NAV

Canagliflozin

Identification

Summary

Canagliflozinis a sodium-glucose co-transporter 2 (SGLT2) inhibitor used to manage hyperglycemia in type 2 diabetes mellitus (DM). Also used to reduce the risk of major cardiovascular events in patients with established cardiovascular disease and type 2 DM.

Brand Names
Invokamet, Invokana
Generic Name
Canagliflozin
DrugBank Accession Number
DB08907
Background

Canagliflozin, also known asInvokana, is a sodium-glucose cotransporter 2 (SGLT2) inhibitor used in the management of type 2 diabetes mellitus along with lifestyle changes including diet and exerciseLabel.

It was initially approved by the FDA in 2013 for the management of diabetes and later approved in 2018 for a second indication of reducing the risk of cardiovascular events in patients diagnosed with type 2 diabetes mellitus8,Label.

Canagliflozin is the first oral antidiabetic drug approved for the prevention of cardiovascular events in patients with type 2 diabetes8. Cardiovascular disease is the most common cause of death in these patients4.

类型
Small Molecule
Groups
Approved
Structure
 3D
Similar Structures
Weight
Average: 444.516
Monoisotopic: 444.140672805
Chemical Formula
C24H25FO5S
Synonyms
  • Canagliflozin
  • Canagliflozin anhydrous
  • Canagliflozina

Pharmacology

Indication

This drug is used in conjunction with diet and exercise to increase glycemic control in adults diagnosed with type 2 diabetes mellitusLabel.

Another indication for canagliflozin is the prevention of major cardiovascular events (myocardial infarction, stroke, or death due to a cardiovascular cause) in patients with type 2 diabetes, as well as hospitalization for heart failure in patients with type 2 diabetes8,10.

除了上述之外,canagliflozin可以使用d to lower the risk of end-stage kidney disease and major increases in serum creatinine and cardiovascular death for patients with a combination of type 2 diabetes mellitus, diabetic nephropathy, and albuminuria.10

It is important to note that this drug isnotindicated for the treatment of type 1 diabetes mellitus or diabetic ketoacidosisLabel.

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

This drug increases urinary glucose excretion and decreases the renal threshold for glucose (RTG) in a dose-dependent mannerLabel. The renal threshold is defined as the lowest level of blood glucose associated with the appearance of detectable glucose in the urine2,7. The end result of canagliflozin administration is increased urinary excretion of glucose and less renal absorption of glucose, decreasing glucose concentration in the blood and improving glycemic control.

A note on type 2 diabetes and cardiovascular disease

The risk of cardiovascular events in diabetes type 2 is increased due to the damaging effects of diabetes on blood vessels and nerves in the cardiovascular system. In particular, there is a tendency for hyperglycemia to create pro-atherogenic (plaque forming) lesions in blood vessels, leading to various fatal and non-fatal events including stroke and myocardial infarction5,9. Long-term glycemic control has been proven to be effective in the prevention of cardiovascular events such as myocardial infarction and stroke in patients with type 2 diabetes6.

Mechanism of action

The sodium-glucose co-transporter2 (SGLT2), is found in the proximal tubules of the kidney, and reabsorbs filtered glucose from the renal tubular lumen. Canagliflozin inhibits the SGLT2 co-transporter. This inhibition leads to lower reabsorption of filtered glucose into the body and decreases the renal threshold for glucose (RTG), leading to increased glucose excretion in the urineLabel.

Target Actions Organism
ASodium/glucose cotransporter 2
inhibitor
 Humans
Absorption

Bioavailability and steady-state

The absolute oral bioavailability of canagliflozin, on average, is approximately 65%Label. Steady-state concentrations are achieved after 4 to 5 days of daily dose administration between the range of 100mg to 300mgLabel.

Effect of food on absorption

Co-administration of a high-fat meal with canagliflozin exerted no appreciable effect on the pharmacokinetic parameters of canagliflozin. This drug may be administered without regard to food. Despite this, because of the potential of canagliflozin to decrease postprandial plasma glucose excretion due to prolonged intestinal glucose absorption, it is advisable to take this drug before the first meal of the dayLabel.

Volume of distribution

This drug is extensively distributed throughout the body. On average, the volume of distribution of canagliflozin at steady state following a single intravenous dose in healthy patients was measured to be 83.5 LLabel.

