Table 1 |
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Partial list of selective estrogen receptor modulators and selective estrogen receptor ligands in clinical development |
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Pharmacologic group |
Compound name |
ER action (main target tissues) |
Indications and stage of development |
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Chloroethylene |
Clomiphene |
ER antagonist (brain) |
Ovulation induction* |
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Triphenylethylenes |
Tamoxifen |
ER antagonist (breast) |
Breast cancer therapy and prevention* |
|
ER agonist (bone, uterus and serum cholesterol) |
Beneficial effects on BMD |
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Beneficial cartilage effect. Animal models |
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Toremifene |
Similar to tamoxifen |
Breast cancer therapy and prevention* |
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Ospemifene |
Similar to tamoxifen |
Vaginal atrophy. Phase III |
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Benzothiophenes |
Raloxifene |
ER antagonist (breast) |
OP therapy and prevention* |
|
ER agonist (bone and serum cholesterol) |
Breast cancer therapy and prevention* |
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Arzoxifene |
ER antagonist (breast and uterus) |
OP therapy and prevention. Phase III |
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ER agonist (bone and serum cholesterol) |
Breast and uterine cancer therapy. Phase II |
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Naphthalenes |
Lasofoxifene |
ER agonist (bone and serum cholesterol) |
OP treatment. Phase III |
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High bioavailability |
Vaginal atrophy. Phase III |
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Indoles |
Pipendoxifene |
ER antagonist (breast) |
Breast cancer therapy. Phase II |
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Bazedoxifene |
ER agonist (bone and blood lipids) |
OP treatment and prevention. Phase III |
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Hydroxy-chromanes |
NNC 45-0781 |
Tissue-selective partial ER agonists |
Postmenopausal OP prevention. Preclinical |
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Beneficial cartilage effect. Animal models |
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NNC 45-0320 |
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NNC 45-1506 |
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Steroidals |
HMR-3339 |
ER agonist (bone and serum cholesterol) |
Decrease serum cholesterol. Phase II |
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Postmenopausal OP treatment. Preclinical |
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Fulvestrant |
Steroid ER antagonist (breast) |
Refractory breast cancer |
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Selective ER ligands |
Pinaberel (ERB-041) |
ERβ-selective agonist |
Chronic arthritis/endometriosis. Phase II |
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WAY-169916 |
NF-κB activity inhibition. No classical ER action |
Anti-inflammatory. Preclinical studies |
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WAY-204688 |
Similar to WAY-169916 |
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*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. |
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Roman-Blas et al. Arthritis Research & Therapy 2009 11:241 doi:10.1186/ar2791 |
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