| Aleglitazar, a dual PPARα and PPARγ agonist for the potential oral treatment of type 2 diabetes mellitus. | |
| | |
MedLine Citation:
|
PMID: 21046527 Owner: NLM Status: In-Process |
Abstract/OtherAbstract:
|
PPARγ and PPARα are nuclear receptors mainly involved in the regulation of glucose homeostasis and lipid levels, respectively. Aleglitazar, being developed by Roche Holding, is a dual agonist for PPARγ and PPARα for the potential simultaneous treatment of hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus (T2DM). In preclinical studies, aleglitazar decreased non-fasted glucose levels, increased glucose clearance and improved insulin resistance, while also increasing HDL-cholesterol and decreasing LDL-cholesterol levels in serum. In phase I and II clinical trials in patients with T2DM, aleglitazar demonstrated beneficial antidiabetic activities and had a higher antihyperglycemic efficacy than pioglitazone (a PPARγ agonist). Aleglitazar improved the lipid profile in patients and decreased levels of cardiovascular markers of inflammation and clotting. The observed adverse events were characteristic of either PPARγ or PPARα agonists; however, when compared to pioglitazone-PPARγ-mediated effects, such as edema and weight gain, these were less severe. PPARγ-mediated adverse events on bone have not been measured and should be addressed in the future. The PPARα-mediated adverse effects on renal function are of concern and are a primary endpoint of ongoing phase II clinical trials in patients with T2DM. A phase III clinical trial was also ongoing in patients with T2DM who had recently experienced a cardiac event. |
| | |
Authors:
|
Beata Lecka-Czernik |
Related Documents
:
|
9100707 - Elevated fasting plasma insulin in a general aged population: an innocent companion of ... 4061967 - Validity of out-patient screening in arteriosclerosis to identify multiple lesions. 19954687 - The eurodiab study: what has this taught us about diabetic peripheral neuropathy? 11554777 - Prospects for predicting and stopping the development of type 1 of diabetes. 18846477 - Renal tubulointerstitial expansion is associated with endothelial dysfunction and infla... 18414077 - Sudden onset of diabetic ketoacidosis during consensus interferon therapy for chronic v... |
Publication Detail:
|
Type: Journal Article |
Journal Detail:
|
Title: IDrugs : the investigational drugs journal Volume: 13 ISSN: 2040-3410 ISO Abbreviation: IDrugs Publication Date: 2010 Nov |
Date Detail:
|
Created Date: 2010-11-03 Completed Date: - Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 100883655 Medline TA: IDrugs Country: England |
Other Details:
|
Languages: eng Pagination: 793-801 Citation Subset: IM |
Affiliation:
|
University of Toledo, College of Medicine, Department of Orthopaedic Surgery, 3000 Arlington Avenue, Toledo, OH 43614, USA. beata.leckaczernik@utoledo.edu |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Lixivaptan, a non-peptide vasopressin V2 receptor antagonist for the potential oral treatment of hyp...
Next Document: [Cochrane reviews. Are coated stents really more effective?].