Identification

Name
Dapagliflozin
Accession Number
DB06292
Description

Dapagliflozin is a sodium-glucose cotransporter 2 inhibitor indicated for managing diabetes mellitus type 21. When combined with diet and exercise in adults, dapagliflozin helps to improve glycemic control by inhibiting glucose resorption in the proximal tubule of the nephron and causing glycosuria1. Dapagliflozin was approved by the FDA on Jan 08, 20143.

Type
Small Molecule
Groups
Approved
Structure
Thumb
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 to improve glycemic control in adult patients with type 2 diabetes mellitus along with diet and exerciseLabel,1,2.

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

TargetActionsOrganism
ASodium/glucose cotransporter 2
antagonist
inhibitor
Humans
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

91%Label,1,2.

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

13.8h1.

Clearance

Oral plasma clearance was 4.9 mL/min/kg, and renal clearance was 5.6 mL/min1.

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

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
AbacavirDapagliflozin may increase the excretion rate of Abacavir which could result in a lower serum level and potentially a reduction in efficacy.
AbametapirThe serum concentration of Dapagliflozin can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Dapagliflozin can be increased when combined with Abatacept.
AbirateroneThe serum concentration of Dapagliflozin can be increased when it is combined with Abiraterone.
AcarboseDapagliflozin may increase the hypoglycemic activities of Acarbose.
AcebutololThe therapeutic efficacy of Dapagliflozin can be increased when used in combination with Acebutolol.
AceclofenacDapagliflozin may increase the excretion rate of Aceclofenac which could result in a lower serum level and potentially a reduction in efficacy.
AcemetacinThe therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Acemetacin.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Dapagliflozin.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Dapagliflozin.
Additional Data Available
  • Extended Description
    Extended Description

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

    Learn more
  • Severity
    Severity

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

    Learn more
  • Evidence Level
    Evidence Level

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

    Learn more
  • Action
    Action

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

    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

Product Ingredients
IngredientUNIICASInChI Key
Dapagliflozin propanediol monohydrate887K2391VH960404-48-2GOADIQFWSVMMRJ-UPGAGZFNSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
EdistrideTablet, film coated5 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
EdistrideTablet, film coated5 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
EdistrideTablet, film coated10 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
EdistrideTablet, film coated5 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
EdistrideTablet, film coated10 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
EdistrideTablet, film coated5 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
EdistrideTablet, film coated10 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
EdistrideTablet, film coated10 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
EdistrideTablet, film coated10 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
EdistrideTablet, film coated5 mgOralAstra Zeneca Ab2015-11-09Not applicableEU flag
Additional Data Available
  • Application Number
    Application Number

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

    Learn more
  • Product Code
    Product Code

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

    Learn more
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
QternDapagliflozin (5 mg) + Saxagliptin (5 mg)TabletOralAstra ZenecaNot applicableNot applicableCanada flag
QternDapagliflozin (5 mg/1) + Saxagliptin hydrochloride (5 mg/1)Tablet, film coatedOralAstraZeneca Pharmaceuticals LP2017-12-04Not applicableUS flag
QternDapagliflozin (10 mg) + Saxagliptin (5 mg)TabletOralAstra ZenecaNot applicableNot applicableCanada flag
QternDapagliflozin (10 mg/1) + Saxagliptin hydrochloride (5 mg/1)Tablet, film coatedOralAstraZeneca Pharmaceuticals LP2017-12-04Not applicableUS flag
Qternmet XRDapagliflozin (5 mg/1) + Metformin hydrochloride (1000 mg/1) + Saxagliptin hydrochloride (2.5 mg/1)Tablet, film coatedOralAstraZeneca Pharmaceuticals LP2020-06-01Not applicableUS flag
Qternmet XRDapagliflozin (10 mg/1) + Metformin hydrochloride (1000 mg/1) + Saxagliptin hydrochloride (5 mg/1)Tablet, film coatedOralAstraZeneca Pharmaceuticals LP2020-06-01Not applicableUS flag
Qternmet XRDapagliflozin (2.5 mg/1) + Metformin hydrochloride (1000 mg/1) + Saxagliptin hydrochloride (2.5 mg/1)Tablet, film coatedOralAstraZeneca Pharmaceuticals LP2020-06-01Not applicableUS flag
Qternmet XRDapagliflozin (5 mg/1) + Metformin hydrochloride (1000 mg/1) + Saxagliptin hydrochloride (5 mg/1)Tablet, film coatedOralAstraZeneca Pharmaceuticals LP2020-06-01Not applicableUS flag
XigduoDapagliflozin propanediol monohydrate (5 mg) + Metformin hydrochloride (850 mg)Tablet, film coatedOralAstra Zeneca Ab2014-01-16Not applicableEU flag
XigduoDapagliflozin (5 mg) + Metformin hydrochloride (850 mg)TabletOralAstra Zeneca2016-02-08Not applicableCanada flag

Categories

ATC Codes
A10BK01 — DapagliflozinA10BD15 — Metformin and dapagliflozinA10BD21 — Saxagliptin and dapagliflozinA10BD25 — Metformin, saxagliptin and dapagliflozin
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 / 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)

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)[[email protected]@H]2O[[email protected]](CO)[[email protected]@H](O)[[email protected]](O)[[email protected]]2O)C=C1

