menu
    • menu

    Find Canagliflozin manufacturers, exporters & distributors on PharmaCompass

    Granules India Limited has high volume world-class facilities for APIs, PFIs, & FDFs, serving customers in over 80 countries.

    Virtual Booth

    Contact Supplier

    Jai Radhe Sales is your partner for all your sourcing needs.

    Virtual Booth

    Contact Supplier

    xyz-pharma-m-2024-10-07

    Virtual Booth

    Contact Supplier

    Egis is a Hungarian generic pharma company with 110 years history. Our activities incorporate all areas of the pharma value chain.

    Virtual Booth

    Contact Supplier

    Biophore is a research-driven global pharmaceutical company focused on niche APIs for the generic industry.

    Virtual Booth

    Contact Supplier

    xyz-pharma-m-2024-10-07

    Virtual Booth

    Contact Supplier

    ACTIVE PHARMA INGREDIENTS

    DEVELOPMENTS

    INTERMEDIATES

    FINISHED DOSAGE FORMULATIONS

    DRUG PRODUCT COMPOSITIONS

    RELATED EXCIPIENT COMPANIES

    EXCIPIENTS BY APPLICATIONS

    DIGITAL CONTENT

    GLOBAL SALES INFORMATION

    MARKET PLACE

    PATENTS & EXCLUSIVITIES

    REF. STANDARDS & IMPURITIES

    PharmaCompass

    Synopsis

    Product SearchProduct Search

    Synopsis

    ACTIVE PHARMA INGREDIENTS

    60

    API Suppliers

    API Suppliers

    27

    USDMF

    US DMFs Filed

    0

    CEP/COS

    CEP/COS Certifications

    0

    JDMF

    JDMFs Filed

    7

    EU WC

    EU WC

    0

    KDMF

    KDMF

    14

    NDC API

    NDC API

    0

    VMF

    NDC API

    41

    Listed Suppliers

    Other Suppliers

    API REF. PRICE (USD/KG)

    $
    $ 2,753

    MARKET PLACE

    18

    API

    2

    FDF

    39INTERMEDIATES

    FINISHED DOSAGE FORMULATIONS

    54

    FDF Dossiers

    FDF Dossiers

    15

    FDA Orange Book

    FDA (Orange Book)

    20

    Europe

    Europe

    6

    Canada

    Canada

    0

    Australia

    Australia

    0

    South Africa

    South Africa

    13

    Listed Dossiers

    Listed Dossiers

    8DRUGS IN DEVELOPMENT

    FDF DossiersDRUG PRODUCT COMPOSITIONS

    REF. STANDARDS OR IMPURITIES

    0

    EDQM

    0

    USP

    0

    JP

    13

    Others

    PATENTS & EXCLUSIVITIES

    130

    US Patents

    0

    US Exclusivities

    4

    Health Canada Patents

    DIGITAL CONTENT

    11

    Data Compilation #PharmaFlow

    0

    Stock Recap #PipelineProspector

    0

    Weekly News Recap #Phispers

    139

    News #PharmaBuzz

    GLOBAL SALES INFORMATION

    US Medicaid

    454,855,715

    Annual Reports

    11,156

    Finished Drug Prices

    Listed Dossiers

    153 RELATED EXCIPIENT COMPANIES

    245EXCIPIENTS BY APPLICATIONS

    Chemistry

    Click the arrow to open the dropdown
    read-moreClick the button for full data set
    read-moreClick the button for full data set
    Also known as: 842133-18-0, Canagliflozin anhydrous, Ta-7284, Jnj-28431754, Jnj 24831754zae, Canagliflozin hemihydrate
    Molecular Formula
    C24H25FO5S
    Molecular Weight
    444.5  g/mol
    InChI Key
    XTNGUQKDFGDXSJ-ZXGKGEBGSA-N
    FDA UNII
    6S49DGR869
    Canagliflozin
    A glucoside-derived SODIUM-GLUCOSE TRANSPORTER 2 inhibitor that stimulates urinary excretion of glucose by suppressing renal glucose reabsorption. It is used to manage BLOOD GLUCOSE levels in patients with TYPE 2 DIABETES.
    Canagliflozin anhydrous is a Sodium-Glucose Cotransporter 2 Inhibitor. The mechanism of action of canagliflozin anhydrous is as a Sodium-Glucose Transporter 2 Inhibitor, and P-Glycoprotein Inhibitor.
    1 2D Structure

    Canagliflozin

    2 Identification
    2.1 Computed Descriptors
    2.1.1 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
    2.1.2 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
    2.1.3 InChI Key
    XTNGUQKDFGDXSJ-ZXGKGEBGSA-N
    2.1.4 Canonical SMILES
    CC1=C(C=C(C=C1)C2C(C(C(C(O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F
    2.1.5 Isomeric SMILES
    CC1=C(C=C(C=C1)[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F
    2.2 Other Identifiers
    2.2.1 UNII
    6S49DGR869
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. 1-(glucopyranosyl)-4-methyl-3-(5-(4-fluorophenyl)-2-thienylmethyl)benzene - T777973

