title: Saxagliptin: a new drug for the treatment of type 2 diabetes.
abstract: Saxagliptin (BMS-477118) has been recently FDA approved drug for the management of T2DM developed by Bristol-Myers Squibb and AstraZeneca under the trade name Onglyza. Saxagliptin is a nitrile-containing selective, potent, reversible and durable DPP IV inhibitor developed as an alternative second-line adds on to Metformin in place of a sulphonylurea. Saxagliptin increases and prolongs the action of incretin hormones by inhibiting the DPP IV enzyme that inactivates incretins usually within minutes. Saxagliptin is well absorbed and has low plasma protein binding and displays slow-binding properties to DPP IV. Saxagliptin is metabolized in vivo to form an active metabolite (BMS-510849), which is twofold less potent than the parent molecule. The X-ray crystallography revealed that Saxagliptin is covalently bound to the DPP IV active site. In drug-native patients with T2DM and inadequate glycemic control, once-daily Saxagliptin monotherapy for 24 wks demonstrated clinically meaningful with no weight gain and generally well tolerated.
authors.affiliation: University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh-160014, India.
authors.forename: Suresh
authors.initials: S
authors.lastname: Thareja
authors.forename: Saurabh
authors.initials: S
authors.lastname: Aggarwal
authors.forename: Priyanka
authors.initials: P
authors.lastname: Malla
authors.forename: Diksha
authors.initials: D
authors.lastname: Haksar
authors.forename: Tilak Raj
authors.initials: TR
authors.lastname: Bhardwaj
authors.forename: Manoj
authors.initials: M
authors.lastname: Kumar
mesh_terms: D000218:Adamantane / Q000031:analogs & derivatives* / Q000737:chemistry / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D004151:Dipeptides / Q000737:chemistry* / Q000627:therapeutic use; D018819:Dipeptidyl Peptidase 4 / Q000378:metabolism; D054873:Dipeptidyl-Peptidase IV Inhibitors; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000627:therapeutic use; D054795:Incretins / Q000378:metabolism; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology
chemical_list: D004151:Dipeptides; D054873:Dipeptidyl-Peptidase IV Inhibitors; D007004:Hypoglycemic Agents; D054795:Incretins; D011480:Protease Inhibitors; C502994:saxagliptin; D018819:Dipeptidyl Peptidase 4; D000218:Adamantane