Small Molecules to Promote Bone Growth


Small molecule sclerostin-inhibitors to enhance the canonical Wnt pathways and promote BMP-induced osteoblast differentiation.

Key Benefits

  • Repurposing opportunities of FDA approved drugs.
  • Lower cost compared to currently available monoclonal antibody or recombinant protein therapies.
  • Stable compounds with established safety profiles in humans that are easier and cheaper to manufacture compared to current technologies.

Market Summary

Regenerative therapies for bone can improve medical outcomes and enhance quality of life. The current strategies in orthopedic surgeries are bone grafting and recombinant human (rh) BMP treatment. The grafting of autologous bone (the current 'gold standard') requires bone sample extraction from patients, causing serious long-term extraction pain. The other commonly used option, local delivery of rhBMP2, an osteoinductive agent, is very expensive and has been associated with adverse side effects, such as seroma formation, bone outgrowth and increased risk of cancer. Therefore, more efficient, safer and lower-cost methods for osteogenesis are needed.

Technical Summary

Emory researchers have discovered repurposing opportunities of FDA-approved small molecules, fluticasone (F1) and valproic acid (VA1), as osteoinductive agents. F1 and VA1 act as inhibitors of sclerostin, an antagonist of the canonical Wnt signaling pathway, to increase BMP efficiency in promoting osteogenesis. In vitro and in vivo experiments showed that these sclerostin-inhibitors synergistically promoted osteoblast differentiation and result in de novo bone formation by enhancing canonical Wnt signaling and BMP signaling intensity and duration. These small molecule inhibitors are stable compounds and easy to use without specialized delivery carriers. In addition, these molecules are cheaper than currently available treatment options. These small molecules may also be applicable in treatment of fractures and osteoporosis.

Developmental Stage

These small molecule sclerostin-inhibitors were tested in vitro and in vivo.

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Patent Information

App Type Country Serial No. Patent No. File Date Issued Date Patent Status
Nationalized PCT - United States United States 17/428,556   8/4/2021   Pending
Nationalized PCT - Foreign EP 20752345.7   9/3/2021   Pending
Tech ID: 19012
Published: 12/3/2019