LGND's partners and collaborators (LLY, GLX, Dana Farber Institute at Harvard) will also be presenting at an upcoming diabetes conference. Here's what GLX has to say about rexinoid agonists (like Targretin. LGD1268, or LGD1324):
Regulation of Adipocyte Metabolism using Multiple Insulin Sensitizers: A Role for PPARg, RXR and b-3 Adrenoreceptor Agonists for Treating NIDDM
James M. Lenhard, Ph.D., Research Investigator II, Metabolic Diseases, Glaxo Wellcome
Given the pleiotropic nature of diabetes, multiple agents are needed to treat the disease. We show antidiabetic PPARg and RXR agonists act synergistically to increase adipocyte differentiation and b3g-adrenoreceptor mediated lipolysis in vitro. In vivo, these agents improved glycemic control in diabetic mice suffering from pancreatic islet degeneration. Although PPARg agonists were more effective at decreasing serum lipids and preventing diabetic cachexia, the RXR agonists were more effective at causing hepatotomigaly in mice. In combination, PPARg agonists improved the antidiabetic efficacy of RXR agonists. Furthermore, PPARg agonists increased b3-adrenoreceptor mediated thermogenesis in these mice, which may explain the antidiabetic effect of these agents |