Saxagliptin (rINN), previously identified as BMS-477118, is a new oral hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. It was developed by Bristol-Myers Squibb. The trade name under which saxagliptin will be marketed has not yet been released.
It is currently in Phase III clinical trials in the U.S. and Europe for the treatment of type 2 diabetes mellitus.
Dipeptidyl peptidase-4's role in blood glucose regulation is thought to be through degradation of GIP and the degradation of GLP-1.
Bristol-Myers Squibb announced on 27 December 2006 that Otsuka Pharmaceutical Co. has been granted exclusive rights to develop and commercialize the compound in Japan. Under the licensing agreement, Otsuka will be responsible for all development costs, but Bristol-Myers Squibb retains rights to co-promote saxagliptin with Otsuka in Japan. Further, on 11 January 2007 it was announced that Bristol-Myers Squibb and AstraZeneca would work together to complete development of the drug an in subsequent marketing.
- ^ Augeri D et al. (2005). "Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes". Journal of Medicinal Chemistry 48 (15): 5025–5037. PMID 16033281.
- ^ Saxagliptin Treatment in Subjects With Type 2 Diabetes Who Are Not Controlled With Diet and Exercise. ClinicalTrials.gov (United States National Institutes of Health) (3 November 2006). Retrieved on 2007-01-11. ClinicalTrials.gov Identifier: NCT00121641
- ^ a b Mentlein, R; Gallwitz, B; Schmidt, WE (15 June 1993). "Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum". European Journal of Biochemistry 214 (3): 829–835. PMID 8100523. Retrieved on 2007-01-11.
- ^ Ahrén, Bo; Landin-Olsson, Mona; Jansson, Per-Anders; Svensson, Maria; Holmes, David; Schweizer, Anja (May 2004). "Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes". Journal of Clinical Endocrinology & Metabolism 89 (5): 2078–2084. PMID 15126524. Retrieved on 2007-01-11.
- ^ Bristol-Myers Squibb (December 27, 2006). "Bristol-Myers Squibb and Otsuka Pharmaceutical Co., Ltd. Announce Exclusive Licensing Agreement for Diabetes Compound Saxagliptin in Japan". Press release. Retrieved on 2006-12-27.
- ^ Associated Press. "AstraZeneca teams with Bristol-Myers on diabetes drugs", Delaware News-Journal, 11 January 2007. Retrieved on 2007-01-11.
|Oral antidiabetic drugs and Insulin analogs (A10)|
|Sulfonylureas||Chlorpropamide, Glibenclamide (Glyburide), Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolazamide, Tolbutamide|
|Alpha-glucosidase inhibitors||Acarbose, Miglitol, Voglibose|
|Thiazolidinediones (TZD)||Pioglitazone, Rosiglitazone, Troglitazone|
|Meglitinides||Nateglinide, Repaglinide, Mitiglinide|
|Dipeptidyl peptidase-4 (DPP-4) inhibitors||Saxagliptin, Sitagliptin, Vildagliptin|
|Glucagon-like peptide-1 analog||Exenatide|
|Insulin analogs||fast acting (Insulin lispro, Insulin aspart, Insulin glulisine), intermediate-acting (NPH insulin), long acting (Insulin glargine, Insulin detemir)|