    2. Canagliflozin Hemihydrate

    3. Canagliflozin, Anhydrous

    4. Invokana

    2.3.2 Depositor-Supplied Synonyms

    1. 842133-18-0

    2. Canagliflozin Anhydrous

    3. Ta-7284

    4. Jnj-28431754

    5. Jnj 24831754zae

    6. Canagliflozin Hemihydrate

    7. Canagliflozin [inn]

    8. Canagliflozin Hydrate

    9. (2s,3r,4r,5s,6r)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)tetrahydro-2h-pyran-3,4,5-triol

    10. Ta 7284

    11. 1-(glucopyranosyl)-4-methyl-3-(5-(4-fluorophenyl)-2-thienylmethyl)benzene

    12. Jnj 28431754

    13. Chebi:73274

    14. 6s49dgr869

    15. (2s,3r,4r,5s,6r)-2-[3-[[5-(4-fluorophenyl)thiophen-2-yl]methyl]-4-methylphenyl]-6-(hydroxymethyl)oxane-3,4,5-triol

    16. (1s)-1,5-anhydro-1-(3-((5-(4-fluorophenyl)-2-thienyl)methyl)-4-methylphenyl)-d-glucitol

    17. (1s)-1,5-anhydro-1-(3-{[5-(4-fluorophenyl)-2-thienyl]methyl}-4-methylphenyl)-d-glucitol

    18. (1s)-1,5-anhydro-1-c-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-d-glucitol

    19. D-glucitol,1,5-anhydro-1-c-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-, (1s)-

    20. (1s)-1,5-anhydro-1-c-(3-((5-(4-fluorophenyl)-2-thienyl)methyl)-4-methylphenyl)-d-glucitol

    21. Unii-6s49dgr869

    22. Jnj 24831754aaa

    23. (2s,3r,4r,5s,6r)-2-(3-{[5-(4-fluorophenyl)thiophen-2-yl]methyl}-4-methylphenyl)-6-(hydroxymethyl)oxane-3,4,5-triol

    24. Jnj 24831754

    25. Canagliflozin [mi]

    26. Mls006011126

    27. Schembl157162

    28. Canagliflozin [who-dd]

    29. Gtpl4582

    30. Chembl2048484

    31. Hsdb 8284

    32. Amy3291

    33. Bcpp000303

    34. Dtxsid601004469

    35. Jnj 28431754aaa

    36. Bdbm50386885

    37. Mfcd18251436

    38. S2760

    39. Zinc43207238

    40. Akos025401827

    41. Bcp9000477

    42. Ccg-229581

    43. Cs-0522

    44. Db08907

    45. Ks-1443

    46. Ncgc00346691-02

    47. (1s)-1,5-anhydro-1-c-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-d-glucitol

    48. Ac-26303

    49. Hy-10451

    50. Smr004702906

    51. Sw219119-1

    52. A25050

    53. J-500391

    54. Q5030940

    55. (1s)-1,5-anhydro-1-(3-{[5-(4-fluorophenyl)-2-thienyl]methyl}-4-methyl-phenyl)-d-glucitol

    56. (1s)-1,5-anhydro-1-c-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-d- Glucitol

    57. D-glucitol, 1,5-anhydro-1-c-(3-((5-(4-fluorophenyl)-2-thienyl)methyl)-4- Methylphenyl)-, (1s)-

    58. D-glucitol, 1,5-anhydro-1-c-(3-((5-(4-fluorophenyl)-2-thienyl)methyl)-4- Methylphenyl)-, (1s)-

    59. D-glucitol, 1,5-anhydro-1-c-(3-((5-(4-fluorophenyl)-2-thienyl)methyl)-4-methylphenyl)-

    60. Jnj24831754zae; Ta 7284;(2s,3r,4r,5s,6r)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)-tetrahydro-2h-pyran-3,4,5-triol

    2.4 Create Date
    2008-06-23
    3 Chemical and Physical Properties
    Molecular Weight 444.5 g/mol
    Molecular Formula C24H25FO5S
    XLogP33.2
    Hydrogen Bond Donor Count4
    Hydrogen Bond Acceptor Count7
    Rotatable Bond Count5
    Exact Mass444.14067323 g/mol
    Monoisotopic Mass444.14067323 g/mol
    Topological Polar Surface Area118 Ų
    Heavy Atom Count31
    Formal Charge0
    Complexity574
    Isotope Atom Count0
    Defined Atom Stereocenter Count5
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 2  
    Drug NameInvokana
    PubMed HealthCanagliflozin (By mouth)
    Drug ClassesEndocrine-Metabolic Agent, Hypoglycemic
    Drug LabelINVOKANA (canagliflozin) contains canagliflozin, an inhibitor of sodium-glucose co-transporter 2 (SGLT2), the transporter responsible for reabsorbing the majority of glucose filtered by the kidney. Canagliflozin, the active ingredient of INVOKANA, is...
    Active IngredientCanagliflozin
    Dosage FormTablet
    RouteOral
    Strength300mg; 100mg
    Market StatusPrescription
    CompanyJanssen Pharms

