Canagliflozin
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| Pronunciation | /ˌkænəɡlɪˈfloʊzɪn/ KAN-ə-glif-LOH-zin |
| Trade names | Invokana, Sulisent, Prominad |
| Synonyms | JNJ-28431754; TA-7284; (1S)-1,5-anhydro-1-C-(3-{[5-(4-fluorophenyl)thiophen-2-yl]methyl]}-4-methylphenyl)-D-glucitol |
| AHFS/Drugs.com | invokana |
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By mouth (tablets) |
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| Pharmacokinetic data | |
| Bioavailability | 65% |
| Protein binding | 99% |
| Metabolism | Hepatic glucuronidation |
| Biological half-life | 11.8 (10–13) hours |
| Excretion | Faecal and 33% renal |
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| ECHA InfoCard | 100.223.671 |
| Chemical and physical data | |
| Formula | C24H25FO5S |
| Molar mass | 444.52 g/mol |
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Canagliflozin (trade name Invokana or Sulisent) is a medication used for the treatment of type 2 diabetes. It is of the gliflozin class or subtype 2 sodium-glucose transport (SGLT-2) inhibitors class.
This mechanism is associated with a low risk of hypoglycaemia (too low blood glucose) compared to sulfonylurea derivatives and insulin. In 2017, the FDA concluded that canagliflozin causes an increased risk of leg and foot amputations. The FDA began requiring a Boxed Warning to be added to the canagliflozin drug labels to describe this risk.
Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine. It was developed by Mitsubishi Tanabe Pharma and is marketed under license by Janssen, a division of Johnson & Johnson.
Canagliflozin is an anti-diabetic drug used to improve glycemic control in people with type 2 diabetes. In extensive clinical trials, canagliflozin produced a consistent dose-dependent decrease in HbA1c levels of 0.77% to 1.16% when administered either as monotherapy, in combination with metformin, in combination with metformin and a sulfonylurea, in combination with metformin and pioglitazone, or in combination with insulin, from initial HbA1c levels of 7.8% to 8.1%. When added to metformin, canagliflozin daily was shown to be non-inferior to both sitagliptin 100 mg daily and glimepiride in reducing HbA1c levels at one year, whilst canagliflozin 300 mg successfully demonstrated statistical superiority over both sitagliptin and glimiperide in decreasing HbA1c levels. Secondary efficacy endpoints of higher reductions in weight and blood pressure (versus sitagliptin and glimiperide) were also observed in studies. Canagliflozin produces beneficial effects on HDL cholesterol whilst increasing LDL cholesterol to produce no change in total cholesterol.
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