PMID- 15618247
OWN - NLM
STAT- MEDLINE
DCOM- 20050630
LR  - 20050324
IS  - 0268-1161 (Print)
IS  - 0268-1161 (Linking)
VI  - 20
IP  - 4
DP  - 2005 Apr
TI  - A selective estrogen receptor-beta agonist causes lesion regression in an 
      experimentally induced model of endometriosis.
PG  - 936-41
AB  - BACKGROUND: Endometriosis is a common gynaecological problem of uncertain 
      aetiology. It affects primarily young, reproductive-aged women and can result in 
      chronic pelvic pain and infertility. Current approved therapies have significant 
      side-effects and hysterectomy is employed as a final solution. ERB-041 is a 
      selective estrogen receptor-beta (ERbeta) agonist that has anti-inflammatory 
      activity in preclinical models of arthritis and inflammatory bowel disease, but 
      is inactive in many preclinical models of classic estrogen activity. Because 
      endometriosis is now thought to be, at least in part, an inflammatory disease, we 
      evaluated ERB-041's activity in an experimentally induced model of endometriosis. 
      METHODS: Athymic nude mice (ovariectomized or intact) were implanted with tissue 
      fragments of normal human endometrium. After establishment of lesions for 11-14 
      days, mice were treated with ERB-041 for 15-17 days. Upon euthanasia, the number 
      of lesions, their size and location were noted. Five lesions were recovered for 
      RNA analysis. RESULTS: Across six studies, ERB-041 caused complete lesion 
      regression in 40-75% of the mice studied. The compound appeared to be equally 
      effective in gonad-intact as in ovariectomized mice, and analysed recovered 
      lesions expressed ERalpha but not ERbeta mRNA. CONCLUSIONS: ERB-041 and possibly 
      other ERbeta selective agonists may be a useful new approach to treating 
      endometriosis.
FAU - Harris, Heather A
AU  - Harris HA
AD  - Women's Health Research Institute, Wyeth Research, Collegeville, PA 19426, USA. 
      harrish@wyeth.com
FAU - Bruner-Tran, Kaylon L
AU  - Bruner-Tran KL
FAU - Zhang, Xiaochun
AU  - Zhang X
FAU - Osteen, Kevin G
AU  - Osteen KG
FAU - Lyttle, C Richard
AU  - Lyttle CR
LA  - eng
PT  - Journal Article
DEP - 20041223
PL  - England
TA  - Hum Reprod
JT  - Human reproduction (Oxford, England)
JID - 8701199
RN  - 0 (ERB 041)
RN  - 0 (Estrogen Receptor beta)
RN  - 0 (Oxazoles)
RN  - 0 (RNA, Messenger)
SB  - IM
MH  - Adolescent
MH  - Adult
MH  - Animals
MH  - Biopsy
MH  - Disease Models, Animal
MH  - Endometriosis/*drug therapy/pathology
MH  - Endometrium/*drug effects/pathology
MH  - Estrogen Receptor beta/*agonists/genetics
MH  - Female
MH  - Humans
MH  - Mice
MH  - Mice, Nude
MH  - Middle Aged
MH  - Organ Culture Techniques
MH  - Ovariectomy
MH  - Oxazoles/chemistry/*pharmacology
MH  - RNA, Messenger/analysis
EDAT- 2004/12/25 09:00
MHDA- 2005/07/01 09:00
CRDT- 2004/12/25 09:00
PHST- 2004/12/25 09:00 [pubmed]
PHST- 2005/07/01 09:00 [medline]
PHST- 2004/12/25 09:00 [entrez]
AID - deh711 [pii]
AID - 10.1093/humrep/deh711 [doi]
PST - ppublish
SO  - Hum Reprod. 2005 Apr;20(4):936-41. doi: 10.1093/humrep/deh711. Epub 2004 Dec 23.