Protein binding

Canagliflozin is mainly bound to albumin. The plasma protein binding of this drug is 99%Label.

Metabolism

Canagliflozin is primarily metabolized by O-glucuronidation. It is mainly glucuronidated by UGT1A9 and UGT2B4 enzymes to two inactive O-glucuronide metabolitesLabel.

The oxidative metabolism of canagliflozin by hepatic cytochrome enzyme CYP3A4 is negligible (about 7%) in humansLabel.

Hover over products below to view reaction partners

Route of elimination

After a single oral radiolabeled dose canagliflozin dose to healthy subjects, the following ratios of canagliflozin or metabolites were measured in the feces and urineLabel:

Feces

41.5% as the unchanged radiolabeled drug

7.0% as a hydroxylated metabolite

3.2% as an O-glucuronide metabolite

Urine

About 33% of the ingested radiolabled dose was measured in the urine, generally in the form of O-glucuronide metabolites. Less than 1% of the dose was found excreted as unchanged drug in urine.

Half-life

In a clinical study, the terminal half-life of canagliflozin was 10.6 hours for the 100mg dose and 13.1 hours for the 300 mg doseLabel.

Clearance

In healthy subjects, canagliflozin clearance was approximately 192 mL/min after intravenous (IV) administrationLabel.

The renal clearance of 100 mg and 300 mg doses of canagliflozin was measured to be in the range of 1.30 - 1.55 mL/minLabel.

Adverse Effects
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Toxicity

Overdose information

If an overdose occurs, contact the Poison Control Center. Normal supportive measures should be taken, including the removal unabsorbed drug from the gastrointestinal tract, initiating clinical monitoring of the patient, and providing supportive treatment as deemed necessary. Canagliflozin has been removed in very small quantities after a 4-hour hemodialysis session. This drug is likely not dialyzable by peritoneal dialysisLabel.

Pregnancy and lactation

Animal data has demonstrated that canagliflozin may cause adverse renal effects in a growing fetus. Data are insufficient at this time in determining a potential canagliflozin related risk for major birth defects or possible miscarriage in humansLabel. There are known risks, however, of uncontrolled diabetes in pregnancyLabel. Inform female patients taking canagliflozin of the potential risk, which is increased during the second and third trimesters. This drug is not recommended during nursingLabel.

Mutagenesis and carcinogenicity

Canagliflozin was not found to be mutagenic in both metabolically activated and inactivated states in the Ames assay. Canagliflozin showed mutagenicity in laboratory mouse lymphoma assay, but only in the activated state. Canagliflozin was not found to be mutagenic in severalin vivoassays performed on ratsLabel.

The carcinogenic risk of canagliflozin was assessed in 2-year studies completed in both CD1 mice and Sprague-Dawley rats. Canagliflozin was not shown to increase tumor incidence in mouse models given doses less than or equal to 14 times the exposure from a typical 300 mg dose in humans. Despite these negative findings in mice, the incidence of several tumors increased in mice, including Leydig cell tumors, renal tubular adenomas, and adrenal pheochromocytomasLabel.

Pathways
Not Available
Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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
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interactions in your software
Abacavir Abacavir may decrease the excretion rate of Canagliflozin which could result in a higher serum level.
Abaloparatide The risk or severity of adverse effects can be increased when Abaloparatide is combined with Canagliflozin.
Abametapir The serum concentration of Canagliflozin can be increased when it is combined with Abametapir.
Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Canagliflozin.
Abrocitinib The serum concentration of Canagliflozin can be increased when it is combined with Abrocitinib.
Acarbose Canagliflozin may increase the hypoglycemic activities of Acarbose.
Acebutolol The therapeutic efficacy of Canagliflozin can be increased when used in combination with Acebutolol.
Aceclofenac The risk or severity of hyperkalemia can be increased when Aceclofenac is combined with Canagliflozin.
Acemetacin The risk or severity of hyperkalemia can be increased when Canagliflozin is combined with Acemetacin.
Acetaminophen Acetaminophen may decrease the excretion rate of Canagliflozin which could result in a higher serum level.
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Food Interactions
  • Avoid alcohol. Excess alcohol intake may promote ketoacidosis.
  • Drink plenty of fluids.
  • Take before a meal. It is recommended to take this drug before the first meal of the day.

