablet, film coated 5 mg Oral Viatris Limited 2023-04-04 Not applicable EU Dapagliflozin Viatris Tablet, film coated 5 mg Oral Viatris Limited 2023-04-04 Not applicable EU Dapagliflozin Viatris Tablet, film coated 10 mg Oral Viatris Limited 2023-04-04 Not applicable EU Dapagliflozin Viatris Tablet, film coated 5 mg Oral Viatris Limited 2023-04-04 Not applicable EU Dapagliflozin Viatris Tablet, film coated 10 mg Oral Viatris Limited 2023-04-04 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ag-dapagliflozin Tablet 5 mg Oral Angita Pharma Inc. 2023-05-15 Not applicable Canada 
Ag-dapagliflozin Tablet 10 mg Oral Angita Pharma Inc. 2023-05-15 Not applicable Canada Apo-dapagliflozin Tablet 5 mg Oral Apotex Corporation 2023-05-16 Not applicable Canada Apo-dapagliflozin Tablet 10 mg Oral Apotex Corporation 2023-05-16 Not applicable Canada Auro-dapagliflozin Tablet 10 mg Oral Auro Pharma Inc 2023-05-16 Not applicable Canada Auro-dapagliflozin Tablet 5 mg Oral Auro Pharma Inc 2023-05-16 Not applicable Canada Jamp Dapagliflozin Tablet 10 mg Oral Jamp Pharma Corporation 2023-05-15 Not applicable Canada Jamp Dapagliflozin Tablet 5 mg Oral Jamp Pharma Corporation 2023-05-15 Not applicable Canada Nat-dapagliflozin Tablet 5 mg Oral Natco Pharma Limited Not applicable Not applicable Canada Nat-dapagliflozin Tablet 10 mg Oral Natco Pharma Limited Not applicable Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Apo-dapagliflozin-metformin Dapagliflozin (5 mg) + Metformin hydrochloride (850 mg) Tablet Oral Apotex Corporation Not applicable Not applicable Canada Apo-dapagliflozin-metformin Dapagliflozin (5 mg) + Metformin hydrochloride (1000 mg) Tablet Oral Apotex Corporation Not applicable Not applicable Canada Auro-dapagliflozin / Metformin Dapagliflozin (5 mg) + Metformin hydrochloride (1000 mg) Tablet Oral Auro Pharma Inc 2023-05-16 Not applicable Canada Auro-dapagliflozin / Metformin Dapagliflozin (5 mg) + Metformin hydrochloride (850 mg) Tablet Oral Auro Pharma Inc 2023-05-16 Not applicable Canada Ebymect Dapagliflozin propanediol monohydrate (5 mg) + Metformin hydrochloride (1000 mg) Tablet, film coated Oral Astra Zeneca Ab 2021-02-10 Not applicable EU Ebymect Dapagliflozin propanediol monohydrate (5 mg) + Metformin hydrochloride (1000 mg) Tablet, film coated Oral Astra Zeneca Ab 2021-02-10 Not applicable EU Ebymect Dapagliflozin propanediol monohydrate (5 mg) + Metformin hydrochloride (850 mg) Tablet, film coated Oral Astra Zeneca Ab 2021-02-10 Not applicable EU Ebymect Dapagliflozin propanediol monohydrate (5 mg) + Metformin hydrochloride (850 mg) Tablet, film coated Oral Astra Zeneca Ab 2021-02-10 Not applicable EU Ebymect Dapagliflozin propanediol monohydrate (5 mg) + Metformin hydrochloride (1000 mg) Tablet, film coated Oral Astra Zeneca Ab 2021-02-10 Not applicable EU Ebymect Dapagliflozin propanediol monohydrate (5 mg) + Metformin hydrochloride (1000 mg) Tablet, film coated Oral Astra Zeneca Ab 2021-02-10 Not applicable EU
Categories
- ATC Codes
- A10BK01 — Dapagliflozin
- A10BK — Sodium-glucose co-transporter 2 (SGLT2) inhibitors
- 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
- 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
- Benzene Derivatives
- Blood Glucose Lowering Agents
- Carbohydrates
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2A6 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Diuretics
- Drugs Used in Diabetes
- Glycosides
- Hypotensive Agents
- Oral Hypoglycemics
