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Table 1 Partial list of selective estrogen receptor modulators and selective estrogen receptor ligands in clinical development

From: Osteoarthritis associated with estrogen deficiency

Pharmacologic group Compound name ER action (main target tissues) Indications and stage of development
Chloroethylene Clomiphene ER antagonist (brain) Ovulation induction*
Triphenylethylenes Tamoxifen ER antagonist (breast) Breast cancer therapy and prevention*
   ER agonist (bone, uterus and serum cholesterol) Beneficial effects on BMD
    Beneficial cartilage effect. Animal models
  Toremifene Similar to tamoxifen Breast cancer therapy and prevention*
  Ospemifene Similar to tamoxifen Vaginal atrophy. Phase III
Benzothiophenes Raloxifene ER antagonist (breast) OP therapy and prevention*
   ER agonist (bone and serum cholesterol) Breast cancer therapy and prevention*
  Arzoxifene ER antagonist (breast and uterus) OP therapy and prevention. Phase III
   ER agonist (bone and serum cholesterol) Breast and uterine cancer therapy. Phase II
Naphthalenes Lasofoxifene ER agonist (bone and serum cholesterol) OP treatment. Phase III
   High bioavailability Vaginal atrophy. Phase III
Indoles Pipendoxifene ER antagonist (breast) Breast cancer therapy. Phase II
  Bazedoxifene ER agonist (bone and blood lipids) OP treatment and prevention. Phase III
Hydroxy-chromanes NNC 45-0781 Tissue-selective partial ER agonists Postmenopausal OP prevention. Preclinical
    Beneficial cartilage effect. Animal models
  NNC 45-0320   
  NNC 45-1506   
Steroidals HMR-3339 ER agonist (bone and serum cholesterol) Decrease serum cholesterol. Phase II
    Postmenopausal OP treatment. Preclinical
  Fulvestrant Steroid ER antagonist (breast) Refractory breast cancer
Selective ER ligands Pinaberel (ERB-041) ERβ-selective agonist Chronic arthritis/endometriosis. Phase II
  WAY-169916 NF-κB activity inhibition. No classical ER action Anti-inflammatory. Preclinical studies
  WAY-204688 Similar to WAY-169916  
  1. *Products currently on the market. Levormeloxifen, a discontinued selective estrogen receptor modulator, also showed beneficial effects on cartilage in an animal model. BMD, bone mineral density; ER, estrogen receptor; OP, osteoporosis.