pharmacopeia
GET
/api/v1/drug/canagliflozin
2D structure
(2S,3R,4R,5S,6R)-2-[3-[[5-(4-fluorophenyl)thiophen-2-yl]methyl]-4-methylphenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
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
InChIKey XTNGUQKDFGDXSJ-ZXGKGEBGSA-N

Mechanism of action

Sourced from openFDA

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.

Sodium-Glucose Transporter 2

Indications

Sourced from openFDA
  • INVOKANA (canagliflozin) is indicated: as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. to reduce the risk of major adverse cardiovascular events (cardiovascular death, nonfatal myocardial infarction and nonfatal stroke) in adults with type 2 diabetes mellitus and established cardiovascular disease (CVD).ICD-10: E11.9, I21.9, I63.9

Contraindications

Sourced from openFDA
  • INVOKANA is contraindicated in patients with a serious hypersensitivity reaction to INVOKANA, such as anaphylaxis or angioedema [see Warnings and Precautions (5.8) and Adverse Reactions (6.1 , 6.2) ] .contraindicated

Dosage & administration

Sourced from openFDA

Assess renal function before initiating and as clinically indicated ( 2.1 ) The recommended starting dose is 100 mg once daily, taken before the first meal of the day ( 2.2 ) Dose can be increased to 300 mg once daily in patients tolerating 100 mg once daily who have an eGFR of 60 mL/min/1.73 m 2 or greater and require additional glycemic control ( 2.2 ) Dose adjustment for patients with renal impairment may be required ( 2.3 ) See full prescribing information for INVOKANA dosage modifications due to drug interactions ( 2.4 ) Withhold INVOKANA at least 3 days, if possible, prior to major surgery or procedures associated with prolonged fasting ( 2.5 ). 2.1 Prior to Initiation of INVOKANA Assess renal function before initiating INVOKANA and as clinically indicated [see Dosage and Administration (2.3) and Warnings and Precautions (5.3) ] . In patients with volume depletion, correct this condition before initiating INVOKANA [see Warnings and Precautions (5.3) and Use in Specific Populations (8.5 , 8.6) ] . 2.2 Recommended Dosage and Administration The recommended dosage of INVOKANA is 100 mg orally once daily, taken before the first meal of the day. For additional glycemic control, the dosage of INVOKANA may be increased to the maximum recommended dosage of 300 mg once daily. 2.3 Recommended Dosage in Patients with Renal Impairment Table 1 provides dosage recommendations for patients with renal impairment, based on estimated glomerular filtration rate (eGFR).

Warnings & precautions

Sourced from openFDA

Diabetic Ketoacidosis in Patients with Type 1 Diabetes Mellitus and Other Ketoacidosis : Consider ketone monitoring in patients at risk for ketoacidosis, as indicated. Assess for ketoacidosis regardless of presenting blood glucose levels and discontinue INVOKANA if ketoacidosis is suspected. Monitor patients for resolution of ketoacidosis before restarting ( 5.1 ) Lower Limb Amputation : Consider factors that may increase the risk of amputation before initiating INVOKANA. Monitor patients for infection or ulcers of lower limb and discontinue if these occur ( 5.2 ) Volume Depletion : May result in acute kidney injury. Before initiating INVOKANA, assess and correct volume status in patients with renal impairment, elderly patients, or patients on loop diuretics. Monitor for signs and symptoms during therapy ( 5.3 ) Urosepsis and pyelonephritis : Evaluate patients for signs and symptoms of urinary tract infections and treat promptly, if indicated ( 5.4 ) Hypoglycemia : Consider a lower dose of insulin or the insulin secretagogue to reduce the risk of hypoglycemia when used in combination with INVOKANA ( 5.5 ) Necrotizing fasciitis of the perineum (Fournier's gangrene) : Serious, life-threatening cases have occurred in both females and males. Assess patients presenting with pain or tenderness, erythema, or swelling in the genital or perineal area, along with fever or malaise.