References

General References
  1. 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. [PubMed:19996149]
  2. 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. [PubMed:24105299]
  3. FDA Drug Approval Package: Dapagliflozin [Link]
KEGG Drug
D08897
PubChem Compound
9887712
PubChem Substance
175427068
ChemSpider
8063384
BindingDB
20880
RxNav
1488564
ChEBI
85078
ChEMBL
CHEMBL429910
ZINC
ZINC000003819138
Drugs.com
Drugs.com Drug Page
Wikipedia
Dapagliflozin
AHFS Codes
  • 68:20.18 — Sodium-glucose Cotransporter 2 (SGLT2) Inhibitors
FDA label
Download (1.22 MB)
MSDS
Download (62.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingOtherGlucose Metabolism Disorders / Renal Function Disorder1
4Active Not RecruitingTreatmentChronic Heart Failure With Reduced Ejection Fraction (HFrEF)1
4Active Not RecruitingTreatmentType 2 Diabetes Mellitus3
4CompletedBasic ScienceHigh Cholesterol / Type 2 Diabetes Mellitus1
4CompletedBasic ScienceSkeletal Muscle Insulin Sensitivity / Type 2 Diabetes Mellitus1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedPreventionNephropathy, Diabetic / Type 2 Diabetes Mellitus1
4CompletedTreatmentBlood Pressures / BMI >30 kg/m2 / Cardiac Hypertrophy / High Blood Pressure (Hypertension) / Microalbuminuria / Type 2 Diabetes Mellitus / Vascular Stiffness1
4CompletedTreatmentCardiovascular Heart Disease / Type2 Diabetes1
4CompletedTreatmentCarotid Artery Diseases / Coronary Artery Disease (CAD) / Type 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, coated10 mg
Tablet, coated5 mg
Tablet, film coatedOral10 mg
Tablet, film coatedOral5 mg
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral5 mg/1
TabletOral
Tablet, coatedOral10 MG
Tablet, coatedOral5 MG
Tablet
TabletOral1000 MG
TabletOral850 MG
TabletOral
Tablet, film coatedOral
Tablet, extended releaseOral10 mg
Tablet, film coated, extended releaseOral
Tablet, extended releaseOral1005.04 mg
Tablet, extended releaseOral5 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8216180No2012-07-102028-01-12US flag
US8439864No2013-05-142028-03-25US flag
US6667061Yes2003-12-232020-11-25US flag
US6495164No2002-12-172020-05-25US flag
US6872700No2005-03-292020-01-14US flag
US6956026No2005-10-182018-01-07US flag
US7741269No2010-06-222018-01-07US flag
US9238076No2016-01-192024-04-15US flag
US8906851No2014-12-092026-08-18US flag
US7612176No2009-11-032025-04-13US flag
US8431685No2013-04-302025-04-13US flag
US8461105No2013-06-112025-04-13US flag
US8329648No2012-12-112026-08-18US flag
US7456254No2008-11-252025-06-30US flag
US7563871No2009-07-212024-04-15US flag
US6824822No2004-11-302022-10-09US flag
US6479065No2002-11-122020-08-10US flag
US7223440No2007-05-292021-08-31US flag
USRE44186No2013-04-302023-07-31US flag
US8628799No2014-01-142025-07-13US flag
US8685934No2014-04-012030-05-26US flag
US8501698No2013-08-062027-06-20US flag
US6414126No2002-07-022020-10-04US flag
US6515117No2003-02-042020-10-04US flag
US6936590No2005-08-302020-10-04US flag
US9198925No2015-12-012020-10-04US flag
US7919598No2011-04-052029-12-16US flag
US8361972No2013-01-292028-03-21US flag
US8716251No2014-05-062028-03-21US flag
US7851502No2010-12-142028-08-19US flag
US8221786No2012-07-172028-03-21US flag
US9616028No2017-04-112030-11-12US flag
US9320853No2016-04-262028-03-25US flag
US8827963No2014-09-092029-02-04US flag
US8712615No2014-04-292030-01-18US flag
US8998876No2015-04-072030-01-07US flag
US8758292No2014-06-242027-11-12US flag
US8690837No2014-04-082029-05-19US flag
US8721615No2014-05-132030-01-18US 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
melting point (°C)65[MSDS]
boiling point (°C)609[MSDS]
logP2.7[MSDS]
Predicted Properties
PropertyValueSource
Water Solubility0.173 mg/mLALOGPS
logP2.52ALOGPS
logP2.11ChemAxon
logS-3.4ALOGPS
pKa (Strongest Acidic)12.57ChemAxon
pKa (Strongest Basic)-3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area99.38 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity104.93 m3·mol-1ChemAxon
Polarizability42.36 Å3ChemAxon
Number of Rings3ChemAxon
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
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. 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. [PubMed:19996149]

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
  1. 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. [PubMed:24105299]
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
  1. 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. [PubMed:24105299]
  2. 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
  1. 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. [PubMed:24105299]
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
  1. 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. [PubMed:24105299]
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
  1. 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. [PubMed:24105299]
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
  1. 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. [PubMed:24105299]
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
  1. 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. [PubMed:24105299]
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
  1. 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. [PubMed:24105299]
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
  1. 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. [PubMed:24105299]

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. 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. [PubMed:24105299]

Drug created on March 19, 2008 10:22 / Updated on October 23, 2020 21:53

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates