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[摘要]：Importance of the field: PPAR-gamma 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 PPAR-gamma modulators (SPPAR-gamma Ms) as safer alternatives to PPAR-gamma full agonists. Areas covered in this review: This review focuses on the preclinical and clinical data of all the SPPAR-gamma Ms 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 SPPAR-gamma Ms' mode of action, briefly examine new ways to identify superior SPPAR-gamma Ms, 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 PPAR-gamma modulators have the potential to become the next generation of PPAR-gamma agonists: effective insulin sensitizers with a superior safety profile to that of PPAR-gamma full agonists. |
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