ERA-63 explained
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.[1] [2] 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.
See also
Notes and References
- Dulos J, Hofstra CL, Joosten L, Veening-Griffioen DH, Lucassen MA, Doorn CM, Graaf JH, Miltenburg A, Dijcks FA, Ederveen TH, Boots AM . 2006 . A selective estrogen receptor alpha agonist (Org 37663) suppresses inflammation and arthritis in mouse models . Annals of the Rheumatic Diseases . 65 . 128 .
- Janssen GB, Penninks AH, Knippels LM, van Zijverden M, Spanhaak S . The evaluation of the immunomodulating properties of ERA-63 a pharmaceutical with estrogenic activity . Toxicol. Lett. . 180 . 3 . 196–201 . 2008 . 18602456 . 10.1016/j.toxlet.2008.06.857 .
- van Vollenhoven RF, Houbiers JG, Buttgereit F, In 't Hout J, Boers M, Leij S, Kvien TK, Dijkmans BA, Szczepański L, Szombati I, Sierakowski S, Miltenburg AM . 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 . 20112368 . 10.1002/art.27196 .
- Cutolo M . 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 . 21120998 . 10.1002/art.27722 . free .
