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Musculoskeletal disease


Peroxisome proliferation-activated receptor-d (PPARD; PPARd)

In vitro and mouse studies suggest activating PPARd could help treat osteoporosis. In cocultured osteoblasts and osteoclasts, pharmacological activation of PPARd with GW501516 increased osteoblast differentiation and decreased osteoclastogenesis compared with no activation. In a mouse model for postmenopausal osteoporosis, GW501516 restored bone turnover and increased bone density to normal levels compared with vehicle. Next steps include studies to determine if a PPARd agonist could be used to treat osteoporosis in patients.
At least five companies have PPARd agonists in clinical and preclinical testing to treat endocrine and metabolic conditions.
GlaxoSmithKline plc discontinued development of GW501516 after finding the molecule induced tumors in rodents. The compound had completed a Phase II trial in patients with dyslipidemia.

SciBX 6(16); doi:10.1038/scibx.2013.392
Published online April 25, 2013

Findings unpatented; available for licensing

Scholtysek, C. et al. Nat. Med.; published online March 31, 2013;
Contact: Gerhard Krönke, University of Erlangen-Nuremberg, Erlangen, Germany