Tofogliflozin Explained

Tofogliflozin (INN,^[1] USAN, codenamed CSG452) is an experimental drug for the treatment of diabetes mellitus and is being developed by Chugai Pharma in collaboration with Kowa and Sanofi.^[2] It is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney., the drug is in Phase III clinical trials.^{[3] [4]}

Chemistry

The active moiety or anhydrous form (ChemSpider ID: 28530778, CHEMBL2110731) has the chemical formula C₂₂H₂₆O₆ and a molecular mass of 386.44 g/mol.

The United States Adopted Name tofogliflozin applies to the monohydrate, which is the form used as a drug.^[5] The International Nonproprietary Name tofogliflozin applies to the anhydrous compound and the drug form is referred to as tofogliflozin hydrate.

See also

• Gliflozin

Notes and References

1. Web site: International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 65. World Health Organization. 15 November 2016.
2. http://www.chugai-pharm.co.jp/hc/ss/english/ir/reports_downloads/pipeline.html Chugai Pharmaceutical: Development Pipeline
3. Nagata T, Fukazawa M, Honda K, Yata T, Kawai M, Yamane M, Murao N, Yamaguchi K, Kato M, Mitsui T, Suzuki Y, Ikeda S, Kawabe Y . 6 . Selective SGLT2 inhibition by tofogliflozin reduces renal glucose reabsorption under hyperglycemic but not under hypo- or euglycemic conditions in rats . American Journal of Physiology. Endocrinology and Metabolism . 304 . 4 . E414-23 . February 2013 . 23249697 . 10.1152/ajpendo.00545.2012 .
4. Ohtake Y, Sato T, Kobayashi T, Nishimoto M, Taka N, Takano K, Yamamoto K, Ohmori M, Yamaguchi M, Takami K, Yeu SY, Ahn KH, Matsuoka H, Morikawa K, Suzuki M, Hagita H, Ozawa K, Yamaguchi K, Kato M, Ikeda S . 6 . Discovery of tofogliflozin, a novel C-arylglucoside with an O-spiroketal ring system, as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes . Journal of Medicinal Chemistry . 55 . 17 . 7828–40 . September 2012 . 22889351 . 10.1021/jm300884k .
5. http://www.ama-assn.org/resources/doc/usan/tofogliflozin.pdf Statement on a nonproprietary name adopted by the USAN council: Tofogliflozin