Luhan Pharmachem Co., Ltd.

Luhan pharmachem Co., Ltd. supplies Canagliflozin bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Canagliflozin is manufactured by cGMP compliant facility. Welcome to contact us for further details including current DMF status for the product and up to date regulatory status of the manufacturing facility. We look forward to assisting you with your research and development projects.

What is Canagliflozin?

Canagliflozin (trade name Invokana) is a drug of the gliflozin class, advice used for the treatment of type 2 diabetes. It was developed by Mitsubishi Tanabe Pharma and is marketed under license by Janssen, a division of Johnson & Johnson.

Canagliflozin is an antidiabetic drug used to improve glycemic control in people with type 2 diabetes. In clinical trials, canagliflozin produced a dose-dependent reduction in HbA1c of 0.91 to 1.16 greater than that obtained with placebo when administered as monotherapy from a baseline of 8.0%, in combination with metformin, or in combination with metformin and a sulfonylurea. Modest effects on the secondary efficacy endpoint of decreased body weight (0.3% to 3.3% greater than placebo) were observed as well. Canagliflozin produces beneficial effects on HDL cholesterol and systolic blood pressure, but these effects are offset by increased LDL cholesterol.

Mechanism of action

Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes about 100 grams of blood glucose per day to be eliminated through the urine, corresponding to 450 kilocalories. Additional water is eliminated by osmotic diuresis, resulting in a lowering of blood pressure. Two thirds of the resulting weight loss are caused by the body using up fat tissue to replace the lost glucose, and the rest is mostly water.
This mechanism is associated with a low risk of hypoglycaemia (too low blood glucose) compared to other antidiabetic drugs such as sulfonylurea derivatives and insulin.

Adverse Effects

Canagliflozin increased (generally mild) urinary tract infections, genital fungal infections, thirst, LDL cholesterol, and was associated with increased urination and episodes of low blood pressure.

There are concerns it may increase the risk of diabetic ketoacidosis.

Cardiovascular problems have been discussed with this class of drugs along with canagliflozin. The pre-specified endpoint for cardiovascular safety in the canagliflozin clinical development program was Major Cardiovascular Events Plus (MACE-Plus), defined as the occurrence of any of the following events: cardiovascular death, non-fatal myocardial infarction, non-fatal stroke, or unstable angina leading to hospitalization. This endpoint occurred in more people in the placebo group (20.5%) than in the canagliflozin treated group (18.9%), but the difference was not statistically significant.

Nonetheless, an FDA advisory committee expressed concern regarding the cardiovascular safety of canagliflozin. A greater number of cardiovascular events was observed during the first 30 days of treatment in canagliflozin treated people (0.45%) relative to placebo treated people (0.07%), suggesting an early period of enhanced cardiovascular risk. In addition, there was an increased risk of stroke in canagliflozin treated people. Neither of these effects was statistically significant. Additional cardiovascular safety data from the ongoing CANVAS trial is expected in 2015.

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.