    2 of 2  
    Drug NameInvokana
    PubMed HealthCanagliflozin (By mouth)
    Drug ClassesEndocrine-Metabolic Agent, Hypoglycemic
    Drug LabelINVOKANA (canagliflozin) contains canagliflozin, an inhibitor of sodium-glucose co-transporter 2 (SGLT2), the transporter responsible for reabsorbing the majority of glucose filtered by the kidney. Canagliflozin, the active ingredient of INVOKANA, is...
    Active IngredientCanagliflozin
    Dosage FormTablet
    RouteOral
    Strength300mg; 100mg
    Market StatusPrescription
    CompanyJanssen Pharms

    4.2 Therapeutic Uses

    /CLINICAL TRIALS/ ClinicalTrials.gov is a registry and results database of publicly and privately supported clinical studies of human participants conducted around the world. The Web site is maintained by the National Library of Medicine (NLM) and the National Institutes of Health (NIH). Each ClinicalTrials.gov record presents summary information about a study protocol and includes the following: Disease or condition; Intervention (for example, the medical product, behavior, or procedure being studied); Title, description, and design of the study; Requirements for participation (eligibility criteria); Locations where the study is being conducted; Contact information for the study locations; and Links to relevant information on other health Web sites, such as NLM's MedlinePlus for patient health information and PubMed for citations and abstracts for scholarly articles in the field of medicine. Canagliflozin is included in the database.

    NIH/NLM; ClinicalTrials.Gov. Available from, as of September 30, 2015: https://clinicaltrials.gov/search/intervention=Canagliflozin

    Invokana (canagliflozin) is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. /Included in US product label/

    NIH; DailyMed. Current Medication Information for Invokana (Canagliflozin) Tablet, Film Coated (Updated: September 2015). Available from, as of November 20, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b9057d3b-b104-4f09-8a61-c61ef9d4a3f3

    EXPL THER The proximal tubule's sodium-glucose linked transporter-2 (SGLT2) accounts for the vast majority of glucose reabsorption by the kidney. Its selective inhibition, accordingly, leads to substantial glycosuria, lowering blood glucose, and facilitating weight loss in individuals with diabetes. During the past year, two SGLT2 inhibitors, canagliflozin and dapagliflozin, have been approved for the treatment of type 2 diabetes. Beyond their anti-hyperglycemic properties, however, this new class of drugs has several other attributes that provide a theoretical basis for kidney protection. Like agents that block the renin-angiotensin system, SGLT2 inhibitors also reduce single-nephron glomerular filtration rate (SNGFR) in the chronically diseased kidney, though by quite different mechanisms. Additional potentially beneficial effects of SGLT2 inhibition include modest reductions in blood pressure and plasma uric acid. Finally, cell culture studies indicate that glucose uptake from the tubular lumen, as well as from the basolateral compartment, can contribute to proximal tubular production of extracellular matrix proteins. Whether such attributes will translate into reducing the progression of chronic kidney disease will require the undertaking of long-term, dedicated studies.

    PMID:24257692 Gilbert RE; Kidney Int 86(4): 693-700 (2014).

    EXPL THER Management of hypertension in diabetes is critical for reduction of cardiovascular mortality and morbidity. While blood pressure (BP) control has improved over the past two decades, the control rate is still well below 50% in the general population of patients with type 2 diabetes mellitus (T2DM). A new class of oral glucose-lowering agents has recently been approved; the sodium-glucose co-transporter 2 (SGLT2) inhibitors, which act by eliminating large amounts of glucose in the urine. Two agents, dapagliflozin and canagliflozin, are currently approved in the United States and Europe, and empagliflozin and ipragliflozin have reported Phase 3 trials. In addition to glucose lowering, SGLT2 inhibitors are associated with weight loss and act as osmotic diuretics, resulting in a lowering of BP. While not approved for BP-lowering, they may potentially aid BP goal achievement in people within 7-10 mm Hg of goal.

    PMID:24631482 Oliva RV et al; J Am Soc Hypertens 8(5): 330-9.

    4.3 Drug Warning

    Hypersensitivity reactions (e.g., generalized urticaria), some serious, have been reported with canagliflozin treatment. These reactions generally occurred within hours to days of canagliflozin initiation. If a hypersensitivity reaction occurs, the drug should be discontinued, appropriate treatment instituted, and the patient monitored until signs and symptoms resolve.

