Product Information
Registration Status: ActiveINVOKANA FILM-COATED TABLET 300mg is approved to be sold in Singapore with effective from 2014-02-21. It is marketed by JOHNSON & JOHNSON PTE LTD, with the registration number of SIN14507P.
This product contains Canagliflozin 300mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Janssen Ortho in PUERTO RICO, and LLC in ITALY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Canagliflozin belongs to a new class of anti-diabetic drugs that works by inhibiting the sodium-glucose transport protein (SGLT2). This transport protein is found in the kidney and is responsible for reabsorbing glucose that has been filtered. FDA approved on March 29, 2013.
Indication
Canagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Use in type 1 diabetes mellitus patients or in treatment of diabetic ketoacidosis is not recommended.
Mechanism of Action
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.
Pharmacokinetics
- Absorption
- The pharmacokinetics of canagliflozin is similar in healthy subjects and patients with type 2 diabetes. Plasma Cmax and AUC of canagliflozin increased in a dose-proportional manner from 50 mg to 300 mg. Accumulation in plasma has been observed following multiple doses of 100 - 300 mg. Food does not affect the absorption of canagliflozin. Tmax = 1- 2 hours; Cmax = 1059 - 3148 ng/mL; Time to steady state, once daily dose, 100 - 300 mg = 4-5 days; Absolute oral bioavailability = 65%.
- Distribution
- Steady state, single IV infusion, healthy subject = 119 L. This high value suggests that cangliflozin is extensively distributed to tissue.
- Metabolism
- Canagliflozin is hepatically metabolized via O-glucuronidation into two inactive O-glucuronide metabolites. The enzymes that facilitate this process are UGT1A9 and UGT2B4. To a lesser extent (7%), canagliflozin also undergoes oxidative metabolism via CYP3A4. Canagliflozin weakly inhibited CYP2B6, CYP2C8, CYP2C9, and CYP3A4 based on in vitro studies with human hepatic microsomes.
- Elimination
Clearance
Mean systemic clearance, healthy subjects, IV administration = 192 mL/min. Renal clearance of canagliflozin 100 mg and 300 mg doses ranged from 1.30 to 1.55 mL/min.
Toxicity
Most common adverse reactions associated with canagliflozin (5% or greater incidence): female genital mycotic infections, urinary tract infection, and increased urination.
Active Ingredient/Synonyms
Canagliflozin anhydrous | Canagliflozin |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.