setrusumab

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Ligands
setrusumab

GtoPdb Ligand ID: 9202

Synonyms: BPS 804 | BPS804 | UX-143 | UX143

Comment: Setrusumab (BPS-804) is a fully human investigational monoclonal antibody targeting sclerostin (SOST; which is a negative regulator of bone formation), that is intended to improve bone density.
Development of anti-sclerostin antibodies by Novartis is claimed in patent WO2009047356 [2], although we cannot definitively conclude that BPS-804 is claimed within that patent application.
The potential of sclerostin as a therapeutic target in bone diseases is reviewed by Lewiecki (2014) [3].

References
1. Ellies DL, Viviano B, McCarthy J, Rey JP, Itasaki N, Saunders S, Krumlauf R. (2006) Bone density ligand, Sclerostin, directly interacts with LRP5 but not LRP5G171V to modulate Wnt activity. J Bone Miner Res, 21 (11): 1738-49. [PMID:17002572]
2. Kneissel M, Halleux C, Hu S-I, Diefenbach-Streiber B, Prassler J. (2009) Compositions and methods for use for antibodies against sclerostin. Patent number: WO2009047356. Assignee: Novartis Ag. Priority date: 12/08/2007. Publication date: 16/04/2009.
3. Lewiecki EM. (2014) Role of sclerostin in bone and cartilage and its potential as a therapeutic target in bone diseases. Ther Adv Musculoskelet Dis, 6 (2): 48-57. [PMID:24688605]
4. Li X, Ominsky MS, Warmington KS, Morony S, Gong J, Cao J, Gao Y, Shalhoub V, Tipton B, Haldankar R et al.. (2009) Sclerostin antibody treatment increases bone formation, bone mass, and bone strength in a rat model of postmenopausal osteoporosis. J Bone Miner Res, 24 (4): 578-88. [PMID:19049336]
5. Li X, Zhang Y, Kang H, Liu W, Liu P, Zhang J, Harris SE, Wu D. (2005) Sclerostin binds to LRP5/6 and antagonizes canonical Wnt signaling. J Biol Chem, 280 (20): 19883-7. [PMID:15778503]
6. Ominsky MS, Vlasseros F, Jolette J, Smith SY, Stouch B, Doellgast G, Gong J, Gao Y, Cao J, Graham K et al.. (2010) Two doses of sclerostin antibody in cynomolgus monkeys increases bone formation, bone mineral density, and bone strength. J Bone Miner Res, 25 (5): 948-59. [PMID:20200929]

References

1. Ellies DL, Viviano B, McCarthy J, Rey JP, Itasaki N, Saunders S, Krumlauf R. (2006)
Bone density ligand, Sclerostin, directly interacts with LRP5 but not LRP5G171V to modulate Wnt activity.
J Bone Miner Res, 21 (11): 1738-49. [PMID:17002572]

2. Kneissel M, Halleux C, Hu S-I, Diefenbach-Streiber B, Prassler J. (2009)
Compositions and methods for use for antibodies against sclerostin.
Patent number: WO2009047356. Assignee: Novartis Ag. Priority date: 12/08/2007. Publication date: 16/04/2009.

3. Lewiecki EM. (2014)
Role of sclerostin in bone and cartilage and its potential as a therapeutic target in bone diseases.
Ther Adv Musculoskelet Dis, 6 (2): 48-57. [PMID:24688605]

4. Li X, Ominsky MS, Warmington KS, Morony S, Gong J, Cao J, Gao Y, Shalhoub V, Tipton B, Haldankar R et al.. (2009)
Sclerostin antibody treatment increases bone formation, bone mass, and bone strength in a rat model of postmenopausal osteoporosis.
J Bone Miner Res, 24 (4): 578-88. [PMID:19049336]

5. Li X, Zhang Y, Kang H, Liu W, Liu P, Zhang J, Harris SE, Wu D. (2005)
Sclerostin binds to LRP5/6 and antagonizes canonical Wnt signaling.
J Biol Chem, 280 (20): 19883-7. [PMID:15778503]

6. Ominsky MS, Vlasseros F, Jolette J, Smith SY, Stouch B, Doellgast G, Gong J, Gao Y, Cao J, Graham K et al.. (2010)
Two doses of sclerostin antibody in cynomolgus monkeys increases bone formation, bone mineral density, and bone strength.
J Bone Miner Res, 25 (5): 948-59. [PMID:20200929]