This technology is a therapeutic treatment for osteoporosis that increases bone formation through the use of peripheral serotonin inhibitors.
Unmet Need: A safe therapeutic agent for increasing bone mass
Current medical approaches for treating osteoporosis aim at preventing initial bone deterioration and reducing the rate of loss after diagnosis. Few medications are capable of rebuilding bone density after it has been lost. Therefore, further efforts are needed to identify treatments capable not only of maintaining bone mass, but also of increasing bone formation in order to restore a healthy bone density.
The Technology: Therapeutic treatment for increasing bone formation
This technology identifies strategies that effectively reduce serum serotonin levels, which results in increased osteoblast proliferation and bone formation. Peripheral serotonin is synthesized by the TPH1 enzyme and regulates bone density through 5-HT1B, a serotonin receptor found in osteoblasts. Inhibiting 5-HT1B or TPH1 lowers serum serotonin levels and induces bone formation, resulting in increased bone mass. Serotonin antagonists can thus effectively rebuild lost bone density in osteoporosis patients and offer an attractive therapeutic option for the treatment of osteoporosis and other bone-related disorders.
This technology has been validated using mouse models for bone loss, with inhibition of serotonin being found to increase bone mass.
Applications:
- Regulation of serum serotonin levels
- Therapeutic for increasing bone formation and density in osteoporosis and other bone mass disorders
- Treatment for preventing bone loss in patients undergoing SSRI therapy
Advantages:
- Increases bone formation
- Rebuilds lost bone mass
- Selectively decreases serum serotonin levels
- Clearly defined pathway and mechanism of action
- Presents a unique strategy for osteoporosis treatment
Lead Inventor:
Gerard Karsenty, M.D., Ph.D.
Patent Information:
Patent Status
Related Publications:
Inose H, Zhou B, Yadav VK, Guo XE, Karsenty G, Ducy P. “Efficacy of serotonin inhibition in mouse models of bone loss’ J Bone Miner Res. 2011 Sep; (26)9: 2002-2011.
Yadav VK, Balaji S, Suresh PS, Liu XS, Lu X, Li Z, Guo XE, Mann JJ, Balapure AK, Gershon MD, Medhamurthy R, Vidal M, Karsenty G, Ducy P. “Pharmacological inhibition of gut-derived serotonin synthesis is a potential bone anabolic treatment for osteoporosis” Nat Med. 2010 Mar; (16)3: 308-312.
Yadav VK, Ryu JH, Suda N, Tanaka KF, Gingirch JA, Shutz G, Glorieux FH, Chiang CY, Zajaz JD, Insigna KL, Mann JJ, Hen R, Ducy P, Karsenty G. “Lrp5 controls bone formation by inhibiting serotonin sunthesis in the duodenum” Cell. 2008 Nov 28; 135(5): 825-837.
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