    American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 3163

    Dose-dependent increases in low-density lipoprotein (LDL)-cholesterol can occur during canagliflozin therapy. Serum LDL-cholesterol concentrations should be monitored during treatment with canagliflozin and such lipid elevations treated according to the standard of care.

    American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 3162

    When canagliflozin is added to therapy with an insulin secretagogue (e.g., a sulfonylurea) or insulin, the incidence of hypoglycemia is increased compared with sulfonylurea or insulin monotherapy. Therefore, patients receiving canagliflozin may require a reduced dosage of the concomitant insulin secretagogue or insulin to reduce the risk of hypoglycemia.

    American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 3162

    Canagliflozin may increase the risk of genital mycotic infections in males (e.g., balanoposthitis, candidal balanitis) and females (e.g., vulvovaginal candidiasis, vulvovaginal mycotic infection, vulvovaginitis). In clinical trials, patients with a history of genital mycotic infections and uncircumcised males were more likely to develop such infections. Patients should be monitored for genital mycotic infections and appropriate treatment should be instituted if these infections occur.

    American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 3162

    For more Drug Warnings (Complete) data for Canagliflozin (14 total), please visit the HSDB record page.

    4.4 Drug Indication

    This drug is used in conjunction with diet and exercise to increase glycemic control in adults diagnosed with type 2 diabetes mellitus. 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 diabetes[L5897,. In addition to the above, canagliflozin can be used 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. It is important to note that this drug is **not** indicated for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis.

    FDA Label

    Invokana is indicated for the treatment of adults with insufficiently controlled type 2 diabetes mellitus as an adjunct to diet and exercise:

    - as monotherapy when metformin is considered inappropriate due to intolerance or contraindications

    - in addition to other medicinal products for the treatment of diabetes.

    For study results with respect to combination of therapies, effects on glycaemic control, cardiovascular and renal events, and the populations studied, see sections 4. 4, 4. 5 and 5. 1.

    Treatment of type II diabetes mellitus

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    This drug increases urinary glucose excretion and decreases the renal threshold for glucose (RTG) in a dose-dependent manner. The renal threshold is defined as the lowest level of blood glucose associated with the appearance of detectable glucose in the urine. 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 infarction. 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 diabetes.

    5.2 MeSH Pharmacological Classification

    Sodium-Glucose Transporter 2 Inhibitors

    Compounds that inhibit SODIUM-GLUCOSE TRANSPORTER 2. They lower blood sugar by preventing the reabsorption of glucose by the kidney and are used in the treatment of TYPE 2 DIABETES MELLITUS. (See all compounds classified as Sodium-Glucose Transporter 2 Inhibitors.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    CANAGLIFLOZIN ANHYDROUS
    5.3.2 FDA UNII
    6S49DGR869
    5.3.3 Pharmacological Classes
    Sodium-Glucose Cotransporter 2 Inhibitor [EPC]; Sodium-Glucose Transporter 2 Inhibitors [MoA]; P-Glycoprotein Inhibitors [MoA]
    5.4 ATC Code

    A10BK02

    A - Alimentary tract and metabolism

    A10 - Drugs used in diabetes

    A10B - Blood glucose lowering drugs, excl. insulins

    A10BK - Sodium-glucose co-transporter 2 (sglt2) inhibitors

    A10BK02 - Canagliflozin

    5.5 Absorption, Distribution and Excretion

    Absorption

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

    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 urine: **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.

    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 L.

    Clearance

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

    /MILK/ Canagliflozin is distributed into milk in rats; it is not known whether the drug is distributed into human milk.

    American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 3163

    Canagliflozin is an oral antihyperglycemic agent used for the treatment of type 2 diabetes mellitus. It blocks the reabsorption of glucose in the proximal renal tubule by inhibiting the sodium-glucose cotransporter 2. This article describes the in vivo biotransformation and disposition of canagliflozin after a single oral dose of [(14)C]canagliflozin to intact and bile duct-cannulated (BDC) mice and rats and to intact dogs and humans. Fecal excretion was the primary route of elimination of drug-derived radioactivity in both animals and humans. In BDC mice and rats, most radioactivity was excreted in bile. The extent of radioactivity excreted in urine as a percentage of the administered [(14)C]canagliflozin dose was 1.2%-7.6% in animals and approximately 33% in humans. The primary pathways contributing to the metabolic clearance of canagliflozin were oxidation in animals and direct glucuronidation of canagliflozin in humans. Unchanged canagliflozin was the major component in systemic circulation in all species. In human plasma, two pharmacologically inactive O-glucuronide conjugates of canagliflozin, M5 and M7, represented 19% and 14% of total drug-related exposure and were considered major human metabolites. Plasma concentrations of M5 and M7 in mice and rats from repeated dose safety studies were lower than those in humans given canagliflozin at the maximum recommended dose of 300 mg. However, biliary metabolite profiling in rodents indicated that mouse and rat livers had significant exposure to M5 and M7. Pharmacologic inactivity and high water solubility of M5 and M7 support glucuronidation of canagliflozin as a safe detoxification pathway.

