Table 1 Partial list of selective estrogen receptor modulators and selective estrogen receptor ligands in clinical development
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* |
| Â | Â | ER agonist (bone, uterus and serum cholesterol) | Beneficial effects on BMD |
| Â | Â | Â | Beneficial cartilage effect. Animal models |
| Â | Toremifene | Similar to tamoxifen | Breast cancer therapy and prevention* |
| Â | Ospemifene | Similar to tamoxifen | Vaginal atrophy. Phase III |
Benzothiophenes | Raloxifene | ER antagonist (breast) | OP therapy and prevention* |
| Â | Â | ER agonist (bone and serum cholesterol) | Breast cancer therapy and prevention* |
| Â | Arzoxifene | ER antagonist (breast and uterus) | OP therapy and prevention. Phase III |
| Â | Â | 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 |
| Â | Â | High bioavailability | Vaginal atrophy. Phase III |
Indoles | Pipendoxifene | ER antagonist (breast) | Breast cancer therapy. Phase II |
| Â | 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 |
| Â | Â | Â | Beneficial cartilage effect. Animal models |
| Â | NNC 45-0320 | Â | Â |
| Â | NNC 45-1506 | Â | Â |
Steroidals | HMR-3339 | ER agonist (bone and serum cholesterol) | Decrease serum cholesterol. Phase II |
| Â | Â | Â | Postmenopausal OP treatment. Preclinical |
| Â | 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 |
| Â | WAY-204688 | Similar to WAY-169916 | Â |