Products

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Product Ingredients
Ingredient UNII CAS InChI Key
Canagliflozin hydrate 0SAC974Z85 928672-86-0 VHOFTEAWFCUTOS-TUGBYPPCSA-N
Product Images
Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Invokana Tablet, film coated 100 mg/1 Oral A-S Medication Solutions 2013-03-29 Not applicable US flag
Invokana Tablet, film coated 300 mg Oral Janssen Cilag International Nv 2020-12-16 Not applicable EU flag
Invokana Tablet, film coated 100 mg Oral Janssen Cilag International Nv 2020-12-16 Not applicable EU flag
Invokana Tablet, film coated 300 mg/1 Oral A-S Medication Solutions 2013-03-29 Not applicable US flag
Invokana Tablet 100 mg Oral Janssen Pharmaceuticals 2014-06-03 Not applicable Canada flag
Invokana Tablet, film coated 300 mg Oral Janssen Cilag International Nv 2020-12-16 Not applicable EU flag
Invokana Tablet, film coated 100 mg/1 Oral Cardinal Health 107, LLC 2013-03-29 Not applicable US flag
Invokana Tablet, film coated 100 mg Oral Janssen Cilag International Nv 2020-12-16 Not applicable EU flag
Invokana Tablet, film coated 300 mg/1 Oral Janssen Pharmaceuticals, Inc. 2013-03-29 Not applicable US flag
Invokana Tablet, film coated 100 mg Oral Janssen Cilag International Nv 2020-12-16 Not applicable EU flag
Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
Invokamet Canagliflozin hydrate(150 mg/1)+Metformin hydrochloride(1000 mg/1) Tablet, film coated Oral Janssen Pharmaceuticals, Inc. 2014-08-08 Not applicable US flag
Invokamet Canagliflozin hydrate(50 mg/1)+Metformin hydrochloride(500 mg/1) Tablet, film coated Oral Janssen Pharmaceuticals, Inc. 2014-08-08 Not applicable US flag
Invokamet Canagliflozin(50 mg)+Metformin hydrochloride(850 mg) Tablet Oral Janssen Pharmaceuticals 2016-06-28 2022-09-06 Canada flag
Invokamet Canagliflozin(50 mg)+Metformin hydrochloride(1000 mg) Tablet Oral Janssen Pharmaceuticals 2016-06-28 Not applicable Canada flag
Invokamet Canagliflozin hydrate(150 mg/1)+Metformin hydrochloride(500 mg/1) Tablet, film coated Oral Janssen Pharmaceuticals, Inc. 2014-08-08 Not applicable US flag
Invokamet Canagliflozin hydrate(150 mg/1)+Metformin hydrochloride(1 g/1) Tablet, film coated Oral bryant ranch prepack 2014-08-08 Not applicable US flag
Invokamet Canagliflozin(150 mg)+Metformin hydrochloride(1000 mg) Tablet Oral Janssen Pharmaceuticals 2016-06-28 Not applicable Canada flag
Invokamet Canagliflozin(50 mg)+Metformin hydrochloride(500 mg) Tablet Oral Janssen Pharmaceuticals 2016-06-28 Not applicable Canada flag
Invokamet Canagliflozin hydrate(50 mg/1)+Metformin hydrochloride(1000 mg/1) Tablet, film coated Oral Janssen Pharmaceuticals, Inc. 2014-08-08 Not applicable US flag
Invokamet Canagliflozin(150 mg)+Metformin hydrochloride(850 mg) Tablet Oral Janssen Pharmaceuticals 2016-06-28 2022-09-06 Canada flag

