ERA-63, also known as ORG-37663, as well as 3-methylene-7α-methyl-17α-ethynylestra-5(10)-en-17β-ol, is a synthetic, steroidalestrogen and a selectiveagonist 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 IIaclinical 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 preclinicalmodels.[4]
^ abJanssen GB, Penninks AH, Knippels LM, van Zijverden M, Spanhaak S (2008). "The evaluation of the immunomodulating properties of ERA-63 a pharmaceutical with estrogenic activity". Toxicol. Lett. 180 (3): 196–201. doi:10.1016/j.toxlet.2008.06.857. PMID 18602456.
^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.
^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 (2010). "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. doi:10.1002/art.27196. PMID 20112368.
^ abCutolo M (2010). "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. doi:10.1002/art.27722. PMID 21120998.
This article about a steroid is a stub. You can help Wikipedia by expanding it.
also, known, 37663, well, methylene, methyl, 17α, ethynylestra, 17β, synthetic, steroidal, estrogen, selective, agonist, erα, that, under, development, treatment, rheumatoid, arthritis, never, marketed, drug, produced, estrogenic, effects, failed, show, effect. ERA 63 also known as ORG 37663 as well as 3 methylene 7a methyl 17a ethynylestra 5 10 en 17b ol is a synthetic steroidal estrogen and a selective agonist of the ERa 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 ERb agonist was ineffective in the treatment of rheumatoid arthritis in spite of activity in preclinical models 4 ERA 63Clinical dataOther names3 Methylene 7a methylethinylestradiol 3 Methylene 7a methyl 17a ethynylestra 5 10 en 17b ol 1 IdentifiersIUPAC name 7R 8R 9S 13S 14S 17R 17 Ethynyl 7 13 dimethyl 3 methylidene 1 2 4 6 7 8 9 11 12 14 15 16 dodecahydrocyclopenta a phenanthren 17 olPubChem CID87921126ChemSpider8058857Chemical and physical dataFormulaC 22H 30OMolar mass310 481 g mol 13D model JSmol Interactive imageSMILES C C H 1CC2 C CCC C C2 C H 3 C H 1 C H 4CC C C 4 CC3 C C C OInChI InChI 1S C22H30O c1 5 22 23 11 9 19 20 15 3 13 16 12 14 2 6 7 17 16 18 20 8 10 21 19 22 4 h1 15 18 20 23H 2 6 13H2 3 4H3 t15 18 19 20 21 22 m1 s1Key ITYURVXIFIQGDB LADQHVHVSA NSee also edit16a LE2 ERA 45 GTx 758 Methylpiperidinopyrazole PropylpyrazoletriolReferences edit a b Janssen GB Penninks AH Knippels LM van Zijverden M Spanhaak S 2008 The evaluation of the immunomodulating properties of ERA 63 a pharmaceutical with estrogenic activity Toxicol Lett 180 3 196 201 doi 10 1016 j toxlet 2008 06 857 PMID 18602456 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 van Vollenhoven RF Houbiers JG Buttgereit F In t Hout J Boers M Leij S Kvien TK Dijkmans BA Szczepanski L Szombati I Sierakowski S Miltenburg AM 2010 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 doi 10 1002 art 27196 PMID 20112368 a b Cutolo M 2010 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 doi 10 1002 art 27722 PMID 21120998 nbsp This article about a steroid is a stub You can help Wikipedia by expanding it vte nbsp This drug article relating to the genito urinary system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title ERA 63 amp oldid 1125839003, wikipedia, wiki, book, books, library,
