Canagliflozin hemihydrate 928672-86-0

Canagliflozin, an orally active and selective sodium–glucose cotransporter 2 (SGLT2) inhibitor, was co-developed by Mitsubishi Tanabe Pharma and Johnson & Johnson (J&J) for the treatment of type 2 diabetes mellitus (T2DM) and obesity. The drug was approved in March by the U.S. FDA and launched in April 2013 in the U.S. SGLT2 is involved in the glucose re-absorption pathway in the kidney, and its inhibition increases urinary glucose excretion, and reduces plasma glucose and HbA1c levels. In addition, canagliflozin is safe in combination with other commonly used antidiabetic agents and has a significant effect on body weight reduction. A recently published process patent from ScinoPharm Taiwan describes the synthesis of canagliflozin.

Canagliflozin Hemihydrate is a derivative of Canagliflozin (C175190), which is a sodium/glucose cotransporter 2 (SGLT2) inhibitor. Canagliflozin has been shown to dose dependently reduce calculated renal threshold for glucose excretion and increase urinary glucose excretion. Canagliflozin is a candidate for the treatment of type 2 diabetes and obesity.

Canagliflozin is the first SGLT2 inhibitor approved by FDA for the treatment of type II diabetes in adult patients. SGLT is a glucose transporter protein that has two subtypes, SGLT1 and SGLT2, respectively distributed in the small intestine mucosa and renal tubules. It can transport glucose into the bloodstream. Kagliflozin can inhibit SLCT2, preventing the smooth reabsorption of glucose in renal tubules into the bloodstream and excreting it in urine, thereby reducing blood sugar concentration. Due to the excretion of glucose into urine through the kidneys, it is accompanied by side effects such as renal dysfunction, symptomatic hypotension, and fungal infections. Nine clinical trials involving Chemicalbook and 10285 patients have demonstrated the safety and efficacy of Invokana, which can be used alone or in combination with other hypoglycemic drugs. In a 26 week double-blind controlled trial, 584 patients with type II diabetes were divided into three groups, namely, 100mg cagelin group, 300mg cagelin group and placebo group. Compared with placebo, 100mg cagelin group had an average additional reduction of 0.91% in HbA1c, and 300mg cagelin group had an average additional reduction of 1.16% in HbA1c. The above information was edited and organized by Xiaonan from Chemicalbook.