Categories

ATC Codes
A10BD16 — Metformin and canagliflozin A10BK02 — Canagliflozin
Drug Categories
Chemical TaxonomyProvided byClassyfire
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
Hexoses/C-glycosyl compounds/Toluenes/Fluorobenzenes/2,5-disubstituted thiophenes/Oxanes/Aryl fluorides/Heteroaromatic compounds/Secondary alcohols/Polyols
show 5 more
Substituents
2,5-disubstituted thiophene/Alcohol/Aromatic heteromonocyclic compound/Aryl fluoride/Aryl halide/Benzenoid/C-glycosyl compound/Dialkyl ether/Ether/Fluorobenzene
show 17 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
organofluorine compound, thiophenes, ring assembly, C-glycosyl compound (CHEBI:73274)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
6S49DGR869
CAS number
842133-18-0
InChI Key
XTNGUQKDFGDXSJ-ZXGKGEBGSA-N
InChI
InChI=1S/C24H25FO5S/c1-13-2-3-15(24-23(29)22(28)21(27)19(12-26)30-24)10-16(13)11-18-8-9-20(31-18)14-4-6-17(25)7-5-14/h2-10,19,21-24,26-29H,11-12H2,1H3/t19-,21-,22+,23-,24+/m1/s1
IUPAC Name
(2S,3R,4R,5S,6R)-2-(3-{[5-(4-fluorophenyl)thiophen-2-yl]methyl}-4-methylphenyl)-6-(hydroxymethyl)oxane-3,4,5-triol
SMILES
[H][C@]1(O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C1=CC=C(C)C(CC2=CC=C(S2)C2=CC=C(F)C=C2)=C1

References

一般引用
  1. Lamos EM, Younk LM, Davis SN: Canagliflozin , an inhibitor of sodium-glucose cotransporter 2, for the treatment of type 2 diabetes mellitus. Expert Opin Drug Metab Toxicol. 2013 Jun;9(6):763-75. doi: 10.1517/17425255.2013.791282. Epub 2013 Apr 17. [Article]
  2. Osaki A, Okada S, Saito T, Yamada E, Ono K, Niijima Y, Hoshi H, Yamada M: Renal threshold for glucose reabsorption predicts diabetes improvement by sodium-glucose cotransporter 2 inhibitor therapy. J Diabetes Investig. 2016 Sep;7(5):751-4. doi: 10.1111/jdi.12473. Epub 2016 Feb 16. [Article]
  3. Deeks ED, Scheen AJ: Canagliflozin: A Review in Type 2 Diabetes. Drugs. 2017 Sep;77(14):1577-1592. doi: 10.1007/s40265-017-0801-6. [Article]
  4. Joseph JJ, Golden SH: Type 2 diabetes and cardiovascular disease: what next? Curr Opin Endocrinol Diabetes Obes. 2014 Apr;21(2):109-20. doi: 10.1097/MED.0000000000000044. [Article]
  5. Gleissner CA, Galkina E, Nadler JL, Ley K: Mechanisms by which diabetes increases cardiovascular disease. Drug Discov Today Dis Mech. 2007;4(3):131-140. doi: 10.1016/j.ddmec.2007.12.005. [Article]
  6. Mannucci E, Dicembrini I, Lauria A, Pozzilli P: Is glucose control important for prevention of cardiovascular disease in diabetes? Diabetes Care. 2013 Aug;36 Suppl 2:S259-63. doi: 10.2337/dcS13-2018. [Article]
  7. Steven L. Cowart and Max E. Stachura (1990). Clinical Methods: The History, Physical, and Laboratory Examinations. 3rd edition. (3rd ed.). Butterworths.
  8. U.S. FDA Approves INVOKANA® (canagliflozin) to Reduce the Risk of Heart Attack, Stroke or Cardiovascular Death in Adults with Type 2 Diabetes and Established Cardiovascular Disease [Link]
  9. Diabetes, Heart Disease, and Stroke: NIDDK [Link]
  10. FDA Approved Drug Products: Invokana (canagliflozin) oral tablets [Link]
  11. FDA Approved Products: INVOKAMET (canagliflozin and metformin hydrochloride tablets), for oral use [Link]
  12. Invokana, Canadian monograph [File]
KEGG Drug
D09592
PubChem Compound
24812758
PubChem Substance
175427146
ChemSpider
26333259
BindingDB
50386885
RxNav
1373458
ChEBI
73274
ChEMBL
CHEMBL2048484
ZINC
ZINC000043207238
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Canagliflozin
FDA label
Download (687 KB)
MSDS
Download (24.7 KB)