    PMID:24568888 Mamidi RN et al. Drug Metab Dispos 42(5): 903-16 (2014).

    The mean absolute oral bioavailability of canagliflozin is approximately 65%. Co-administration of a high-fat meal with canagliflozin had no effect on the pharmacokinetics of canagliflozin; therefore, INVOKANA may be taken with or without food. However, based on the potential to reduce postprandial plasma glucose excursions due to delayed intestinal glucose absorption, it is recommended that INVOKANA be taken before the first meal of the day. The mean steady-state volume of distribution of canagliflozin following a single intravenous infusion in healthy subjects was 119 L, suggesting extensive tissue distribution. Canagliflozin is extensively bound to proteins in plasma (99%), mainly to albumin. Protein binding is independent of canagliflozin plasma concentrations. Plasma protein binding is not meaningfully altered in patients with renal or hepatic impairment. Following administration of a single oral [14C] canagliflozin dose to healthy subjects, 41.5%, 7.0%, and 3.2% of the administered radioactive dose was recovered in feces as canagliflozin, a hydroxylated metabolite, and an O-glucuronide metabolite, respectively. Enterohepatic circulation of canagliflozin was negligible. Approximately 33% of the administered radioactive dose was excreted in urine, mainly as O-glucuronide metabolites (30.5%). Less than 1% of the dose was excreted as unchanged canagliflozin in urine. Renal clearance of canagliflozin 100 mg and 300 mg doses ranged from 1.30 to 1.55 mL/min. Mean systemic clearance of canagliflozin was approximately 192 mL/min in healthy subjects following intravenous administration.

    NIH; DailyMed. Current Medication Information for Invokana (Canagliflozin) Tablet, Film Coated (Updated: September 2015). Available from, as of November 20, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b9057d3b-b104-4f09-8a61-c61ef9d4a3f3

    5.6 Metabolism/Metabolites

    Canagliflozin is primarily metabolized by O-glucuronidation. It is mainly glucuronidated by UGT1A9 and UGT2B4 enzymes to two inactive O-glucuronide metabolites. The oxidative metabolism of canagliflozin by hepatic cytochrome enzyme CYP3A4 is negligible (about 7%) in humans.

    O-glucuronidation is the major metabolic elimination pathway for canagliflozin, which is mainly glucuronidated by UGT1A9 and UGT2B4 to two inactive O-glucuronide metabolites. CYP3A4-mediated (oxidative) metabolism of canagliflozin is minimal (approximately 7%) in humans.

    NIH; DailyMed. Current Medication Information for Invokana (Canagliflozin) Tablet, Film Coated (Updated: September 2015). Available from, as of November 20, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b9057d3b-b104-4f09-8a61-c61ef9d4a3f3

    5.7 Biological 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 dose.

    5.8 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 urine.

    Sodium-glucose co-transporter 2 (SGLT2), expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen. Canagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, canagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose (RTG), and thereby increases urinary glucose excretion (UGE).

    NIH; DailyMed. Current Medication Information for Invokana (Canagliflozin) Tablet, Film Coated (Updated: September 2015). Available from, as of November 20, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b9057d3b-b104-4f09-8a61-c61ef9d4a3f3

    API SUPPLIERS

    read-more
    read-more
    Full Screen ViewFULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]

