Saxagliptin, a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Saxagliptin, a dipeptidyl peptidase-IV (DPP-IV) inhibitor, is currently under development by Bristol-Myers Squibb Co, AstraZeneca plc and Otsuka Pharmaceutical Co Ltd for the treatment of type 2 diabetes. The compound has high selectivity for DPP-IV compared with other dipeptidyl peptidases and a duration profile designed for once-daily dosing. DPP-IV inhibitors act by increasing levels of glucagon-like peptide-1, which stimulates insulin secretion. In animal studies, saxagliptin improved glucose clearance and raised insulin levels in rodents. Clinical trials have demonstrated a dose-dependent inhibition of DPP-IV by saxagliptin without serious side effects. Results have demonstrated that treatment with saxagliptin lowers blood glucose levels, with good tolerability and safety. The specific advantages of saxagliptin over other DPP-IV inhibitors may lie in its long-lived, effective and highly specific inhibition of DPP-IV, making once-daily treatment feasible, effective and safe.
Gallwitz
Baptist
B
Eberhard-Karls-University, Department of Medicine IV, Otfried-Müller-Strasse 10, 72076 Tübingen, Germany. baptist.gallwitz@med.uni-tuebingen.de
D000218:Adamantane / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D004151:Dipeptides / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use* / Q000633:toxicity; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000009:adverse effects / Q000627:therapeutic use* / Q000633:toxicity; D006801:Humans; D007004:Hypoglycemic Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use* / Q000633:toxicity; D010330:Patents as Topic; D013329:Structure-Activity Relationship
D004151:Dipeptides; D054873:Dipeptidyl-Peptidase IV Inhibitors; D007004:Hypoglycemic Agents; C502994:saxagliptin; D000218:Adamantane