- P-glycoprotein substrates
- Sodium-glucose Cotransporter 2 (SGLT2) Inhibitors
- Sodium-Glucose Transport Proteins, antagonists & inhibitors
- Sodium-Glucose Transporter 2 Inhibitors
- 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 / Hexoses / C-glycosyl compounds / Phenoxy compounds / Phenol ethers / Alkyl aryl ethers / Chlorobenzenes / Aryl chlorides / Oxanes / Secondary alcohols show 6 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, organochlorine compound, C-glycosyl compound (CHEBI:85078)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 1ULL0QJ8UC
- CAS number
- 461432-26-8
- InChI Key
- JVHXJTBJCFBINQ-ADAARDCZSA-N
- InChI
- InChI=1S/C21H25ClO6/c1-2-27-15-6-3-12(4-7-15)9-14-10-13(5-8-16(14)22)21-20(26)19(25)18(24)17(11-23)28-21/h3-8,10,17-21,23-26H,2,9,11H2,1H3/t17-,18-,19+,20-,21+/m1/s1
- IUPAC Name
- (2S,3R,4R,5S,6R)-2-{4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl}-6-(hydroxymethyl)oxane-3,4,5-triol
- SMILES
- CCOC1=CC=C(CC2=C(Cl)C=CC(=C2)[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)C=C1
References
- General References
- Obermeier M, Yao M, Khanna A, Koplowitz B, Zhu M, Li W, Komoroski B, Kasichayanula S, Discenza L, Washburn W, Meng W, Ellsworth BA, Whaley JM, Humphreys WG: In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans. Drug Metab Dispos. 2010 Mar;38(3):405-14. doi: 10.1124/dmd.109.029165. Epub 2009 Dec 8. [Article]
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
- FDA Drug Approval Package: Dapagliflozin [Link]
- FDA Approved Drug Products: Farxiga Dapagliflozin Oral Tablets [Link]
- FDA Approved Drug Products: Qtern (dapagliflozin/saxagliptin) tablets for oral use [Link]
- FDA Approved Drug Products: Xigduo XR (metformin hydrochloride/dapagliflozin) extended-release tablets for oral use [Link]
- FDA Approved Drug Products: FARXIGA® (dapagliflozin) tablets, for oral use (May 2023) [Link]
- External Links
- KEGG Drug
- D08897
- PubChem Compound
- 9887712
- PubChem Substance
- 175427068
- ChemSpider
- 8063384
- BindingDB
- 20880
- 1488564
- ChEBI
- 85078
- ChEMBL
- CHEMBL429910
- ZINC
- ZINC000003819138
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Dapagliflozin
- FDA label
- Download (1.22 MB)
- MSDS
- Download (62.4 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Basic Science Type 2 Diabetes Mellitus 1 4 Active Not Recruiting Prevention BMD / Lupus Nephritis / SGLT2 Inhibitors 1 4 Active Not Recruiting Treatment Atrial Fibrillation 1 4 Active Not Recruiting Treatment Coronavirus Disease 2019 (COVID‑19) 1 4 Active Not Recruiting Treatment Hearth Failure With Reduced Ejection Fraction (HFrEF) / Type 2 Diabetes Mellitus 1 4 Active Not Recruiting Treatment Type 2 Diabetes Mellitus 5 4 Completed Basic Science Diabetes Mellitus / Heart Failure 1 4 Completed Basic Science High Cholesterol / Type 2 Diabetes Mellitus 1 4 Completed Basic Science Impaired Glucose Tolerance / Substrate Oxidation 1 4 Completed Basic Science Skeletal Muscle Insulin Sensitivity / Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 5 mg/1 Tablet Oral 10 mg Tablet Oral 5 mg Tablet, film coated Oral Tablet, coated Oral 10 mg Tablet, film coated Oral 10 mg Tablet, film coated Oral 5 mg Tablet, film coated Oral Tablet, coated Oral Tablet Oral Tablet, film coated, extended release Oral Tablet, extended release Oral Tablet, film coated, extended release Oral 10 mg Tablet, film coated, extended release Oral 5 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8216180 Yes 2012-07-10 2028-07-12 US 