Adverse reactions

Sourced from openFDA

The following important adverse reactions are described below and elsewhere in the labeling: Diabetic Ketoacidosis in Patients with Type 1 Diabetes and Other Ketoacidosis [see Warnings and Precautions (5.1) ] Lower Limb Amputation [see Warnings and Precautions (5.2) ] Volume Depletion [see Warnings and Precautions (5.3) ] Urosepsis and Pyelonephritis [see Warnings and Precautions (5.4) ] Hypoglycemia with Concomitant Use with Insulin and Insulin Secretagogues [see Warnings and Precautions (5.5) ] Necrotizing Fasciitis of the Perineum (Fournier's gangrene) [see Warnings and Precautions (5.6) ] Genital Mycotic Infections [see Warnings and Precautions (5.7) ] Hypersensitivity Reactions [see Warnings and Precautions (5.8) ] Bone Fracture [see Warnings and Precautions (5.9) ] Most common adverse reactions (5% or greater incidence): female genital mycotic infections, urinary tract infection, and increased urination ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Janssen Pharmaceuticals, Inc. at 1-800-526-7736 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Studies Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to the rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

Use in specific populations

Sourced from openFDA

Pregnancy : Advise females of the potential risk to a fetus especially during the second and third trimesters ( 8.1 ) Lactation : Not recommended when breastfeeding ( 8.2 ) Geriatrics : Higher incidence of adverse reactions related to reduced intravascular volume ( 8.5 ) Renal impairment : Higher incidence of adverse reactions related to hypotension and renal function ( 8.6 ) Hepatic impairment : Not recommended in patients with severe hepatic impairment ( 8.7 ) 8.1 Pregnancy Risk Summary Based on animal data showing adverse renal effects, INVOKANA is not recommended during the second and third trimesters of pregnancy. Limited data with INVOKANA in pregnant women are not sufficient to determine a drug-associated risk for major birth defects or miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy [see Clinical Considerations ]. In animal studies, adverse renal pelvic and tubule dilatations that were not reversible were observed in rats when canagliflozin was administered during a period of renal development corresponding to the late second and third trimesters of human pregnancy, at an exposure 0.5-times the 300 mg clinical dose, based on AUC.

Pharmacokinetics

Sourced from openFDA
Metabolism
The pharmacokinetics of canagliflozin is similar in healthy subjects and patients with type 2 diabetes. Following single-dose oral administration of 100 mg and 300 mg of INVOKANA, peak plasma concentrations (median T max ) of canagliflozin occurs within 1 to 2 hours post-dose.

Overdosage

Sourced from openFDA

In the event of an overdose, contact the Poison Control Center. It is also reasonable to employ the usual supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive treatment as dictated by the patient's clinical status. Canagliflozin was negligibly removed during a 4-hour hemodialysis session. Canagliflozin is not expected to be dialyzable by peritoneal dialysis.

Approval history

Sourced from openFDA
  • Mar 29, 2013NDANDA204042Janssen Pharms
  • Aug 8, 2014NDANDA204353Janssen Pharms
  • Sep 20, 2016NDANDA205879Janssen Pharms

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
30,943 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Diabetic Ketoacidosis3,50811%
  2. 2Toe Amputation2,2637.3%
  3. 3Osteomyelitis2,2337.2%
  4. 4Acute Kidney Injury2,0346.6%
  5. 5Fungal Infection1,4904.8%
  6. 6Weight Decreased1,4034.5%
  7. 7Blood Glucose Increased1,3004.2%
  8. 8Gangrene1,1123.6%
  9. 9Nausea1,0843.5%
  10. 10Off Label Use1,0643.4%
  11. 11Cellulitis1,0633.4%
  12. 12Drug Ineffective1,0473.4%
  13. 13Urinary Tract Infection1,0473.4%
  14. 14Dizziness8812.8%
  15. 15Diabetic Foot Infection8642.8%

Literature

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Recent PubMed references pinned to Canagliflozin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 180 ClinicalTrials.gov registrations naming Canagliflozin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Canagliflozin work?
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.
What is Canagliflozin used for?
According to FDA labeling, Canagliflozin carries indications including: INVOKANA (canagliflozin) is indicated: as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. to reduce the risk of major adverse cardiovascular events (cardiovascular death, nonfatal myocardial infarction and nonfatal stroke) in adults with type 2 diabetes mellitus and established cardiovascular disease (CVD).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Canagliflozin?
Canagliflozin is classified as Sodium-glucose co-transporter 2 (SGLT2) inhibitors, Sodium-Glucose Transporter 2 Inhibitors, Increased Renal Organic Ion Excretion, Renal Ion Transport Alteration.
What are the brand names for Canagliflozin?
Canagliflozin is marketed under brand names including Invokamet, Invokana.
What are the contraindications for Canagliflozin?
Canagliflozin labeling lists contraindications including: INVOKANA is contraindicated in patients with a serious hypersensitivity reaction to INVOKANA, such as anaphylaxis or angioedema [see Warnings and Precautions (5.8) and Adverse Reactions (6.1 , 6.2) ] .. Always consult the full prescribing information and a clinician.
Note. Data for canagliflozin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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