Biology and toxicology of PPARγ ligands

Abstract

The peroxisome proliferator activated receptor-gamma (PPARγ) is an attractive target for therapeutic intervention, as modulation of PPARγ-regulated pathways is potentially beneficial in a number of disease areas. This review provides an overview of what is known about the biology of PPARγ, and an indication of what progress has been made towards drug development in several therapy areas. As well as efficacy, the safety of drugs is of course an important issue, and a substantial volume of preclinical and clinical information has already accumulated for PPARγ agonists. Here we discuss some of the major toxicology issues with PPARγ agonists, and give a perspective on likely issues concerning the development of PPARγ modulators in the future.