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*

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


*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.

Roman-Blas et al. Arthritis Research & Therapy 2009 11:241   doi:10.1186/ar2791