    API Reference Price

    read-more
    read-more
    [{"dataSource":"API Export","activeIngredients":"CANAGLIFLOZIN","year":"2021","qtr":"Q1","strtotime":1612463400,"product":"CANAGLIFLOZIN (USDMF MSN) USA (CANAGLIF LOZIN)","address":"ZYDUS TOWER, SARKHEJ-GANDHINAGARHIGHWAY SATELLITE CROSS ROADS,","city":"AHMEDABAD\/GUJRAT","supplier":"ZYDUS LIFESCIENCES","supplierCountry":"INDIA","foreign_port":"YANGON","customer":"ALIDAC HEALTHCARE MYANMAR ","customerCountry":"MYANMAR","quantity":"208.61","actualQuantity":"208.611","unit":"KGS","unitRateFc":"2614.9","totalValueFC":"539820","currency":"USD","unitRateINR":188400.96255710392,"date":"05-Feb-2021","totalValueINR":"39302513.2","totalValueInUsd":"539820","indian_port":"AHMEDABAD AIR","hs_no":"29054400","bill_no":"8422059","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"MYANMAR","selfForZScoreResived":"Pharma Grade","supplierPort":"AHMEDABAD AIR","supplierAddress":"ZYDUS TOWER, SARKHEJ-GANDHINAGARHIGHWAY SATELLITE CROSS ROADS,, AHMEDABAD\/GUJRAT","customerAddress":""},{"dataSource":"API Export","activeIngredients":"CANAGLIFLOZIN","year":"2021","qtr":"Q2","strtotime":1620585000,"product":"METROCHEM PRODUCT BATCH NO: PD\/CFZ-VII \/21001 CANAGLIFLOZIN HEMIHYDRATE IHS","address":"FLAT NO.302, BHANU ENCLAVESUNDER NAGAR ,ERRAGADDA","city":"HYDERABAD.AP","supplier":"METROCHEM API PRIVATE LIMITED","supplierCountry":"INDIA","foreign_port":"CAIRO","customer":"\"TO THE ORDER OF\"","customerCountry":"EGYPT","quantity":"0.35","actualQuantity":"0.35","unit":"KGS","unitRateFc":"5692.9","totalValueFC":"1959.9","currency":"USD","unitRateINR":410171.42857142858,"date":"10-May-2021","totalValueINR":"143560","totalValueInUsd":"1959.9","indian_port":"HYDERABAD AIR","hs_no":"29420090","bill_no":"1681805","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"EGYPT","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"FLAT NO.302, BHANU ENCLAVESUNDER NAGAR ,ERRAGADDA, HYDERABAD.AP","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2021","qtr":"Q3","strtotime":1625682600,"product":"CANAGLIFLOZIN HEMIHYDRATE","address":"8-3-166\/7\/1, HETERO HOUSE,\\r\\nERRAGADDA,","city":"HYDERABAD, AP.","supplier":"HONOUR LAB LTD","supplierCountry":"INDIA","foreign_port":"BANGKOK","customer":"SPG INTERNATIONAL CO.LTD","customerCountry":"THAILAND","quantity":"5.00","actualQuantity":"5","unit":"KGS","unitRateFc":"1516.2","totalValueFC":"7329.1","currency":"USD","unitRateINR":109243.39999999999,"date":"08-Jul-2021","totalValueINR":"546217","totalValueInUsd":"7329.1","indian_port":"HYDERABAD AIR","hs_no":"29329990","bill_no":"3002306","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"THAILAND","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"8-3-166\/7\/1, HETERO HOUSE,\\r\\nERRAGADDA,, HYDERABAD, AP.","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2022","qtr":"Q1","strtotime":1648578600,"product":"CANAGLIFLOZINE HEMIHYDRATE IH","address":"H.NO.8-3-166\/7\/1, HETERO HOUSE, ERRAGADDA Contact No: 919396743330","city":"HYDERABAD","supplier":"HONOUR LAB LTD","supplierCountry":"INDIA","foreign_port":"CAIRO","customer":"M\/S.ZETA PHARMA FOR PHARMACEUTICAL","customerCountry":"EGYPT","quantity":"2.50","actualQuantity":"2.5","unit":"KGS","unitRateFc":"1550","totalValueFC":"3765.4","currency":"USD","unitRateINR":114800,"date":"30-Mar-2022","totalValueINR":"287000","totalValueInUsd":"3765.4","indian_port":"HYDERABAD AIR","hs_no":"29420090","bill_no":"9334363","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"EGYPT","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"H.NO.8-3-166\/7\/1, HETERO HOUSE, ERRAGADDA Contact No: 919396743330, HYDERABAD","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2022","qtr":"Q3","strtotime":1659897000,"product":"CANAGLIFLOZIN HEMIHYDRATE IH","address":"H.NO. 8-2-337, BESIDE TV9 OFFICE,,","city":"HYDERABAD,TELANGANA","supplier":"DR. REDDY\\'S LABORATORIES","supplierCountry":"INDIA","foreign_port":"LISBOA","customer":"DR. REDDY\\'S LABORATORIES","customerCountry":"PORTUGAL","quantity":"84.00","actualQuantity":"84","unit":"KGS","unitRateFc":"2399","totalValueFC":"198056.4","currency":"USD","unitRateINR":187604.54761904763,"date":"08-Aug-2022","totalValueINR":"15758782","totalValueInUsd":"198056.4","indian_port":"Reddy r-SEZ\/Srikakulam","hs_no":"29141990","bill_no":"4000327","productDescription":"API","marketType":"REGULATED MARKET","country":"PORTUGAL","selfForZScoreResived":"Pharma Grade","supplierPort":"Reddy r-SEZ\/Srikakulam","supplierAddress":"H.NO. 8-2-337, BESIDE TV9 OFFICE,,, HYDERABAD,TELANGANA","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2023","qtr":"Q4","strtotime":1699900200,"product":"CANAGLIFLOZIN HEMIHYDRATE IH","address":"H.NO. 8-2-337,BESIDE TV9 OFFICE","city":"HYDERABAD ANDHRA PRADESH","supplier":"DR. REDDY\\'S LABORATORIES","supplierCountry":"INDIA","foreign_port":"LISBOA","customer":"XX.REXXY