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
4 Active Not Recruiting Treatment Coronavirus Disease 2019 (COVID‑19) 1
4 Active Not Recruiting Treatment 类型2 Diabetes Mellitus 1
4 Completed Treatment Albuminuria/类型2 Diabetes Mellitus 1
4 Completed Treatment BMI >27 kg/m2/Obesity/类型2 Diabetes Mellitus 1
4 Completed Treatment Diabetes Mellitus 1
4 Completed Treatment Hearth Failure With Reduced Ejection Fraction (HFrEF)/类型2 Diabetes Mellitus 1
4 Completed Treatment Hypertension/类型2 Diabetes Mellitus 1
4 Completed Treatment Polycystic Ovarian Syndrome (PCOS) 1
4 Completed Treatment 类型2 Diabetes Mellitus 8
4 Completed Treatment 类型II Diabetes in Subjects BMI 27 to 32 1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Form Route Strength
Tablet Oral
Tablet, film coated Oral
Tablet, extended release Oral
Tablet, film coated, extended release Oral
Tablet Oral 100 mg
Tablet Oral 300 mg
Tablet, film coated Oral 100 mg/1
Tablet, film coated Oral 300 mg/1
Tablet, film coated Oral
Tablet, film coated Oral 100 mg
Tablet, film coated Oral 300 mg
Tablet, coated Oral
Tablet, film coated Oral 150.00 mg
Tablet, film coated Oral 50.00 mg
Tablet, coated Oral 100 mg
Tablet, coated Oral 300 mg
Prices
Not Available
Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region
US6723340 No 2004-04-20 2021-10-25 US flag
US8222219 No 2012-07-17 2024-07-30 US flag
US8513202 No 2013-08-20 2027-12-03 US flag
US7943582 No 2011-05-17 2029-02-26 US flag
US8785403 No 2014-07-22 2024-07-30 US flag
US7943788 No 2011-05-17 2027-07-14 US flag
US10617668 No 2020-04-14 2031-05-11 US flag

Properties

State
Solid
Experimental Properties
Property Value Source
melting point (°C) 68-72 https://www.trc-canada.com/product-detail/?CatNum=C175190
boiling point (°C) ‎642.9±55.0 http://www.chemspider.com/Chemical-Structure.26333259.html
water solubility almost insoluble https://www.ema.europa.eu/en/documents/assessment-report/invokana-epar-public-assessment-report_en.pdf
logP 3.44 https://www.tga.gov.au/file/824/download
pKa 13.34 https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL2103841/
Predicted Properties
Property Value Source
Water Solubility 0.0045 mg/mL ALOGPS
logP 3.09 ALOGPS
logP 3.52 Chemaxon
logS -5 ALOGPS
pKa (Strongest Acidic) 12.57 Chemaxon
pKa (Strongest Basic) -3 Chemaxon
Physiological Charge 0 Chemaxon
Hydrogen Acceptor Count 5 Chemaxon
Hydrogen Donor Count 4 Chemaxon
Polar Surface Area 90.15 Å2 Chemaxon
Rotatable Bond Count 5 Chemaxon
Refractivity 116.14 m3·mol-1 Chemaxon
Polarizability 46.64 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规则 No Chemaxon
Predicted ADMET Features
Property Value Probability
Human Intestinal Absorption + 0.9541
Blood Brain Barrier + 0.7708
Caco-2 permeable - 0.6554
P-glycoprotein substrate Substrate 0.6058
P-glycoprotein inhibitor I Non-inhibitor 0.8414
P-glycoprotein inhibitor II Non-inhibitor 0.9447
Renal organic cation transporter Non-inhibitor 0.8544
CYP450 2C9 substrate Non-substrate 0.6853
CYP450 2D6 substrate Non-substrate 0.8293
CYP450 3A4 substrate Non-substrate 0.5929
CYP450 1A2 substrate Non-inhibitor 0.6579
CYP450 2C9 inhibitor Non-inhibitor 0.6178
CYP450 2D6 inhibitor Non-inhibitor 0.8683
CYP450 2C19 inhibitor Non-inhibitor 0.5958
CYP450 3A4 inhibitor Non-inhibitor 0.7086
CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7691
Ames test Non AMES toxic 0.584
Carcinogenicity Non-carcinogens 0.9103
Biodegradation Not ready biodegradable 0.9936
Rat acute toxicity 2.5975 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9912
hERG inhibition (predictor II) Non-inhibitor 0.7246
ADMET data is predicted usingadmetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Spectrum Spectrum Type Splash Key
预测MS / MS谱- 10 v,正面(注释d) 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

