Chemistry:ERA-63
From HandWiki
Short description: Chemical compound
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| Other names | 3-Methylene-7α-methylethinylestradiol; 3-Methylene-7α-methyl-17α-ethynylestra-5(10)-en-17β-ol[1] |
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| Formula | C22H30O |
| Molar mass | 310.481 g·mol−1 |
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ERA-63, also known as ORG-37663, as well as 3-methylene-7α-methyl-17α-ethynylestra-5(10)-en-17β-ol, is a synthetic, steroidal estrogen and a selective agonist of the ERα that was under development for the treatment of rheumatoid arthritis but was never marketed.[2][1] The drug produced estrogenic effects but failed to show effectiveness for rheumatoid arthritis in a phase IIa clinical study.[3][4] A large clinical trial also found that prinaberel (ERB-041), a selective ERβ agonist, was ineffective in the treatment of rheumatoid arthritis in spite of activity in preclinical models.[4]
See also
References
- ↑ 1.0 1.1 "The evaluation of the immunomodulating properties of ERA-63 a pharmaceutical with estrogenic activity". Toxicol. Lett. 180 (3): 196–201. 2008. doi:10.1016/j.toxlet.2008.06.857. PMID 18602456.
- ↑ "A selective estrogen receptor alpha agonist (Org 37663) suppresses inflammation and arthritis in mouse models". Annals of the Rheumatic Diseases 65: 128. 2006.
- ↑ "The selective estrogen receptor alpha agonist Org 37663 induces estrogenic effects but lacks antirheumatic activity: a phase IIa trial investigating efficacy and safety of Org 37663 in postmenopausal female rheumatoid arthritis patients receiving stable background methotrexate or sulfasalazine". Arthritis Rheum. 62 (2): 351–8. 2010. doi:10.1002/art.27196. PMID 20112368.
- ↑ 4.0 4.1 "Selective estrogen receptor agonism lacks clinical benefit in rheumatoid arthritis: comment on the article by van Vollenhoven et al". Arthritis Rheum. 62 (12): 3832–3. 2010. doi:10.1002/art.27722. PMID 21120998.
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