SXXABOXXTORXXS SXX.","customerCountry":"PORTUGAL","quantity":"49.00","actualQuantity":"49","unit":"KGS","unitRateFc":"2389.7","totalValueFC":"115871.7","currency":"USD","unitRateINR":196913.10204081633,"date":"14-Nov-2023","totalValueINR":"9648742","totalValueInUsd":"115871.7","indian_port":"Reddy r-SEZ\/Srikakulam","hs_no":"29141990","bill_no":"4000735","productDescription":"API","marketType":"REGULATED MARKET","country":"PORTUGAL","selfForZScoreResived":"Pharma Grade","supplierPort":"Reddy r-SEZ\/Srikakulam","supplierAddress":"H.NO. 8-2-337,BESIDE TV9 OFFICE, HYDERABAD ANDHRA PRADESH","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2023","qtr":"Q4","strtotime":1703183400,"product":"CANAGLIFLOZIN HEMIHYDRATE (*LUT ARN NO:AD271223002123V DATE: 01\/12\/2023)","address":"","city":"","supplier":"GALLEAN HEALTHCARE PRIVATE LIMITED","supplierCountry":"INDIA","foreign_port":"ALGIERS","customer":"SARL BEKER LABORATORIES","customerCountry":"ALGERIA","quantity":"61.73","actualQuantity":"61.73","unit":"KGS","unitRateFc":"1500","totalValueFC":"91983.5","currency":"USD","unitRateINR":124040.17495545116,"date":"22-Dec-2023","totalValueINR":"7657000","totalValueInUsd":"91983.5","indian_port":"Bombay Air","hs_no":"29322090","bill_no":"6245222","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"ALGERIA","selfForZScoreResived":"Pharma Grade","supplierPort":"Bombay Air","supplierAddress":"","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1720722600,"product":"CANAGLIFLOZIN IN-HOUSE","address":"INDOCO HOUSE,166 CST RD.VIDYANAGRI,","city":"MUMBAI.MAHARASHTRA","supplier":"INDOCO REMEDIES LIMITED","supplierCountry":"INDIA","foreign_port":"TAIPEI","customer":"TO ORDER","customerCountry":"TAIWAN","quantity":"1.50","actualQuantity":"1.5","unit":"KGS","unitRateFc":"1475","totalValueFC":"2080.1","currency":"USD","unitRateINR":115917.83333333333,"date":"12-Jul-2024","totalValueINR":"173876.75","totalValueInUsd":"2080.1","indian_port":"Bombay Air","hs_no":"29420090","bill_no":"2387289","productDescription":"API","marketType":"REGULATED MARKET","country":"TAIWAN","selfForZScoreResived":"Pharma Grade","supplierPort":"Bombay Air","supplierAddress":"INDOCO HOUSE,166 CST RD.VIDYANAGRI,, MUMBAI.MAHARASHTRA","customerAddress":""},{"dataSource":"API Import","activeIngredients":"CANAGLIFLOZIN","year":"2021","qtr":"Q2","strtotime":1617561000,"product":"(N.C.V) CANAGLIFLOZIN (FOR TESTING PURPOSE ONLY)","address":"30 FORJETT STREETPOST BOX NO 9301","city":"MUMBAI, MAHARASHTRA.","supplier":"JOHNSON & JOHNSON","supplierCountry":"BELGIUM","foreign_port":"BRUSSELS","customer":"JOHNSON & JOHNSON","customerCountry":"INDIA","quantity":"0.13","actualQuantity":"130.5","unit":"GMS","unitRateFc":"1.8","totalValueFC":"270.3","currency":"EUR","unitRateINR":"154.2","date":"05-Apr-2021","totalValueINR":"20120.93","totalValueInUsd":"270.3","indian_port":"BOMBAY AIR","hs_no":"29339990","bill_no":"3441316","productDescription":"API","marketType":"REGULATED MARKET","country":"BELGIUM","selfForZScoreResived":"Pharma Grade","supplierPort":"BRUSSELS","supplierAddress":"","customerAddress":"30 FORJETT STREETPOST BOX NO 9301"},{"dataSource":"API Import","activeIngredients":"","year":"2022","qtr":"Q2","strtotime":1652812200,"product":"(N.C.V) CANAGLIFLOZIN (FOR TESTING PURPOSE ONLY)","address":"L.B.S. MARG,,MULUND-WEST","city":"MUMBAI,MAHARASHTRA","supplier":"JOHNSON & JOHNSON","supplierCountry":"BELGIUM","foreign_port":"NA","customer":"JOHNSON & JOHNSON","customerCountry":"INDIA","quantity":"0.08","actualQuantity":"83.19","unit":"GMS","unitRateFc":"1.9","totalValueFC":"165.1","currency":"EUR","unitRateINR":"153.4","date":"18-May-2022","totalValueINR":"12757.49","totalValueInUsd":"165.1","indian_port":"BOMBAY AIR","hs_no":"29332990","bill_no":"8731653","productDescription":"API","marketType":"REGULATED MARKET","country":"BELGIUM","selfForZScoreResived":"Pharma Grade","supplierPort":"NA","supplierAddress":"","customerAddress":"L.B.S. MARG,,MULUND-WEST"},{"dataSource":"API Import","activeIngredients":"","year":"2023","qtr":"Q2","strtotime":1680546600,"product":"(N.C.V) CANAGLIFLOZIN (FOR TESTING PURPOSE ONLY)","address":"L.B.S. MARG,,MULUND-WEST","city":"MUMBAI,MAHARASHTRA","supplier":"JOHNSON & JOHNSON","supplierCountry":"BELGIUM","foreign_port":"NA","customer":"JOHNSON & JOHNSON","customerCountry":"INDIA","quantity":"0.56","actualQuantity":"560.84","unit":"GMS","unitRateFc":"1.8","totalValueFC":"1074.3","currency":"EUR","unitRateINR":"157","date":"04-Apr-2023","totalValueINR":"88045.47","totalValueInUsd":"1074.3","indian_port":"BOMBAY AIR","hs_no":"29349990","bill_no":"5367779","productDescription":"API","marketType":"REGULATED MARKET","country":"BELGIUM","selfForZScoreResived":"Pharma Grade","supplierPort":"NA","supplierAddress":"","customerAddress":"L.B.S. MARG,,MULUND-WEST"}]
    05-Feb-2021
    12-Jul-2024
    KGS
    overview
    Loading...