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insights and accelerate drug research.
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Details 1.Sodium/glucose cotransporter 2
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
分子量
72895.995 Da
References
  1. Lamos EM, Younk LM, Davis SN: Canagliflozin , an inhibitor of sodium-glucose cotransporter 2, for the treatment of type 2 diabetes mellitus. Expert Opin Drug Metab Toxicol. 2013 Jun;9(6):763-75. doi: 10.1517/17425255.2013.791282. Epub 2013 Apr 17. [Article]
  2. FDA label, Invokana [File]
  3. Invokana, Canadian monograph [File]

Enzymes

Details 1.UDP-glucuronosyltransferase 1-9
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
分子量
59940.495 Da
References
  1. Sarnoski-Brocavich S, Hilas O: Canagliflozin (invokana), a novel oral agent for type-2 diabetes. P T. 2013 Nov;38(11):656-66. [Article]
  2. Devineni D, Vaccaro N, Murphy J, Curtin C, Mamidi RN, Weiner S, Wang SS, Ariyawansa J, Stieltjes H, Wajs E, Di Prospero NA, Rothenberg P: Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants. Int J Clin Pharmacol Ther. 2015 Feb;53(2):115-28. doi: 10.5414/CP202158. [Article]
  3. FDA label, Invokana [File]
  4. Invokana, Canadian monograph [File]
Details 2.UDP-glucuronosyltransferase 2B4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
结合UDPGTs是十分重要的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
分子量
60512.035 Da
References
  1. Sarnoski-Brocavich S, Hilas O: Canagliflozin (invokana), a novel oral agent for type-2 diabetes. P T. 2013 Nov;38(11):656-66. [Article]
  2. Devineni D, Vaccaro N, Murphy J, Curtin C, Mamidi RN, Weiner S, Wang SS, Ariyawansa J, Stieltjes H, Wajs E, Di Prospero NA, Rothenberg P: Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants. Int J Clin Pharmacol Ther. 2015 Feb;53(2):115-28. doi: 10.5414/CP202158. [Article]
  3. FDA label, Invokana [File]
  4. Invokana, Canadian monograph [File]
Details 3.Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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
分子量
57342.67 Da
References
  1. 莫斯利摩根富林明2日,史密斯L,埃弗顿E,有梭底Fellner C:迦叠um-Glucose Linked Transporter 2 (SGLT2) Inhibitors in the Management Of Type-2 Diabetes: A Drug Class Overview. P T. 2015 Jul;40(7):451-62. [Article]
  2. FDA label, Invokana [File]

Carriers

Details 1.Alpha-1-acid glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
分子量
23511.38 Da
References
  1. Lamos EM, Younk LM, Davis SN: Canagliflozin , an inhibitor of sodium-glucose cotransporter 2, for the treatment of type 2 diabetes mellitus. Expert Opin Drug Metab Toxicol. 2013 Jun;9(6):763-75. doi: 10.1517/17425255.2013.791282. Epub 2013 Apr 17. [Article]

Transporters

Details 1.P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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
分子量
141477.255 Da
References
  1. Mamidi RNVS, Dallas S, Sensenhauser C, Lim HK, Scheers E, Verboven P, Cuyckens F, Leclercq L, Evans DC, Kelley MF, Johnson MD, Snoeys J: In vitro and physiologically-based pharmacokinetic based assessment of drug-drug interaction potential of canagliflozin. Br J Clin Pharmacol. 2017 May;83(5):1082-1096. doi: 10.1111/bcp.13186. Epub 2016 Dec 20. [Article]
  2. Devineni D, Vaccaro N, Murphy J, Curtin C, Mamidi RN, Weiner S, Wang SS, Ariyawansa J, Stieltjes H, Wajs E, Di Prospero NA, Rothenberg P: Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants. Int J Clin Pharmacol Ther. 2015 Feb;53(2):115-28. doi: 10.5414/CP202158. [Article]
  3. FDA label, Invokana [File]
  4. Invokana, Canadian monograph [File]
Details 2.Canalicular multispecific organic anion transporter 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
分子量
174205.64 Da
References
  1. Invokana, Canadian monograph [File]
Details 3.ATP-binding cassette sub-family G member 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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
分子量
72313.47 Da
References
  1. Invokana, Canadian monograph [File]

Drug created at June 17, 2013 06:21 / Updated at April 26, 2023 07:53