| Autor: |
Doshi, Lalit S, Brahma, Manoja Kumar, Bahirat, Umakant A, Dixit, Amol V, Nemmani, Kumar VS |
| Zdroj: |
Expert Opinion on Investigational Drugs; January 2010, Vol. 19 Issue: 4 p489-512, 24p |
| Abstrakt: |
Importance of the field:PPARγγ full agonists (pioglitazone and rosiglitazone) are the mainstay drugs for the treatment of type 2 diabetes; however, mechanism-based side effects have limited their full therapeutic potential. In recent years, much progress has been achieved in the discovery and development of selective PPARγγ modulators (SPPARγγMs) as safer alternatives to PPARγγ full agonists.Areas covered in this review:This review focuses on the preclinical and clinical data of all the SPPARγγMs discovered so far, retrieved by searching PubMed, Prous Integrity database and company news updates from 1999 to date.What the reader will gain:Here we thoroughly discuss SPPARγγMs' mode of action, briefly examine new ways to identify superior SPPARγγMs, and finally, compare and contrast the pharmacological and safety profile of various agents.Take home message:The preclinical and clinical findings clearly suggest that selective PPARγγ modulators have the potential to become the next generation of PPARγγ agonists: effective insulin sensitizers with a superior safety profile to that of PPARγγ full agonists. |
| Databáze: |
Supplemental Index |
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