Regulation of bone regeneration with approved small molecule compounds

Stimulation of bone formation using recombinant growth factors has been a promising strategy for bone repair and regeneration. However, small molecules have been suggested as alternatives to recombinant protein-based treatments because of their unique advantages. To date, therapeutic methods for orthopaedic applications still heavily rely on therapeutic protein-based growth factors. This trend is likely to be reversed since innovative drug discovery strategies, such as broad-spectrum database analysis and high throughput functional screens, have led to the discovery of many novel small molecule compounds and the development of novel applications of existing approved small molecule compounds. It should be noted that some of these small molecules with osteoinductive potential have been approved for human use due to their efficacy in treating other health ailments. Thus, these approved small molecule compounds are highly translatable to orthopaedic applications. In this article, we review the literature, paying attention to the prospects of existing approved small molecule therapeutics with bone regenerative capacity. Future directions of bone repair and regeneration using these approved small molecule drugs will be discussed as well. Keywords: small molecules; bone regeneration; drug discovery (Published: 26 September 2014) Citation: Advances in Regenerative Biology 2014, 1 : 25276 - http://dx.doi.org/10.3402/arb.v1.25276 Abstract in popular science Skeletal diseases and injuries, such as bone fractures, affect a significant portion of the population. While several protein-based medications are currently approved for the treatment of skeletal disorders via bone repair and regeneration, it is known that these protein-based therapeutics can cause significant side-effects. An alternative to protein-based pharmaceuticals is urgently needed in order for the therapeutics to be safer, more effective, and more affordable. Small molecule-based drugs are more appealing for treating bone diseases because they are more affordable, more stable, and require a smaller dosage to achieve a bone regenerative effect. Interestingly, some small molecule drugs that are already being prescribed to treat a variety of medical conditions have shown potential to be used as therapeutics for bone repair and regeneration. This review article provides a summary of recent findings of approved small molecule compounds with bone regenerative capability.