    Average Price (USD/KGS)

    Number of Transactions

    Total Quantity (KGS)

    Total Value (USD)

    Quantity (KGS) & Unit rate (USD/KGS) over time

    API Imports and Exports

    Importing Country Total Quantity
    (KGS)    		 Average Price
    (USD/KGS)    		 Number of Transactions

    Upgrade, download data, analyse, strategize, subscribe with us contact

    DRUG PRODUCT COMPOSITIONS

    Do you need Business Intel? Ask us

    DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 150M...DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 150MG;1GM

    USFDA APPLICATION NUMBER - 205879

    read-more

    DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 150M...DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 150MG;500MG

    USFDA APPLICATION NUMBER - 205879

    read-more

    DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 50MG...DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 50MG;1GM

    USFDA APPLICATION NUMBER - 205879

    read-more

    DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 50MG...DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 50MG;500MG

    USFDA APPLICATION NUMBER - 205879

    read-more

    Related Excipient Companies

    Upload your portfolio for free, ask us

    Excipients by Applications

    Click here to find the perfect excipient manufacturers by their capabilities

    Coating Systems & Additives

    read-more
    read-more

    Fillers, Diluents & Binders

    read-more
    read-more

    Controlled & Modified Release

    read-more
    read-more

    Direct Compression

    read-more
    read-more

    Disintegrants & Superdisintegrants

    read-more
    read-more

    Thickeners and Stabilizers

    read-more
    read-more

    Lubricants & Glidants

    read-more
    read-more

    Granulation

    read-more
    read-more

    Co-Processed Excipients

    read-more
    read-more

    Topical

    read-more
    read-more

    Film Formers & Plasticizers

    read-more
    read-more

    Empty Capsules

    read-more
    read-more

    Coloring Agents

    read-more
    read-more

    Solubilizers

    read-more
    read-more

    Parenteral

    read-more
    read-more

    Vegetarian Capsules

    read-more
    read-more

    API Stability Enhancers

    read-more
    read-more

    Taste Masking

    read-more
    read-more

    Rheology Modifiers

    read-more
    read-more

    Chewable & Orodispersible Aids

    read-more
    read-more

    Emulsifying Agents

    read-more
    read-more

    Digital Content read-more

    Create Content with PharmaCompass, ask us

    DATA COMPILATION #PharmaFlow

    read-more
    read-more

    NEWS #PharmaBuzz

    read-more
    read-more

    Global Sales Information

    Do you need Business Intel? Ask us

    Market Place

    Do you need sourcing support? Ask us

    Patents & EXCLUSIVITIES

    Check the patents & exclusivity for this product

    REF. STANDARDS & IMPURITIES

    Upload your portfolio for free, ask us

    ABOUT THIS PAGE

    Ask Us for Pharmaceutical Supplier and Partner
    Ask Us, Find A Supplier / Partner
    No Commissions, No Strings Attached, Get Connected for FREE

    What are you looking for?

    How can we help you?

    The request can't be empty

    Please read our Privacy Policy carefully

    You must agree to the privacy policy

    The name can't be empty
    The company can't be empty.
    The email can't be empty Please enter a valid email.
    The mobile can't be empty

    Market Place

    Market Place

    PharmaCompass

    Home

    Market Place

    Menu

    Post Enquiry

    Post Enquiry

    Market Place

    Market Place

    Search