US8439864 Yes 2013-05-14 2028-09-25 US US6667061 Yes 2003-12-23 2020-11-25 US US6495164 No 2002-12-17 2020-05-25 US US6872700 No 2005-03-29 2020-01-14 US US6956026 No 2005-10-18 2018-01-07 US US7741269 No 2010-06-22 2018-01-07 US US9238076 Yes 2016-01-19 2024-10-15 US US8906851 Yes 2014-12-09 2027-02-18 US US7612176 Yes 2009-11-03 2025-10-13 US US8431685 Yes 2013-04-30 2025-10-13 US US8461105 Yes 2013-06-11 2025-10-13 US US8329648 Yes 2012-12-11 2027-02-18 US US7456254 Yes 2008-11-25 2025-12-30 US US7563871 Yes 2009-07-21 2024-10-15 US US6824822 Yes 2004-11-30 2023-04-09 US US6479065 No 2002-11-12 2020-08-10 US US7223440 Yes 2007-05-29 2022-03-03 US USRE44186 No 2013-04-30 2023-07-31 US US8628799 No 2014-01-14 2025-07-13 US US8685934 No 2014-04-01 2030-05-26 US US8501698 Yes 2013-08-06 2027-12-20 US US6414126 No 2002-07-02 2020-10-04 US US6515117 Yes 2003-02-04 2026-04-04 US US6936590 No 2005-08-30 2020-10-04 US US9198925 No 2015-12-01 2020-10-04 US US7919598 No 2011-04-05 2029-12-16 US US8361972 Yes 2013-01-29 2028-09-21 US US8716251 No 2014-05-06 2028-03-21 US US7851502 No 2010-12-14 2028-08-19 US US8221786 No 2012-07-17 2028-03-21 US US9616028 No 2017-04-11 2030-11-12 US US9320853 Yes 2016-04-26 2028-09-25 US US8827963 Yes 2014-09-09 2029-08-04 US US8712615 No 2014-04-29 2030-01-18 US US8998876 Yes 2015-04-07 2030-07-07 US US8758292 Yes 2014-06-24 2028-05-12 US US8690837 Yes 2014-04-08 2029-11-19 US US8721615 Yes 2014-05-13 2030-07-18 US US10973836 No 2021-04-13 2040-03-09 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 65 [MSDS] boiling point (°C) 609 [MSDS] logP 2.7 [MSDS] - Predicted Properties
Property Value Source Water Solubility 0.173 mg/mL ALOGPS logP 2.52 ALOGPS logP 2.11 Chemaxon logS -3.4 ALOGPS pKa (Strongest Acidic) 12.57 Chemaxon pKa (Strongest Basic) -3 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 99.38 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 104.93 m3·mol-1 Chemaxon Polarizability 42.88 Å3 Chemaxon Number of Rings 3 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
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AntagonistInhibitor
- 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
- Obermeier M, Yao M, Khanna A, Koplowitz B, Zhu M, Li W, Komoroski B, Kasichayanula S, Discenza L, Washburn W, Meng W, Ellsworth BA, Whaley JM, Humphreys WG: In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans. Drug Metab Dispos. 2010 Mar;38(3):405-14. doi: 10.1124/dmd.109.029165. Epub 2009 Dec 8. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Vitamin d 24-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 58164.815 Da
References
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
- Forxiga Assessment report [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
- Gene Name
- CYP2A6
- Uniprot ID
- P11509
- Uniprot Name
- Cytochrome P450 2A6
- Molecular Weight
- 56501.005 Da
References
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGTs are of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isozyme is active on polyhydroxylated estrogens (such as...
- Gene Name
- UGT2B4
- Uniprot ID
- P06133
- Uniprot Name
- UDP-glucuronosyltransferase 2B4
- Molecular Weight
- 60512.035 Da
References
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
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
- Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. [Article]
Drug created at March 19, 2008 16:22 / Updated at June 06, 2023 09:54